Target Information

Target General Information

Top

Target ID

T92072 (Former ID: TTDS00186)

Target Name

Adenosine A1 receptor (ADORA1)

Synonyms

Adenosine receptor A1; A(1) adenosine receptor

Click to Show/Hide

Gene Name

ADORA1

Target Type

Successful target

[1]

Disease

[+] 1 Target-related Diseases

Orthostatic hypotension [ICD-11: BA21]

Function

The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Receptor for adenosine.

Click to Show/Hide

BioChemical Class

GPCR rhodopsin

UniProt ID

AA1R_HUMAN

Sequence

MPPSISAFQAAYIGIEVLIALVSVPGNVLVIWAVKVNQALRDATFCFIVSLAVADVAVGA
LVIPLAILINIGPQTYFHTCLMVACPVLILTQSSILALLAIAVDRYLRVKIPLRYKMVVT
PRRAAVAIAGCWILSFVVGLTPMFGWNNLSAVERAWAANGSMGEPVIKCEFEKVISMEYM
VYFNFFVWVLPPLLLMVLIYLEVFYLIRKQLNKKVSASSGDPQKYYGKELKIAKSLALIL
FLFALSWLPLHILNCITLFCPSCHKPSILTYIAIFLTHGNSAMNPIVYAFRIQKFRVTFL
KIWNDHFRCQPAPPIDEDLPEERPDD

Click to Show/Hide

3D Structure

Click to Show 3D Structure of This Target

PDB

ADReCS ID

BADD_A01328 ; BADD_A01334

HIT2.0 ID

T35LKG

Drugs and Modes of Action

Top

Approved Drug(s)

[+] 1 Approved Drugs

Caffeine

Drug Info

Approved

Orthostatic hypotension

[2], [3]

Clinical Trial Drug(s)

[+] 10 Clinical Trial Drugs

AMP-579

Drug Info

Phase 2

Hyperlipidaemia

[6]

Apaxifylline

Drug Info

Phase 2

Cognitive impairment

[7]

BAY 1067197

Drug Info

Phase 2

Heart failure

[8]

Capadenoson

Drug Info

Phase 2

Atrial fibrillation

[9]

DTI-0009

Drug Info

Phase 2

Atrial fibrillation

[10]

SELODENOSON

Drug Info

Phase 2

Cardiac arrhythmias

[10]

SLV320

Drug Info

Phase 2

Heart failure

[11], [12]

Tonapofylline

Drug Info

Phase 2

Acute and chronic heart failure

[13]

INO-8875

Drug Info

Phase 1/2

Glaucoma/ocular hypertension

[14]

KF-17837

Drug Info

Phase 1

Parkinson disease

[18]

Discontinued Drug(s)

[+] 9 Discontinued Drugs

CVT-124

Drug Info

Discontinued in Phase 3

Autoimmune diabetes

[19]

N-0861

Drug Info

Discontinued in Phase 3

Cardiac disease

[20]

Tecadenoson

Drug Info

Discontinued in Phase 3

Cardiac arrhythmias

[21], [22]

BRL-61063

Drug Info

Discontinued in Phase 2

Allergy

[24]

FK-352

Drug Info

Discontinued in Phase 2

Hypertension

[25]

FK-453

Drug Info

Discontinued in Phase 2

Renal failure

[26], [27]

FK-838

Drug Info

Discontinued in Phase 2

Hypertension

[28]

SDZ-WAG-994

Drug Info

Discontinued in Phase 1

Hypertension

[31]

METHYLTHIOADENOSINE

Drug Info

Terminated

Multiple sclerosis

[33]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

BAY 60-6583

Drug Info

Preclinical

Myocardial ischemia

[32]

Mode of Action

[+] 4 Modes of Action

Antagonist

[+] 37 Antagonist drugs

Caffeine

Drug Info

[1], [34]

Apaxifylline

Drug Info

[36]

SLV320

Drug Info

[12]

CVT-124

Drug Info

[48], [49]

N-0861

Drug Info

[50]

FK-352

Drug Info

[52]

(E)-8-(3-chlorostyryl)-caffeine

Drug Info

[61]

4-Ethoxy-7-((E)-styryl)-furo[3,2-g]chromen-5-one

Drug Info

[90]

8-cyclopentyltheophylline

Drug Info

[96]

AS100

Drug Info

[101]

AS70

Drug Info

[101]

AS99

Drug Info

[101]

ATL802

Drug Info

[102]

CPFPX

Drug Info

[104]

flavone

Drug Info

[90]

FR194921

Drug Info

[108]

isobutylmethylxanthine

Drug Info

[114], [115]

KF26777

Drug Info

[116]

MRE 2029F20

Drug Info

[120]

MRE 3008F20

Drug Info

[103]

MRS1041

Drug Info

[90]

MRS1062

Drug Info

[90]

MRS1065

Drug Info

[90]

MRS1084

Drug Info

[90]

MRS1086

Drug Info

[90]

MRS1093

Drug Info

[90]

MRS1132

Drug Info

[90]

MRS1191

Drug Info

[118]

MRS923

Drug Info

[90]

MRS928

Drug Info

[90]

PSB-10

Drug Info

[131]

PSB-11

Drug Info

[131]

PSB36

Drug Info

[132]

sakuranetin

Drug Info

[90]

VUF5574

Drug Info

[137]

xanthine amine congener

Drug Info

[114]

[3H]DPCPX

Drug Info

[138]

Modulator

[+] 6 Modulator drugs

AMP-579

Drug Info

[35]

BAY 1067197

Drug Info

[37]

FK-453

Drug Info

[53]

FK-838

Drug Info

[54]

L-97-1 intravenous

Drug Info

[118]

Paeoniflorin

Drug Info

[118]

Agonist

[+] 19 Agonist drugs

Capadenoson

Drug Info

[38]

DTI-0009

Drug Info

[39], [40]

SELODENOSON

Drug Info

[39], [40], [41]

INO-8875

Drug Info

[44]

PMID27387065-Compound-6

Drug Info

[47]

Tecadenoson

Drug Info

[48], [49]

SDZ-WAG-994

Drug Info

[55]

BAY 60-6583

Drug Info

[56]

(S)-PIA

Drug Info

[62]

2-chloroadenosine

Drug Info

[84]

5-Cl-5-deoxy-(+/-)-ENBA

Drug Info

[69]

CP608,039

Drug Info

[103]

LUF5831

Drug Info

[119]

MRS5151

Drug Info

[121]

N(6)-cyclohexyladenosine

Drug Info

[122]

PENECA

Drug Info

[128]

TCPA

Drug Info

[135]

[3H]CCPA

Drug Info

[133], [67]

[3H]HEMADO

Drug Info

[139]

Inhibitor

[+] 205 Inhibitor drugs

Tonapofylline

Drug Info

[42], [43]

KF-17837

Drug Info

[45]

SCH-442416

Drug Info

[46]

BRL-61063

Drug Info

[51]

ARISTEROMYCIN

Drug Info

[57]

METHYLTHIOADENOSINE

Drug Info

[58]

METRIFUDIL

Drug Info

[59]

(1-Phenyl-propyl)-(9-phenyl-9H-purin-6-yl)-amine

Drug Info

[60]

(9-Methyl-9H-purin-6-yl)-phenyl-amine

Drug Info

[60]

1,3-Diallyl-3,7-dihydro-purine-2,6-dione

Drug Info

[63]

1,3-Diethyl-3,7-dihydro-purine-2,6-dione

Drug Info

[63]

1,3-Diisobutyl-3,7-dihydro-purine-2,6-dione

Drug Info

[63]

1,3-Dipropyl-3,7-dihydro-purine-2,6-dione

Drug Info

[63]

1-Methyl-8-phenyl-3,7-dihydro-purine-2,6-dione

Drug Info

[64]

1-METHYLXANTHINE

Drug Info

[63]

1-Propyl-3,7-dihydro-purine-2,6-dione

Drug Info

[65]

