Target Information
Target General Information | Top | |||||
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Target ID |
T83193
(Former ID: TTDC00049)
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Target Name |
Transient receptor potential cation channel V1 (TRPV1)
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Synonyms |
Vanilloid receptor 1; VR1; TrpV1; Transient receptor potential cation channel subfamily V member 1; Osm-9-like TRP channel 1; OTRPC1; Capsaicin receptor
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Gene Name |
TRPV1
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 1 Target-related Diseases | + | ||||
1 | General pain disorder [ICD-11: 8E43] | |||||
Function |
Ligand-activated non-selective calcium permeant cation channel involved in detection of noxious chemical and thermal stimuli. Seems to mediate proton influx and may be involved in intracellular acidosis in nociceptive neurons. Involved in mediation of inflammatory pain and hyperalgesia. Sensitized by a phosphatidylinositol second messenger system activated by receptor tyrosine kinases, which involves PKC isozymes and PCL. Activation by vanilloids, like capsaicin, and temperatures higher than 42 degrees Celsius, exhibits a time- and Ca(2+)-dependent outward rectification, followed by a long-lasting refractory state. Mild extracellular acidic pH (6.5) potentiates channel activation by noxious heat and vanilloids, whereas acidic conditions (pH <6) directly activate the channel. Can be activated by endogenous compounds, including 12-hydroperoxytetraenoic acid and bradykinin. Acts as ionotropic endocannabinoid receptor with central neuromodulatory effects. Triggers a form of long-term depression (TRPV1-LTD) mediated by the endocannabinoid anandamine in the hippocampus and nucleus accumbens by affecting AMPA receptors endocytosis.
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BioChemical Class |
Transient receptor potential catioin channel
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UniProt ID | ||||||
Sequence |
MKKWSSTDLGAAADPLQKDTCPDPLDGDPNSRPPPAKPQLSTAKSRTRLFGKGDSEEAFP
VDCPHEEGELDSCPTITVSPVITIQRPGDGPTGARLLSQDSVAASTEKTLRLYDRRSIFE AVAQNNCQDLESLLLFLQKSKKHLTDNEFKDPETGKTCLLKAMLNLHDGQNTTIPLLLEI ARQTDSLKELVNASYTDSYYKGQTALHIAIERRNMALVTLLVENGADVQAAAHGDFFKKT KGRPGFYFGELPLSLAACTNQLGIVKFLLQNSWQTADISARDSVGNTVLHALVEVADNTA DNTKFVTSMYNEILMLGAKLHPTLKLEELTNKKGMTPLALAAGTGKIGVLAYILQREIQE PECRHLSRKFTEWAYGPVHSSLYDLSCIDTCEKNSVLEVIAYSSSETPNRHDMLLVEPLN RLLQDKWDRFVKRIFYFNFLVYCLYMIIFTMAAYYRPVDGLPPFKMEKTGDYFRVTGEIL SVLGGVYFFFRGIQYFLQRRPSMKTLFVDSYSEMLFFLQSLFMLATVVLYFSHLKEYVAS MVFSLALGWTNMLYYTRGFQQMGIYAVMIEKMILRDLCRFMFVYIVFLFGFSTAVVTLIE DGKNDSLPSESTSHRWRGPACRPPDSSYNSLYSTCLELFKFTIGMGDLEFTENYDFKAVF IILLLAYVILTYILLLNMLIALMGETVNKIAQESKNIWKLQRAITILDTEKSFLKCMRKA FRSGKLLQVGYTPDGKDDYRWCFRVDEVNWTTWNTNVGIINEDPGNCEGVKRTLSFSLRS SRVSGRHWKNFALVPLLREASARDRQSAQPEEVYLRQFSGSLKPEDAEVFKSPAASGEK Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T67KTV |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 12 Clinical Trial Drugs | + | ||||
1 | DWP-05195 | Drug Info | Phase 2 | Neuropathic pain | [6] | |
2 | GRC-15300 | Drug Info | Phase 2 | Pain | [7] | |
3 | PAC-14028 | Drug Info | Phase 2 | Atopic dermatitis | [8] | |