1H-Imidazo[4,5-c]quinolin-4-ylamine HCl

Drug Info

[66]

2'-Me-tecadenoson

Drug Info

[67]

2,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

2,5'-dichloro-5'-deoxy-N6-cyclopentyladenosine

Drug Info

[69]

2,6,8-triphenyl-9H-purine

Drug Info

[70]

2,6-bis(4-tolyl)-9H-purine

Drug Info

[70]

2,6-dimethyl-8-ethyl-1-deazapurine

Drug Info

[71]

2,6-diphenyl-1-deazapurine

Drug Info

[71]

2,6-diphenyl-8-(1-ethylpropyl)-1-deazapurine

Drug Info

[71]

2,6-diphenyl-8-ethyl-1-deazapurine

Drug Info

[71]

2,6-diphenyl-8-methyl-1-deazapurine

Drug Info

[71]

2,6-diphenyl-8-tButyl-1-deazapurine

Drug Info

[71]

2,6-diphenyl-9H-purine

Drug Info

[70]

2,6-Diphenyl-pyrimidin-4-ylamine

Drug Info

[72]

2,6-dphenyl-8-propyl-1-deazapurine

Drug Info

[71]

2-(1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[73]

2-(2''-indolylethyloxy)adenosine

Drug Info

[74]

2-(2-furyl)-6-(1H-pyrazol-1-yl)pyrimidin-4-amine

Drug Info

[75]

2-(3''(5''-chloro-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''(7''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(4''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(5''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(5''-fluoro-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(5''-hydroxyindolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(5''-iodo-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(5''-methoxy-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(6''-bromo-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-(6''-chloro-indolyl)ethyloxy)adenosine

Drug Info

[74]

2-(3''-indolylethyloxy)adenosine

Drug Info

[74]

2-(3''-pyrrolylethyloxy)adenosine

Drug Info

[74]

2-(4-chloro-1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[76]

2-(4-chlorophenyl)-6-phenyl-9H-purine

Drug Info

[70]

2-(4-ethylthiobenzimidazol-2-yl)quinoxaline

Drug Info

[76]

2-(4-hydroxypent-1-yl)-N6-methoxyadenosine

Drug Info

[77]

2-(4-methoxyphenyl)-6-phenyl-9H-purine

Drug Info

[70]

2-(4-methyl-1H-benzo[d]imidazol-2-yl)quinoxaline

Drug Info

[73]

2-(5-cyano-1-pent-1-ynyl)-N6-methoxyadenosine

Drug Info

[77]

2-(6-amino-8-bromo-9H-purin-9-yl)ethanol

Drug Info

[78]

2-(6-Cyclopentylamino-purin-9-yl)-ethanol

Drug Info

[60]

2-(hex-1-ynyl)-N6-methoxyadenosine

Drug Info

[77]

2-Amino-4,6-di-furan-2-yl-nicotinonitrile

Drug Info

[79]

2-Amino-4,6-di-thiophen-2-yl-nicotinonitrile

Drug Info

[79]

2-Amino-4,6-diphenyl-nicotinonitrile

Drug Info

[79]

2-Amino-4,6-diphenyl-pyrimidin-5-carbonitrile

Drug Info

[72]

2-Amino-4,6-diphenyl-pyrimidine

Drug Info

[72]

2-Amino-4-furan-2-yl-6-phenyl-nicotinonitrile

Drug Info

[79]

2-Amino-4-phenyl-6-thiophen-2-yl-nicotinonitrile

Drug Info

[79]

2-amino-6-phenyl-4-p-tolylnicotinonitrile

Drug Info

[80]

2-Amino-6-phenyl-4-thiophen-2-yl-nicotinonitrile

Drug Info

[79]

2-amino-N-benzyl-6-phenyl-9H-purine-9-carboxamide

Drug Info

[81]

2-azido-N6-methyl-9-(beta-D-ribofuranosyl)adenine

Drug Info

[82]

2-chloro-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[83]

2-Cyclopentyl-1H-imidazo[4,5-c]quinolin-4-ylamine

Drug Info

[66]

2-ethyl-4-(furan-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[83]

2-ethyl-4-(pyridin-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[83]

2-ethyl-4-(thiazol-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[83]

2-ethyl-4-(thiophen-2-yl)thieno[3,2-d]pyrimidine

Drug Info

[83]

2-ethynyl-N6-methoxyadenosine

Drug Info

[77]

2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one

Drug Info

[85]

2-m-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine

Drug Info

[85]

2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one

Drug Info

[85]

2-p-tolyl-2H-pyrazolo[3,4-c]quinolin-4-amine

Drug Info

[85]

2-Phenyl-1H-imidazo[4,5-c]quinolin-4-ylamine

Drug Info

[66]

2-phenyl-2H-pyrazolo[3,4-c]quinolin-4(5H)-one

Drug Info

[85]

2-phenyl-2H-pyrazolo[3,4-c]quinolin-4-amine

Drug Info

[85]

2-phenylpropoxyadenosine

Drug Info

[74]

2-tolyl-6-phenyl-9H-purine

Drug Info

[70]

2-[(4-acetylphenyl)ethynyl]-N6-methoxyadenosine

Drug Info

[77]

2-[(4-fluorophenyl)ethynyl]-N6-methoxyadenosine

Drug Info

[77]

3,4-Dichloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

3-(3-chloro-1H-pyrazol-5-yl)quinoxalin-2(1H)-one

Drug Info

[73]

3-Benzyl-7-methyl-[1,8]naphthyridin-4-ol

Drug Info

[86]

3-Benzyl-7-methyl-[1,8]naphthyridine-4-thiol

Drug Info

[86]

3-noradamantyl-1,3-dipropylxanthine

Drug Info

[87]

4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one

Drug Info

[88]

4-(ethylthio)-6-phenyl-1,3,5-triazin-2-amine

Drug Info

[80]

4-(furan-2-yl)thieno[3,2-d]pyrimidin-2-amine

Drug Info

[81]

4-(thiazol-2-yl)thieno[3,2-d]pyrimidin-2-amine

Drug Info

[83]

4-Amino-2,6-diphenyl-pyrimidine-5-carbonitrile

Drug Info

[72]

4-Bromo-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

4-Chloro-7-methyl-2-phenyl-[1,8]naphthyridine

Drug Info

[89]

4-Chloro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

4-Methoxy-N-(3-phenyl-isoquinolin-1-yl)-benzamide

Drug Info

[68]

100

4-Nitro-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

101

4-tert-Butyl-N-(4-phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

102

5,7-dibromo-9H-pyrido[3,4-b]indol-6-ol

Drug Info

[91]

103

6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[92]

104

6-ethylamino-2-(3''-indolyl)ethyloxy)adenosine

Drug Info

[74]

105

6-guanidino-2-(3''-indolylethyloxy)adenosine

Drug Info

[74]

106

7-(3,6,9,12-tetraoxatricos-22-enyl)theophylline

Drug Info

[93]

107

7-Bromo-2-phenyl-[1,8]naphthyridin-4-ol

Drug Info

[94]

108

7-Chloro-2-phenyl-[1,8]naphthyridin-4-ol

Drug Info

[94]

109

7-Dimethylamino-2-phenyl-[1,8]naphthyridin-4-ol

Drug Info

[94]

110

7-Methyl-2-propyl-[1,8]naphthyridin-4-ol

Drug Info

[94]

111

8-Bromo-9-(2,3-dihydroxypropyl)-9H-adenine

Drug Info

[95]

112

8-Bromo-9-(2-butyl)-9H-adenine

Drug Info

[95]

113

8-Bromo-9-(3-hydroxypropyl)-9H-adenine

Drug Info

[95]

114

8-Bromo-9-cyclobutyl-9H-adenine

Drug Info

[95]

115

8-Bromo-9-cyclohexyl-9H-adenine

Drug Info

[95]

116

8-Bromo-9-cyclopentyl-9H-adenine

Drug Info

[95]

117

8-Bromo-9-ethyl-9H-adenine

Drug Info

[95]

118

8-bromo-9-isobutyl-9H-purin-6-amine

Drug Info

[78]

119

8-Bromo-9-isopropyl-9H-adenine

Drug Info

[95]

120

8-Bromo-9-methyl-9H-adenine

Drug Info

[95]

121

8-Bromo-9-phenylethyl-9H-adenine

Drug Info

[95]

122

8-Bromo-9-propyl-9H-adenine

Drug Info

[95]

123

8-cyclohexyl-6-(4-tolyl)-2-phenyl-9H-purine

Drug Info

[70]

124

8-Phenyl-1-propyl-3,7-dihydro-purine-2,6-dione

Drug Info

[97]

125

8-Phenyl-3,7-dihydro-purine-2,6-dione

Drug Info

[97]

126

9-(3-aminobenzyl)-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[81]

127

9-(3-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[81]

128

9-(4-nitrobenzyl)-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[81]

129

9-Allyl-8-bromo-9H-adenine

Drug Info

[95]

130

9-benzyl-6-(furan-2-yl)-9H-purin-2-amine

Drug Info

[81]

131

9-Benzyl-8-bromo-9H-adenine

Drug Info

[95]

132

9-Cyclobutyl-9H-adenine

Drug Info

[95]

133

9-Cyclopentyl-9H-adenine

Drug Info

[60]

134

9-Ethyl-8-phenylethynyl-9H-purin-6-ylamine

Drug Info

[98]

135

9-Ethyl-9H-adenine

Drug Info

[95]

136

9-Isopropyl-9H-adenine

Drug Info

[95]

137

9-Methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine

Drug Info

[99]

138

9-Methyl-9H-adenine

Drug Info

[58]

139

9-Phenyl-9H-purin-6-ylamine

Drug Info

[60]

140

9-Propyl-9H-adenine

Drug Info

[95]

141

A-987306

Drug Info

[100]

142

Cyclohexyl-(2-phenylsulfanyl-9H-purin-6-yl)-amine

Drug Info

[105]

143

Cyclohexyl-(9-ethyl-9H-purin-6-yl)-amine

Drug Info

[60]

144

Cyclohexyl-(9-methyl-9H-purin-6-yl)-amine

Drug Info

[60]

145

Cyclopentyl-(9-cyclopentyl-9H-purin-6-yl)-amine

Drug Info

[60]

146

Cyclopentyl-(9-ethyl-9H-purin-6-yl)-amine

Drug Info

[60]

147

Cyclopentyl-(9-methyl-9H-purin-6-yl)-amine

Drug Info

[60]

148

Cyclopentyl-(9-phenyl-9H-purin-6-yl)-amine

Drug Info

[60]

149

DEPX

Drug Info

[106]

150

Ethyl 5-benzoyl-4-phenylthiazol-2-ylcarbamate

Drug Info

[42]

151

FR-166124

Drug Info

[107]

152

GNF-PF-2224

Drug Info

[109], [110], [111], [112]

153

GNF-PF-2700

Drug Info

[78]

154

Hexanoic Acid (2,6-diphenylpyrimidin-4-yl)amide

Drug Info

[113]

155

Kuanoniamine D

Drug Info

[117]

156

LUF-5417

Drug Info

[42]

157

LUF-5433

Drug Info

[42]

158

LUF-5737

Drug Info

[113]

159

LUF-5767

Drug Info

[113]

160

LUF-5816

Drug Info

[71]

161

LUF-5853

Drug Info

[72]

162

LUF-5956

Drug Info

[70]

163

LUF-5957

Drug Info

[70]

164

LUF-5978

Drug Info

[71]

165

N*6*-Cyclohexyl-N*2*-phenyl-9H-purine-2,6-diamine

Drug Info

[105]

166

N*6*-Cyclooctyl-N*2*-phenyl-9H-purine-2,6-diamine

Drug Info

[105]

167

N-(2,6-diphenylpyrimidin-4-yl)-3-methylbutyramide

Drug Info

[113]

168

N-(2,6-diphenylpyrimidin-4-yl)benzamide

Drug Info

[113]

169

N-(2,6-diphenylpyrimidin-4-yl)butyramide

Drug Info

[113]

170

N-(2,6-diphenylpyrimidin-4-yl)isobutyramide

Drug Info

[113]

171

N-(2,6-diphenylpyrimidin-4-yl)propionamide

Drug Info

[113]

172

N-(2-(furan-2-yl)-3,4'-bipyridin-6-yl)acetamide

Drug Info

[123]

173

N-(4,5-diphenylpyrimidin-2-yl)acetamide

Drug Info

[113]

174

N-(4,6-diphenylpyrimidin-2-yl)-3-chlorobenzamide

Drug Info

[113]

175

N-(4,6-diphenylpyrimidin-2-yl)-3-methylbutyramide

Drug Info

[113]

176

N-(4,6-diphenylpyrimidin-2-yl)benzamide

Drug Info

[113]

177

N-(4,6-diphenylpyrimidin-2-yl)propionamide

Drug Info

[113]

178

N-(4-Phenyl-thiazol-2-yl)-benzamide

Drug Info

[68]

179

N-(5-Benzoyl-4-phenylthiazol-2-yl)benzamide

Drug Info

[42]

180

N6-((+/-)-endo-norborn-2-yl)adenosine

Drug Info

[69]

181

N6-CYCLOPENTYLADENOSINE

Drug Info

[67]

182

N6-methoxy-2-phenylethynyladenosine

Drug Info

[77]

183

N6-methoxy-2-[(2-pyridinyl)ethynyl]adenosine

Drug Info

[77]

184

N6-methoxy-2-[(4-methoxyphenyl)ethynyl]adenosine

Drug Info

[77]

185

N6-methoxy-2-[(4-methylphenyl)ethynyl]adenosine

Drug Info

[77]

186

N6-methoxy-2-[(4-pentylphenyl)ethynyl]adenosine

Drug Info

[77]

187

N6-methoxy-2-[(4-pyridinyl)ethynyl]adenosine

Drug Info

[77]

188

N6-methoxy-2-[2-(trimethylsilyl)ethynyl]adenosine

Drug Info

[77]

189

N6-[(4-Amino)-phenyl]-9-benzyl-2-phenyladenine

Drug Info

[124]

190

N6-[(4-Nitro)-phenyl]-9-benzyl-2-phenyladenine

Drug Info

[124]

191

P-IODOAMPHETAMINE

Drug Info

[125]

192

PD-115199

Drug Info

[126]

193

PD-81723

Drug Info

[127]

194

Pentanoic acid (4,6-diphenylpyrimidin-2-yl)amide

Drug Info

[113]

195

Phenyl(2-(trifluoromethyl)quinolin-4-yl)methanol

Drug Info

[129]

196

Phenyl-(9-phenyl-9H-purin-6-yl)-amine

Drug Info

[60]

197

PSB-0788

Drug Info

[130]

198

PSB-1115

Drug Info

[130]

199

PSB-601

Drug Info

[130]

200

R-N6-(phenylisopropyl)adenosine

Drug Info

[133], [74]

201

SCH-63390

Drug Info

[134]

202

ST-1535

Drug Info

[99]

203

VUF-8507

Drug Info

[136]

204

[3H]NECA

Drug Info

[140]

205

[3H]OSIP339391

Drug Info

[78]

Cell-based Target Expression Variations

Top

Cell-based Target Expression Variations

Cell-based Target Expression Variations Info

Different Human System Profiles of Target	Top
Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target. A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020). Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues. The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021). Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function. Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006). Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database. The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017). Human Similarity Proteins Human Tissue Distribution Human Pathway Affiliation Biological Network Descriptors

Different Human System Profiles of Target

Top

Human Similarity Proteins of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.

A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs (Brief Bioinform, 21: 649-662, 2020).

Human Tissue Distribution of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.

The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects (Nat Rev Drug Discov, 20: 64-81, 2021).