4 | Resiniferatoxin | Drug Info | Phase 2 | Neuropathic pain | [9], [10] | |
5 | XEN-D0501 | Drug Info | Phase 2 | Overactive bladder | [11] | |
6 | ABT-102 | Drug Info | Phase 1 | Chronic pain | [14] | |
7 | CA-011 | Drug Info | Phase 1 | Chronic pain | [4] | |
8 | GRC-6211 | Drug Info | Phase 1 | Asthma | [15] | |
9 | JNJ-39439335 | Drug Info | Phase 1 | Musculoskeletal pain | [16] | |
10 | MR-1817 | Drug Info | Phase 1 | Pain | [17] | |
11 | PF-3864086 | Drug Info | Phase 1 | Pain | [18] | |
12 | PHE-377 | Drug Info | Phase 1 | Pain | [19] | |
Patented Agent(s) | [+] 137 Patented Agents | + | ||||
1 | PMID25666693-Compound-1 | Drug Info | Patented | Osteoarthritis pain | [20] | |
2 | PMID25666693-Compound-10 | Drug Info | Patented | Osteoarthritis pain | [20] | |
3 | PMID25666693-Compound-101 | Drug Info | Patented | Osteoarthritis pain | [20] | |
4 | PMID25666693-Compound-102 | Drug Info | Patented | Osteoarthritis pain | [20] | |
5 | PMID25666693-Compound-103 | Drug Info | Patented | Osteoarthritis pain | [20] | |
6 | PMID25666693-Compound-104 | Drug Info | Patented | Osteoarthritis pain | [20] | |
7 | PMID25666693-Compound-106 | Drug Info | Patented | Osteoarthritis pain | [20] | |
8 | PMID25666693-Compound-108 | Drug Info | Patented | Osteoarthritis pain | [20] | |
9 | PMID25666693-Compound-109 | Drug Info | Patented | Osteoarthritis pain | [20] | |
10 | PMID25666693-Compound-11 | Drug Info | Patented | Osteoarthritis pain | [20] | |
11 | PMID25666693-Compound-110 | Drug Info | Patented | Osteoarthritis pain | [20] | |
12 | PMID25666693-Compound-111 | Drug Info | Patented | Osteoarthritis pain | [20] | |
13 | PMID25666693-Compound-112 | Drug Info | Patented | Osteoarthritis pain | [20] | |
14 | PMID25666693-Compound-113 | Drug Info | Patented | Osteoarthritis pain | [20] | |
15 | PMID25666693-Compound-114 | Drug Info | Patented | Osteoarthritis pain | [20] | |
16 | PMID25666693-Compound-115 | Drug Info | Patented | Osteoarthritis pain | [20] | |
17 | PMID25666693-Compound-116 | Drug Info | Patented | Osteoarthritis pain | [20] | |
18 | PMID25666693-Compound-117 | Drug Info | Patented | Osteoarthritis pain | [20] | |
19 | PMID25666693-Compound-118 | Drug Info | Patented | Osteoarthritis pain | [20] | |
20 | PMID25666693-Compound-119 | Drug Info | Patented | Osteoarthritis pain | [20] | |
21 | PMID25666693-Compound-12 | Drug Info | Patented | Osteoarthritis pain | [20] | |
22 | PMID25666693-Compound-121 | Drug Info | Patented | Osteoarthritis pain | [20] | |
23 | PMID25666693-Compound-122 | Drug Info | Patented | Osteoarthritis pain | [20] | |
24 | PMID25666693-Compound-123 | Drug Info | Patented | Osteoarthritis pain | [20] | |
25 | PMID25666693-Compound-124 | Drug Info | Patented | Osteoarthritis pain | [20] | |
26 | PMID25666693-Compound-126 | Drug Info | Patented | Osteoarthritis pain | [20] | |
27 | PMID25666693-Compound-127 | Drug Info | Patented | Osteoarthritis pain | [20] | |
28 | PMID25666693-Compound-128 | Drug Info | Patented | Osteoarthritis pain | [20] | |
29 | PMID25666693-Compound-129 | Drug Info | Patented | Osteoarthritis pain | [20] | |
30 | PMID25666693-Compound-13 | Drug Info | Patented | Osteoarthritis pain | [20] | |