Human Pathway Affiliation of target is determined by the life-essential pathways provided on KEGG database. The target-affiliated pathways were defined based on the following two criteria (a) the pathways of the studied target should be life-essential for both healthy individuals and patients, and (b) the studied target should occupy an upstream position in the pathways and therefore had the ability to regulate biological function.

Targets involved in a fewer pathways have greater likelihood to be successfully developed, while those associated with more human pathways increase the chance of undesirable interferences with other human processes (Pharmacol Rev, 58: 259-279, 2006).

Biological Network Descriptors of target is determined based on a human protein-protein interactions (PPI) network consisting of 9,309 proteins and 52,713 PPIs, which were with a high confidence score of ≥ 0.95 collected from STRING database.

The network properties of targets based on protein-protein interactions (PPIs) have been widely adopted for the assessment of target’s druggability. Proteins with high node degree tend to have a high impact on network function through multiple interactions, while proteins with high betweenness centrality are regarded to be central for communication in interaction networks and regulate the flow of signaling information (Front Pharmacol, 9, 1245, 2018; Curr Opin Struct Biol. 44:134-142, 2017).

Human Similarity Proteins

Human Tissue Distribution

Human Pathway Affiliation

Biological Network Descriptors

Protein Name	Pfam ID	Percentage of Identity (%)	E value
Olfactory receptor 1N1 (OR1N1)	PF13853	27.184 (56/206)	3.83E-12
Olfactory receptor 1A2 (OR1A2)	PF13853	26.738 (50/187)	4.32E-10
Olfactory receptor 1G1 (OR1G1)	PF13853	21.498 (66/307)	4.49E-10
Olfactory receptor 10A6 (OR10A6)	PF13853	25.121 (52/207)	6.47E-10
Olfactory receptor 10G7 (OR10G7)	PF13853	23.881 (32/134)	1.58E-09
Olfactory receptor 1P1 (OR1P1)	PF13853	24.731 (46/186)	2.42E-09
Olfactory receptor 7A17 (OR7A17)	PF13853	22.635 (67/296)	3.20E-09
Olfactory receptor 10G9 (OR10G9)	PF13853	19.620 (62/316)	9.41E-09
Olfactory receptor 10G4 (OR10G4)	PF13853	23.134 (31/134)	1.36E-08
Olfactory receptor 7G2 (OR7G2)	PF13853	32.381 (34/105)	4.00E-08
Olfactory receptor 4C16 (OR4C16)	PF13853	28.926 (35/121)	5.01E-08
Olfactory receptor 10G8 (OR10G8)	PF13853	22.388 (30/134)	6.86E-08
Olfactory receptor 1J1 (OR1J1)	PF13853	21.538 (28/130)	7.36E-08
Olfactory receptor 1D2 (OR1D2)	PF13853	29.268 (36/123)	8.33E-08
Olfactory receptor 1N2 (OR1N2)	PF13853	27.692 (36/130)	8.52E-08
Olfactory receptor 7C2 (OR7C2)	PF13853	26.316 (35/133)	1.39E-07
Olfactory receptor 7C1 (OR7C1)	PF13853	26.471 (36/136)	1.42E-07
Olfactory receptor 7A5 (OR7A5)	PF13853	26.190 (44/168)	1.42E-07
Olfactory receptor 7A10 (OR7A10)	PF13853	26.515 (35/132)	1.49E-07
Olfactory receptor 2T34 (OR2T34)	PF13853	26.277 (36/137)	1.76E-07
Olfactory receptor 2T4 (OR2T4)	PF13853	21.160 (62/293)	1.81E-07
Olfactory receptor 7E24 (OR7E24)	PF13853	28.369 (40/141)	1.87E-07
Olfactory receptor 7D2 (OR7D2)	PF13853	21.088 (62/294)	2.26E-07
Olfactory receptor 52E5 (OR52E5)	PF13853	27.027 (30/111)	2.99E-07
Olfactory receptor 52A1 (OR52A1)	PF13853	27.907 (36/129)	3.13E-07
Olfactory receptor 9A4 (OR9A4)	PF13853	26.772 (34/127)	3.30E-07
Olfactory receptor 6S1 (OR6S1)	PF13853	25.000 (37/148)	4.27E-07
Olfactory receptor 1E1 (OR1E1)	PF13853	25.641 (30/117)	4.58E-07
Olfactory receptor 5B17 (OR5B17)	PF13853	24.232 (71/293)	4.66E-07
Olfactory receptor 2T3 (OR2T3)	PF13853	22.491 (65/289)	4.77E-07
Olfactory receptor 2J2 (OR2J2)	PF13853	23.239 (66/284)	5.85E-07
Putative olfactory receptor 7A2 (OR7A2P)	PF13853	24.800 (31/125)	7.83E-07
Olfactory receptor 4C6 (OR4C6)	PF13853	25.000 (30/120)	8.62E-07
Olfactory receptor 2T29 (OR2T29)	PF13853	22.456 (64/285)	9.55E-07
Olfactory receptor 1B1 (OR1B1)	PF13853	22.917 (44/192)	9.65E-07
Olfactory receptor 2T5 (OR2T5)	PF13853	22.456 (64/285)	1.02E-06
Olfactory receptor 5D14 (OR5D14)	PF13853	23.179 (70/302)	1.05E-06
Olfactory receptor 1A1 (OR1A1)	PF13853	24.064 (45/187)	1.08E-06
Olfactory receptor 2T10 (OR2T10)	PF13853	27.338 (38/139)	1.11E-06
Olfactory receptor 52J3 (OR52J3)	PF13853	27.972 (40/143)	1.17E-06
Olfactory receptor 4K2 (OR4K2)	PF13853	24.031 (31/129)	1.22E-06
Olfactory receptor 9A2 (OR9A2)	PF13853	24.324 (36/148)	1.32E-06
Olfactory receptor 11L1 (OR11L1)	PF13853	21.886 (65/297)	1.37E-06
Olfactory receptor 11G2 (OR11G2)	PF13853	21.017 (62/295)	1.39E-06
Olfactory receptor 2A14 (OR2A14)	PF13853	25.833 (31/120)	1.45E-06
Olfactory receptor 5D13 (OR5D13)	PF13853	26.351 (39/148)	1.52E-06
Olfactory receptor 52I1 (OR52I1)	PF13853	28.283 (28/99)	1.68E-06
Olfactory receptor 52E8 (OR52E8)	PF13853	26.563 (34/128)	1.84E-06
Olfactory receptor 51E1 (OR51E1)	PF13853	29.204 (33/113)	1.93E-06
Olfactory receptor 1L1 (OR1L1)	PF13853	21.595 (65/301)	2.00E-06
Olfactory receptor 9A1 (OR9A1P)	PF13853	23.944 (51/213)	2.03E-06
Olfactory receptor 6N1 (OR6N1)	PF13853	29.323 (39/133)	2.04E-06
Olfactory receptor 10P1 (OR10P1)	PF13853	28.333 (34/120)	2.18E-06
Olfactory receptor 14J1 (OR14J1)	PF13853	24.590 (30/122)	2.45E-06
Olfactory receptor 2A12 (OR2A12)	PF13853	24.793 (30/121)	2.90E-06
Olfactory receptor 52I2 (OR52I2)	PF13853	25.962 (27/104)	3.25E-06
Olfactory receptor 4S1 (OR4S1)	PF13853	24.590 (30/122)	3.86E-06
Olfactory receptor 2AG2 (OR2AG2)	PF13853	20.863 (58/278)	4.10E-06
Olfactory receptor 11H4 (OR11H4)	PF13853	26.718 (35/131)	4.68E-06
Olfactory receptor 1D4 (OR1D4)	PF13853	29.412 (35/119)	6.86E-06
Olfactory receptor 6N2 (OR6N2)	PF13853	27.350 (32/117)	6.87E-06
Olfactory receptor 6M1 (OR6M1)	PF13853	22.764 (28/123)	6.91E-06
Olfactory receptor 1S1 (OR1S1)	PF13853	25.806 (32/124)	7.16E-06
Olfactory receptor 6F1 (OR6F1)	PF13853	24.818 (34/137)	7.37E-06
Olfactory receptor 4N5 (OR4N5)	PF13853	25.000 (30/120)	7.50E-06
Olfactory receptor 4F15 (OR4F15)	PF13853	21.053 (64/304)	8.94E-06
Olfactory receptor 52R1 (OR52R1)	PF13853	25.490 (26/102)	9.61E-06
Olfactory receptor 1J2 (OR1J2)	PF13853	21.379 (31/145)	1.04E-05
Olfactory receptor 7G3 (OR7G3)	PF13853	26.271 (31/118)	1.06E-05
Olfactory receptor 1D5 (OR1D5)	PF13853	29.412 (35/119)	1.20E-05
Olfactory receptor 2J1 (OR2J1)	PF13853	23.239 (66/284)	1.25E-05
Olfactory receptor 51I2 (OR51I2)	PF13853	27.966 (33/118)	1.35E-05
Olfactory receptor 10H4 (OR10H4)	PF13853	24.786 (29/117)	1.50E-05
Olfactory receptor 8U3 (OR8U3)	PF13853	26.667 (36/135)	1.55E-05
Olfactory receptor 12D3 (OR12D3)	PF13853	22.857 (32/140)	1.79E-05
Olfactory receptor 52H1 (OR52H1)	PF13853	28.378 (42/148)	1.81E-05
Olfactory receptor 52E4 (OR52E4)	PF13853	23.423 (26/111)	1.82E-05
Olfactory receptor 52Z1P (OR52Z1P)	PF13853	29.825 (34/114)	1.82E-05
Olfactory receptor 7G1 (OR7G1)	PF13853	29.412 (30/102)	1.95E-05
Olfactory receptor 10A3 (OR10A3)	PF13853	22.685 (49/216)	2.42E-05
Olfactory receptor 4Q3 (OR4Q3)	PF13853	26.496 (31/117)	2.48E-05
Olfactory receptor 52A5 (OR52A5)	PF13853	28.846 (30/104)	2.68E-05
Olfactory receptor 5AL1 (OR5AL1)	PF13853	26.027 (38/146)	2.71E-05
Putative olfactory receptor 1F12P (OR1F12P)	PF13853	24.576 (29/118)	2.73E-05
Olfactory receptor 13J1 (OR13J1)	PF13853	24.800 (31/125)	3.15E-05
Olfactory receptor 1J4 (OR1J4)	PF13853	25.758 (34/132)	3.16E-05
Olfactory receptor 52D1 (OR52D1)	PF13853	32.692 (34/104)	3.29E-05
Olfactory receptor 2J3 (OR2J3)	PF13853	24.648 (70/284)	3.50E-05
Olfactory receptor 11A1 (OR11A1)	PF13853	29.825 (34/114)	3.50E-05
Olfactory receptor 1L6 (OR1L6)	PF13853	21.608 (43/199)	3.93E-05
Olfactory receptor 5M10 (OR5M10)	PF13853	21.575 (63/292)	4.01E-05
Olfactory receptor 10AG1 (OR10AG1)	PF13853	22.759 (66/290)	4.25E-05
Olfactory receptor 4K15 (OR4K15)	PF13853	27.193 (31/114)	4.33E-05
Olfactory receptor 51H1 (OR51H1)	PF13853	26.852 (29/108)	4.92E-05
Olfactory receptor 6C2 (OR6C2)	PF13853	20.792 (42/202)	5.16E-05
Olfactory receptor 7D4 (OR7D4)	PF13853	22.901 (30/131)	5.16E-05
Olfactory receptor 4D9 (OR4D9)	PF13853	22.764 (28/123)	5.23E-05
Olfactory receptor 8H2 (OR8H2)	PF13853	25.191 (33/131)	5.49E-05
Olfactory receptor 1E2 (OR1E2)	PF13853	23.913 (33/138)	5.51E-05
Olfactory receptor 2A1/2A42 (OR2A1; OR2A42)	PF13853	26.724 (31/116)	5.87E-05
Olfactory receptor 10H1 (OR10H1)	PF13853	26.891 (32/119)	6.44E-05
Olfactory receptor 11H7 (OR11H7)	PF13853	21.212 (28/132)	6.61E-05
Olfactory receptor 8H1 (OR8H1)	PF13853	24.561 (28/114)	7.70E-05
Olfactory receptor 1S2 (OR1S2)	PF13853	21.622 (64/296)	8.89E-05
Olfactory receptor 4C11 (OR4C11)	PF13853	24.786 (29/117)	9.19E-05
Olfactory receptor 8D4 (OR8D4)	PF13853	24.167 (29/120)	9.29E-05
Olfactory receptor 6K3 (OR6K3)	PF13853	21.818 (60/275)	9.35E-05
Olfactory receptor 52M1 (OR52M1)	PF13853	31.132 (33/106)	9.45E-05
Olfactory receptor 4F3/4F16/4F29 (OR4F3; OR4F16; OR4F29)	PF13853	24.348 (28/115)	9.58E-05
Olfactory receptor 1F1 (OR1F1)	PF13853	27.119 (32/118)	9.84E-05
Putative olfactory receptor 14L1 (OR14L1P)	PF13853	19.863 (58/292)	1.01E-04
Olfactory receptor 6Q1 (OR6Q1)	PF13853	24.219 (31/128)	1.02E-04
Olfactory receptor 4A15 (OR4A15)	PF13853	23.810 (30/126)	1.03E-04
Olfactory receptor 4K5 (OR4K5)	PF13853	21.262 (64/301)	1.07E-04
Olfactory receptor 10C1 (OR10C1)	PF13853	23.188 (32/138)	1.08E-04
Olfactory receptor 5M1 (OR5M1)	PF13853	21.233 (62/292)	1.33E-04
Olfactory receptor 8H3 (OR8H3)	PF13853	26.515 (35/132)	1.36E-04
Olfactory receptor 1L4 (OR1L4)	PF13853	21.106 (42/199)	1.47E-04
Olfactory receptor 51A7 (OR51A7)	PF13853	25.439 (29/114)	1.47E-04
Olfactory receptor 6C65 (OR6C65)	PF13853	27.200 (34/125)	1.50E-04
Olfactory receptor 2AT4 (OR2AT4)	PF13853	22.464 (31/138)	1.57E-04
Olfactory receptor 1M1 (OR1M1)	PF13853	24.000 (30/125)	1.64E-04
Olfactory receptor 13H1 (OR13H1)	PF13853	24.242 (32/132)	1.65E-04
Olfactory receptor 4F21 (OR4F21)	PF13853	23.478 (27/115)	1.75E-04
Olfactory receptor 52K1 (OR52K1)	PF13853	29.508 (36/122)	1.79E-04
Olfactory receptor 52B2 (OR52B2)	PF13853	28.571 (38/133)	2.26E-04