31 | PMID25666693-Compound-130 | Drug Info | Patented | Osteoarthritis pain | [20] | |
32 | PMID25666693-Compound-131 | Drug Info | Patented | Osteoarthritis pain | [20] | |
33 | PMID25666693-Compound-133 | Drug Info | Patented | Osteoarthritis pain | [20] | |
34 | PMID25666693-Compound-134 | Drug Info | Patented | Osteoarthritis pain | [20] | |
35 | PMID25666693-Compound-135 | Drug Info | Patented | Osteoarthritis pain | [20] | |
36 | PMID25666693-Compound-136 | Drug Info | Patented | Osteoarthritis pain | [20] | |
37 | PMID25666693-Compound-137 | Drug Info | Patented | Osteoarthritis pain | [20] | |
38 | PMID25666693-Compound-138 | Drug Info | Patented | Osteoarthritis pain | [20] | |
39 | PMID25666693-Compound-139 | Drug Info | Patented | Osteoarthritis pain | [20] | |
40 | PMID25666693-Compound-14 | Drug Info | Patented | Osteoarthritis pain | [20] | |
41 | PMID25666693-Compound-140 | Drug Info | Patented | Osteoarthritis pain | [20] | |
42 | PMID25666693-Compound-141 | Drug Info | Patented | Osteoarthritis pain | [20] | |
43 | PMID25666693-Compound-142 | Drug Info | Patented | Osteoarthritis pain | [20] | |
44 | PMID25666693-Compound-143 | Drug Info | Patented | Osteoarthritis pain | [20] | |
45 | PMID25666693-Compound-145 | Drug Info | Patented | Osteoarthritis pain | [20] | |
46 | PMID25666693-Compound-146 | Drug Info | Patented | Osteoarthritis pain | [20] | |
47 | PMID25666693-Compound-147 | Drug Info | Patented | Osteoarthritis pain | [20] | |
48 | PMID25666693-Compound-148 | Drug Info | Patented | Osteoarthritis pain | [20] | |
49 | PMID25666693-Compound-149 | Drug Info | Patented | Osteoarthritis pain | [20] | |
50 | PMID25666693-Compound-15 | Drug Info | Patented | Osteoarthritis pain | [20] | |
51 | PMID25666693-Compound-150 | Drug Info | Patented | Osteoarthritis pain | [20] | |
52 | PMID25666693-Compound-153 | Drug Info | Patented | Osteoarthritis pain | [20] | |
53 | PMID25666693-Compound-154 | Drug Info | Patented | Osteoarthritis pain | [20] | |
54 | PMID25666693-Compound-155 | Drug Info | Patented | Osteoarthritis pain | [20] | |
55 | PMID25666693-Compound-156 | Drug Info | Patented | Osteoarthritis pain | [20] | |
56 | PMID25666693-Compound-157 | Drug Info | Patented | Osteoarthritis pain | [20] | |
57 | PMID25666693-Compound-158 | Drug Info | Patented | Osteoarthritis pain | [20] | |
58 | PMID25666693-Compound-159 | Drug Info | Patented | Osteoarthritis pain | [20] | |
59 | PMID25666693-Compound-16 | Drug Info | Patented | Osteoarthritis pain | [20] | |
60 | PMID25666693-Compound-162 | Drug Info | Patented | Osteoarthritis pain | [20] | |
61 | PMID25666693-Compound-17 | Drug Info | Patented | Osteoarthritis pain | [20] | |
62 | PMID25666693-Compound-19 | Drug Info | Patented | Osteoarthritis pain | [20] | |
63 | PMID25666693-Compound-2 | Drug Info | Patented | Osteoarthritis pain | [20] | |
64 | PMID25666693-Compound-20 | Drug Info | Patented | Osteoarthritis pain | [20] | |
65 | PMID25666693-Compound-22 | Drug Info | Patented | Osteoarthritis pain | [20] | |
66 | PMID25666693-Compound-23 | Drug Info | Patented | Osteoarthritis pain | [20] | |
67 | PMID25666693-Compound-24 | Drug Info | Patented | Osteoarthritis pain | [20] | |