Olfactory receptor 52A4 (OR52A4P)	PF13853	25.000 (28/112)	2.34E-04
Olfactory receptor 2D2 (OR2D2)	PF13853	28.455 (35/123)	2.61E-04
Olfactory receptor 51G2 (OR51G2)	PF13853	26.415 (28/106)	2.63E-04
Olfactory receptor 4D5 (OR4D5)	PF13853	23.140 (28/121)	2.82E-04
Olfactory receptor 6A2 (OR6A2)	PF13853	23.077 (30/130)	2.88E-04
Olfactory receptor 8J2 (OR8J2)	PF13853	26.230 (32/122)	2.98E-04
Olfactory receptor 10V1 (OR10V1)	PF13853	23.529 (32/136)	3.05E-04
Olfactory receptor 5P3 (OR5P3)	PF13853	24.762 (26/105)	3.29E-04
Olfactory receptor 10H2 (OR10H2)	PF13853	26.891 (32/119)	3.32E-04
Olfactory receptor 5V1 (OR5V1)	PF13853	22.794 (31/136)	3.37E-04
Olfactory receptor 1I1 (OR1I1)	PF13853	26.667 (32/120)	3.94E-04
Olfactory receptor 4N4C (OR4N4C)	PF13853	21.284 (63/296)	4.09E-04
Olfactory receptor 2C1 (OR2C1)	PF13853	25.833 (31/120)	4.12E-04
Olfactory receptor 5M11 (OR5M11)	PF13853	27.344 (35/128)	4.39E-04
Olfactory receptor 4N2 (OR4N2)	PF13853	22.549 (69/306)	4.45E-04
Olfactory receptor 4M1 (OR4M1)	PF13853	21.154 (66/312)	4.52E-04
Olfactory receptor 1L3 (OR1L3)	PF13853	20.915 (64/306)	4.64E-04
Olfactory receptor 2G6 (OR2G6)	PF13853	26.230 (32/122)	4.89E-04
Olfactory receptor 6K6 (OR6K6)	PF13853	26.543 (43/162)	5.41E-04
Olfactory receptor 1L8 (OR1L8)	PF13853	25.000 (29/116)	6.69E-04
Olfactory receptor 8J3 (OR8J3)	PF13853	26.718 (35/131)	6.73E-04
Olfactory receptor 13A1 (OR13A1)	PF13853	24.561 (28/114)	6.93E-04
Olfactory receptor 51D1 (OR51D1)	PF13853	27.835 (27/97)	6.99E-04
Olfactory receptor 14A16 (OR14A16)	PF13853	20.906 (60/287)	7.52E-04
Putative olfactory receptor 52L2 (OR52L2P)	PF13853	27.027 (30/111)	1.00E-03
Olfactory receptor 4N4 (OR4N4)	PF13853	20.946 (62/296)	1.00E-03
Olfactory receptor 52E2 (OR52E2)	PF13853	25.410 (31/122)	1.00E-03
Olfactory receptor 10G3 (OR10G3)	PF13853	26.119 (35/134)	1.00E-03
Olfactory receptor 51E2 (OR51E2)	PF13853	28.431 (29/102)	1.00E-03
Olfactory receptor 51F1 (OR51F1)	PF13853	25.000 (26/104)	1.00E-03
Olfactory receptor 13C8 (OR13C8)	PF13853	22.807 (26/114)	1.00E-03
Olfactory receptor 14I1 (OR14I1)	PF13853	25.000 (34/136)	1.00E-03
Olfactory receptor 4C12 (OR4C12)	PF13853	21.849 (26/119)	1.00E-03
Olfactory receptor 10A4 (OR10A4)	PF13853	24.812 (33/133)	1.00E-03
Olfactory receptor 2A25 (OR2A25)	PF13853	23.622 (30/127)	1.00E-03
Olfactory receptor 2B11 (OR2B11)	PF13853	22.837 (66/289)	2.00E-03
Olfactory receptor 52N2 (OR52N2)	PF13853	26.016 (32/123)	2.00E-03
Olfactory receptor 10H3 (OR10H3)	PF13853	22.936 (25/109)	2.00E-03
Olfactory receptor 2H2 (OR2H2)	PF13853	25.833 (31/120)	2.00E-03
Olfactory receptor 6C3 (OR6C3)	PF13853	19.244 (56/291)	2.00E-03
Olfactory receptor 10J3 (OR10J3)	PF13853	23.664 (31/131)	2.00E-03
Olfactory receptor 4D10 (OR4D10)	PF13853	21.053 (24/114)	2.00E-03
Olfactory receptor 51V1 (OR51V1)	PF13853	28.000 (28/100)	2.00E-03
Olfactory receptor 52N4 (OR52N4)	PF13853	27.586 (32/116)	2.00E-03
Olfactory receptor 2M3 (OR2M3)	PF13853	20.000 (58/290)	2.00E-03
Olfactory receptor 8K5 (OR8K5)	PF13853	25.000 (31/124)	2.00E-03
Olfactory receptor 2AJ1 (OR2AJ1)	PF13853	22.069 (64/290)	2.00E-03
Olfactory receptor 10Q1 (OR10Q1)	PF13853	23.276 (27/116)	2.00E-03
Olfactory receptor 4K1 (OR4K1)	PF13853	22.481 (29/129)	2.00E-03
Olfactory receptor 1C1 (OR1C1)	PF13853	25.203 (31/123)	3.00E-03
Olfactory receptor 6K2 (OR6K2)	PF13853	25.000 (33/132)	3.00E-03
Olfactory receptor 51B2 (OR51B2)	PF13853	25.439 (29/114)	3.00E-03
Olfactory receptor 2H1 (OR2H1)	PF13853	26.829 (33/123)	3.00E-03
Olfactory receptor 4K13 (OR4K13)	PF13853	22.963 (31/135)	3.00E-03
Olfactory receptor 2A2 (OR2A2)	PF13853	22.314 (27/121)	3.00E-03
Olfactory receptor 6C1 (OR6C1)	PF13853	19.549 (26/133)	3.00E-03
Olfactory receptor 8U1 (OR8U1)	PF13853	26.400 (33/125)	3.00E-03
Olfactory receptor 6C74 (OR6C74)	PF13853	19.200 (24/125)	3.00E-03
Olfactory receptor 9Q1 (OR9Q1)	PF13853	26.772 (34/127)	4.00E-03
Olfactory receptor 2B6 (OR2B6)	PF13853	22.222 (26/117)	4.00E-03
Olfactory receptor 8U8 (OR8U8)	PF13853	26.400 (33/125)	4.00E-03
Olfactory receptor 5AP2 (OR5AP2)	PF13853	25.874 (37/143)	4.00E-03
Olfactory receptor 4K3 (OR4K3)	PF13853	24.167 (29/120)	4.00E-03
Olfactory receptor 2W1 (OR2W1)	PF13853	21.683 (67/309)	4.00E-03
Olfactory receptor 10A5 (OR10A5)	PF13853	23.577 (29/123)	4.00E-03
Olfactory receptor 2L2 (OR2L2)	PF13853	23.333 (28/120)	5.00E-03
Olfactory receptor 13F1 (OR13F1)	PF13853	22.302 (31/139)	5.00E-03
Olfactory receptor 1Q1 (OR1Q1)	PF13853	24.806 (32/129)	5.00E-03
Putative olfactory receptor 1F2 (OR1F2P)	PF13853	25.000 (29/116)	5.00E-03
Olfactory receptor 4K17 (OR4K17)	PF13853	18.667 (56/300)	5.00E-03
Olfactory receptor 52B4 (OR52B4)	PF13853	27.731 (33/119)	5.00E-03
Olfactory receptor 10W1 (OR10W1)	PF13853	24.348 (28/115)	5.00E-03
Putative olfactory receptor 10D3 (OR10D3)	PF13853	24.107 (27/112)	5.00E-03
Olfactory receptor 8K3 (OR8K3)	PF13853	24.615 (32/130)	5.00E-03
Click to Show/Hide the Information of Human Similarity Proteins


Note: If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.

KEGG Pathway	Pathway ID	Affiliated Target
cGMP-PKG signaling pathway	hsa04022	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
cAMP signaling pathway	hsa04024	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Sphingolipid signaling pathway	hsa04071	Affiliated Target
Class: Environmental Information Processing => Signal transduction	Pathway Hierarchy
Neuroactive ligand-receptor interaction	hsa04080	Affiliated Target
Class: Environmental Information Processing => Signaling molecules and interaction	Pathway Hierarchy
Regulation of lipolysis in adipocytes	hsa04923	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Renin secretion	hsa04924	Affiliated Target
Class: Organismal Systems => Endocrine system	Pathway Hierarchy
Click to Show/Hide the Information of Affiliated Human Pathways

Degree	1	Degree centrality	1.07E-04	Betweenness centrality	0.00E+00
Closeness centrality	1.84E-01	Radiality	1.31E+01	Clustering coefficient	0.00E+00
Neighborhood connectivity	1.60E+01	Topological coefficient	1.00E+00	Eccentricity	12
Download	Click to Download the Full PPI Network of This Target

Chemical Structure based Activity Landscape of Target

Top

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target Poor or Non Binders

Top

Target Poor or Non Binders

Target Poor or Non Binders Info

Target Profiles in Patients

Top

Target Expression
Profile (TEP)

Target Expression Profile Info

Target Affiliated Biological Pathways

Top

KEGG Pathway

[+] 5 KEGG Pathways

cGMP-PKG signaling pathway

cAMP signaling pathway

Sphingolipid signaling pathway

Neuroactive ligand-receptor interaction

Morphine addiction

NetPath Pathway

[+] 2 NetPath Pathways

TCR Signaling Pathway

RANKL Signaling Pathway

Panther Pathway

[+] 2 Panther Pathways

Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway

Heterotrimeric G-protein signaling pathway-Gq alpha and Go alpha mediated pathway

Reactome

[+] 2 Reactome Pathways

Adenosine P1 receptors

G alpha (i) signalling events

WikiPathways

[+] 4 WikiPathways

Nucleotide GPCRs

GPCRs, Class A Rhodopsin-like

GPCR ligand binding

GPCR downstream signaling

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

Target QSAR Model

References

Top

REF 1

Caffeine as a psychomotor stimulant: mechanism of action. Cell Mol Life Sci. 2004 Apr;61(7-8):857-72.

REF 2

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 407).

REF 3

Fatigue: an overview. Am Fam Physician. 2008 Nov 15;78(10):1173-9.

REF 4

REF 5

Association between the PDE4D gene and ischaemic stroke in the Chinese Han population. Clin Sci (Lond). 2009 Aug 17;117(7):265-72.

REF 6

Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May; 1808(5): 1290-1308.

REF 7

Xanthines as Adenosine Receptor Antagonists. Handb Exp Pharmacol. 2011; (200): 10.1007/978-3-642-13443-2_6.

REF 8

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035637)

REF 9

ClinicalTrials.gov (NCT00568945) Study to Investigate the Effect of the A1 Agonist Capadenoson on Ventricular HR in Patients With Persistent or Permanent Atrial Fibrillation.. U.S. National Institutes of Health.

REF 10

ClinicalTrials.gov (NCT00040001) Safety and Efficacy Study of an A1-Adenosine Receptor Agonist to Slow Heart Rate in Atrial Fibrillation. U.S. National Institutes of Health.

REF 11

REF 12

Role of matrix metalloproteinases and their tissue inhibitors as potential biomarkers of left ventricular remodelling in the athlete's heart. Clin Sci (Lond). 2009 Jul 16;117(4):157-64.

REF 13

Emerging drugs for acute and chronic heart failure: current and future developments. Expert Opin Emerg Drugs. 2007 Mar;12(1):75-95.

REF 14

ClinicalTrials.gov (NCT01123785) A Dose-Escalation Study Designed to Evaluate the Tolerability, Safety, Pharmacokinetics (PK), and Efficacy of Chronic Topical Ocular Application of INO-8875 in AdultsWith Ocular Hypertension or Primary Open-Angle Glaucoma. U.S. National Institutes of Health.

REF 15

REF 16

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018030)

REF 17

Clinical pipeline report, company report or official report of Astrocyte Pharmaceuticals

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005980)

REF 19

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015498)

REF 20

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003285)

REF 21

REF 22

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010504)

REF 23

Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.

REF 24

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004678)

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005374)

REF 26

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001559)

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005145)

REF 29

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001436)

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003507)

REF 32

Circadian rhythm as a therapeutic target. Nat Rev Drug Discov. 2021 Apr;20(4):287-307.

REF 33

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000987)

REF 34

Adenosine receptor antagonists intensify the benzodiazepine withdrawal signs in mice. Pharmacol Rep. 2006 Sep-Oct;58(5):643-51.

REF 35

Adenosine A1/A2a receptor agonist AMP-579 induces acute and delayed preconditioning against in vivo myocardial stunning. Am J Physiol Heart Circ Physiol. 2004 Dec;287(6):H2746-53.

REF 36

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004779)

REF 37

Separation of on-target efficacy from adverse effects through rational design of a bitopic adenosine receptor agonist. Current Issue vol. 111 no. 12 Celine Valant, 4614-4619.

REF 38

A1 adenosine receptor agonists and their potential therapeutic applications. Expert Opin Investig Drugs. 2008 Dec;17(12):1901-10.

REF 39

Recent developments in adenosine receptor ligands and their potential as novel drugs. Biochim Biophys Acta. 2011 May;1808(5):1290-308.

REF 40

International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and classification of adenosine receptors--an update. Pharmacol Rev. 2011 Mar;63(1):1-34.

REF 41

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 42

2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. Bioorg Med Chem. 2010 Mar 15;18(6):2195-2203.

REF 43

Effects of BG9928, an adenosine A receptor antagonist, in patients with congestive heart failure.J Clin Pharmacol.2011 Jun;51(6):899-907.

REF 44

INO-8875, a highly selective A1 adenosine receptor agonist: evaluation of chronotropic, dromotropic, and hemodynamic effects in rats. J Pharmacol Exp Ther. 2013 Jan;344(1):59-67.

REF 45

2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic gluc... J Med Chem. 2001 Jan 18;44(2):170-9.

REF 46

Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using p... J Med Chem. 2000 Nov 16;43(23):4359-62.

REF 47

Carbonic anhydrase inhibitors: a review on the progress of patent literature (2011-2016).Expert Opin Ther Pat. 2016 Aug;26(8):947-56.

REF 48

CV Therapeutics. Company report from CV Therapeutics, Inc. CV Therapeutics. 2009.

REF 49

Adenosine receptors and cardiovascular disease: the adenosine-1 receptor (A1) and A1 selective ligands. Cardiovasc Toxicol. 2003;3(1):71-88.

REF 50

N-0861 selectively antagonizes adenosine A1 receptors in vivo. Eur J Pharmacol. 1992 May 27;216(1):9-16.

REF 51

Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine. J Med Chem. 1994 Feb 18;37(4):476-85.

REF 52

Adenosine A1 receptor antagonist improves intradialytic hypotension. Kidney Int. 2006 Mar;69(5):877-83.

REF 53

Cardiovascular and renal effects of blocking A1 adenosine receptors. J Cardiovasc Pharmacol. 1993 May;21(5):822-8.

REF 54

An orally active adenosine A1 receptor antagonist, FK838, increases renal excretion and maintains glomerular filtration rate in furosemide-resistan... Br J Pharmacol. 2003 Aug;139(8):1383-8.

REF 55

The cardiac effects of a novel A1-adenosine receptor agonist in guinea pig isolated heart. J Pharmacol Exp Ther. 1994 Dec;271(3):1371-82.

REF 56

Protein kinase C protects preconditioned rabbit hearts by increasing sensitivity of adenosine A2b-dependent signaling during early reperfusion. J Mol Cell Cardiol. 2007 Sep;43(3):262-71.

REF 57

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. J Med Chem. 2000 Jun 1;43(11):2196-203.

REF 58

Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique aden... J Med Chem. 2004 Apr 22;47(9):2243-55.

REF 59

N-substituted adenosines as novel neuroprotective A(1) agonists with diminished hypotensive effects. J Med Chem. 1999 Sep 9;42(18):3463-77.

REF 60

N6,9-disubstituted adenines: potent, selective antagonists at the A1 adenosine receptor. J Med Chem. 1991 Sep;34(9):2877-82.

REF 61

Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists. J Med Chem. 1993 May 14;36(10):1333-42.

REF 62

A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. J Biol Chem. 1994 Jan 28;269(4):2373-6.

REF 63

Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists. J Med Chem. 1988 Oct;31(10):2034-9.

REF 64

Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-,... J Med Chem. 1989 Jun;32(6):1231-7.

REF 65

Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. J Med Chem. 2002 May 23;45(11):2131-8.

REF 66

1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. J Med Chem. 1991 Mar;34(3):1202-6.

REF 67

5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 ... Bioorg Med Chem. 2008 Jan 1;16(1):336-53.

REF 68

Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. Bioorg Med Chem Lett. 2001 Aug 6;11(15):2017-9.

REF 69

N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine recept... J Med Chem. 2009 Apr 23;52(8):2393-406.

REF 70

2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. J Med Chem. 2006 May 18;49(10):2861-7.

REF 71

2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. J Med Chem. 2007 Feb 22;50(4):828-34.

REF 72

A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. Bioorg Med Chem. 2008 Mar 15;16(6):2741-52.

REF 73

Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists. J Med Chem. 2008 Mar 27;51(6):1764-70.

REF 74

Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor. J Med Chem. 2007 Apr 19;50(8):1810-27.

REF 75

Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. J Med Chem. 2008 Feb 14;51(3):400-6.

REF 76

2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database search... J Med Chem. 2005 Dec 29;48(26):8253-60.

REF 77

N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. J Med Chem. 2007 Mar 22;50(6):1222-30.

REF 78

Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. Eur J Med Chem. 2010 Aug;45(8):3459-71.

REF 79

2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. J Med Chem. 2008 Aug 14;51(15):4449-55.

REF 80

Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches. Bioorg Med Chem Lett. 2006 Dec 1;16(23):5993-7.

REF 81

Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpu... Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9.

REF 82

2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. J Med Chem. 2006 Dec 14;49(25):7373-83.

REF 83

Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3.

REF 84

Identification of the adenine binding site of the human A1 adenosine receptor. J Biol Chem. 1999 Feb 5;274(6):3617-21.

REF 85

New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluati... J Med Chem. 2007 Aug 23;50(17):4061-74.

REF 86

1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors. Bioorg Med Chem Lett. 2005 Oct 15;15(20):4604-10.

REF 87

Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31.

REF 88

Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 rec... J Med Chem. 2010 Sep 9;53(17):6386-97.

REF 89

A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives. J Med Chem. 2000 Jul 27;43(15):2814-23.

REF 90

Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. J Med Chem. 1996 Jun 7;39(12):2293-301.

REF 91

Synthesis of eudistomin D analogues and its effects on adenosine receptors. Bioorg Med Chem. 2008 Apr 1;16(7):3825-30.

REF 92

Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. J Med Chem. 2009 Jan 8;52(1):33-47.

REF 93

Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. Bioorg Med Chem. 2010 Mar 15;18(6):2081-2088.

REF 94

Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives. J Med Chem. 2004 Jun 3;47(12):3019-31.

REF 95

8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. Bioorg Med Chem. 2009 Apr 1;17(7):2812-22.

REF 96

Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors. Biochem Pharmacol. 1998 Dec 1;56(11):1437-45.

REF 97

Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationshi... J Med Chem. 1993 Oct 29;36(22):3341-9.

REF 98

Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1931-4.

REF 99

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacolog... J Med Chem. 2005 Nov 3;48(22):6887-96.

REF 100

cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8.

REF 101

Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12.

REF 102

Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. J Med Chem. 2000 Mar 23;43(6):1165-72.

REF 103

Adenosine receptors as therapeutic targets. Nat Rev Drug Discov. 2006 Mar;5(3):247-64.

REF 104

Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): a potent and selective A(1)-adenosine receptor antagonist for in vivo imaging. J Med Chem. 2002 Nov 7;45(23):5150-6.

REF 105

Reversine and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. J Med Chem. 2005 Jul 28;48(15):4910-8.

REF 106

125I-labeled 8-phenylxanthine derivatives: antagonist radioligands for adenosine A1 receptors. J Med Chem. 1988 Apr;31(4):745-51.

REF 107

Discovery of FR166124, a novel water-soluble pyrazolo-[1,5-a]pyridine adenosine A1 receptor antagonist. Bioorg Med Chem Lett. 1999 Jul 19;9(14):1979-84.

REF 108

Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52.

REF 109

Minoxidil-induced hair growth is mediated by adenosine in cultured dermal papilla cells: possible involvement of sulfonylurea receptor 2B as a target of minoxidil. J Invest Dermatol. 2001 Dec;117(6):1594-600.

REF 110

Influence of the antagonist of adenosine A1 receptors, 8-cyclopentyl-1 ,3-dipropylxanthine, upon the anticonvulsant activity of antiepileptic drugs in mice. Przegl Lek. 2008;65(11):759-63.

REF 111

Potent adenosine receptor antagonists that are selective for the A1 receptor subtype. Mol Pharmacol. 1987 Mar;31(3):247-52.

REF 112

Synthesis and theoretical studies on energetics of novel N- and O- perfluoroalkyl triazole tagged thienopyrimidines--their potential as adenosine r... Eur J Med Chem. 2010 May;45(5):1739-45.

REF 113

2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. J Med Chem. 2004 Dec 16;47(26):6529-40.

REF 114

Species difference in the G protein selectivity of the human and bovine A1-adenosine receptor. J Biol Chem. 1994 Dec 23;269(51):32077-84.

REF 115

Adenosine receptors: targets for future drugs. J Med Chem. 1982 Mar;25(3):197-207.

REF 116

KF26777 (2-(4-bromophenyl)-7,8-dihydro-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one dihydrochloride), a new potent and selective adenosine A3 receptor antagonist. Eur J Pharmacol. 2002 May 31;444(3):133-41.

REF 117

Bioactive pyridoacridine alkaloids from the micronesian sponge Oceanapia sp. J Nat Prod. 1998 Feb;61(2):301-5.

REF 118

REF 119

Allosteric modulation, thermodynamics and binding to wild-type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine-like agonist. Br J Pharmacol. 2006 Mar;147(5):533-41.

REF 120

Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists. J Med Chem. 2004 Mar 11;47(6):1434-47.

REF 121

Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9.

REF 122

Structure-activity relationships for 2-substituted adenosines at A1 and A2 adenosine receptors. Pharmacology. 1993;46(2):91-100.

REF 123

Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1697-700.

REF 124

N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A... Eur J Med Chem. 2008 Aug;43(8):1639-47.

REF 125

Synthesis and biological activity of N6-(p-sulfophenyl)alkyl and N6-sulfoalkyl derivatives of adenosine: water-soluble and peripherally selective a... J Med Chem. 1992 Oct 30;35(22):4143-9.

REF 126

(E)-1,3-dialkyl-7-methyl-8-(3,4,5-trimethoxystyryl)xanthines: potent and selective adenosine A2 antagonists. J Med Chem. 1992 Jun 12;35(12):2342-5.

REF 127

Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of t... J Med Chem. 2008 Sep 25;51(18):5875-9.

REF 128

N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands. J Med Chem. 2002 Jul 18;45(15):3271-9.

REF 129

Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. Bioorg Med Chem Lett. 2008 May 1;18(9):2916-9.

REF 130

1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with... J Med Chem. 2009 Jul 9;52(13):3994-4006.

REF 131

2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorg Med Chem. 2003 Feb 6;11(3):347-56.

REF 132

Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66.

REF 133

Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 1998 Jan;357(1):1-9.

REF 134

Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A... J Med Chem. 1998 Jun 4;41(12):2126-33.

REF 135

N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. J Med Chem. 2003 Apr 10;46(8):1492-503.

REF 136

Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. J Med Chem. 2000 Jun 1;43(11):2227-38.

REF 137

A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. J Med Chem. 1998 Oct 8;41(21):3987-93.

REF 138

Inhibition of human mast cell activation with the novel selective adenosine A(2B) receptor antagonist 3-isobutyl-8-pyrrolidinoxanthine (IPDX)(2). Biochem Pharmacol. 2001 Nov 1;62(9):1163-73.

REF 139

[3H]HEMADO--a novel tritiated agonist selective for the human adenosine A3 receptor. Eur J Pharmacol. 2007 Feb 5;556(1-3):14-8.

REF 140

Adenosine receptor agonists: synthesis and biological evaluation of 1-deaza analogues of adenosine derivatives. J Med Chem. 1988 Jun;31(6):1179-83.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.

Prof. Yuzong CHEN

Prof. Feng ZHU