68 | PMID25666693-Compound-25 | Drug Info | Patented | Osteoarthritis pain | [20] | |
69 | PMID25666693-Compound-26 | Drug Info | Patented | Osteoarthritis pain | [20] | |
70 | PMID25666693-Compound-27 | Drug Info | Patented | Osteoarthritis pain | [20] | |
71 | PMID25666693-Compound-28 | Drug Info | Patented | Osteoarthritis pain | [20] | |
72 | PMID25666693-Compound-29 | Drug Info | Patented | Osteoarthritis pain | [20] | |
73 | PMID25666693-Compound-3 | Drug Info | Patented | Osteoarthritis pain | [20] | |
74 | PMID25666693-Compound-30 | Drug Info | Patented | Osteoarthritis pain | [20] | |
75 | PMID25666693-Compound-31 | Drug Info | Patented | Osteoarthritis pain | [20] | |
76 | PMID25666693-Compound-32 | Drug Info | Patented | Osteoarthritis pain | [20] | |
77 | PMID25666693-Compound-34 | Drug Info | Patented | Osteoarthritis pain | [20] | |
78 | PMID25666693-Compound-35 | Drug Info | Patented | Osteoarthritis pain | [20] | |
79 | PMID25666693-Compound-37 | Drug Info | Patented | Osteoarthritis pain | [20] | |
80 | PMID25666693-Compound-38 | Drug Info | Patented | Osteoarthritis pain | [20] | |
81 | PMID25666693-Compound-4 | Drug Info | Patented | Osteoarthritis pain | [20] | |
82 | PMID25666693-Compound-40 | Drug Info | Patented | Osteoarthritis pain | [20] | |
83 | PMID25666693-Compound-41 | Drug Info | Patented | Osteoarthritis pain | [20] | |
84 | PMID25666693-Compound-42 | Drug Info | Patented | Osteoarthritis pain | [20] | |
85 | PMID25666693-Compound-43 | Drug Info | Patented | Osteoarthritis pain | [20] | |
86 | PMID25666693-Compound-44 | Drug Info | Patented | Osteoarthritis pain | [20] | |
87 | PMID25666693-Compound-46 | Drug Info | Patented | Osteoarthritis pain | [20] | |
88 | PMID25666693-Compound-47 | Drug Info | Patented | Osteoarthritis pain | [20] | |
89 | PMID25666693-Compound-48 | Drug Info | Patented | Osteoarthritis pain | [20] | |
90 | PMID25666693-Compound-49 | Drug Info | Patented | Osteoarthritis pain | [20] | |
91 | PMID25666693-Compound-5 | Drug Info | Patented | Osteoarthritis pain | [20] | |
92 | PMID25666693-Compound-50 | Drug Info | Patented | Osteoarthritis pain | [20] | |
93 | PMID25666693-Compound-51 | Drug Info | Patented | Osteoarthritis pain | [20] | |
94 | PMID25666693-Compound-52 | Drug Info | Patented | Osteoarthritis pain | [20] | |
95 | PMID25666693-Compound-53 | Drug Info | Patented | Osteoarthritis pain | [20] | |
96 | PMID25666693-Compound-55 | Drug Info | Patented | Osteoarthritis pain | [20] | |
97 | PMID25666693-Compound-56 | Drug Info | Patented | Osteoarthritis pain | [20] | |
98 | PMID25666693-Compound-57 | Drug Info | Patented | Osteoarthritis pain | [20] | |
99 | PMID25666693-Compound-58 | Drug Info | Patented | Osteoarthritis pain | [20] | |
100 | PMID25666693-Compound-59 | Drug Info | Patented | Osteoarthritis pain | [20] | |
101 | PMID25666693-Compound-6 | Drug Info | Patented | Osteoarthritis pain | [20] | |
102 | PMID25666693-Compound-60 | Drug Info | Patented | Osteoarthritis pain | [20] | |
103 | PMID25666693-Compound-61 | Drug Info | Patented | Osteoarthritis pain | [20] | |
104 | PMID25666693-Compound-62 | Drug Info | Patented | Osteoarthritis pain | [20] | |
105 | PMID25666693-Compound-63 | Drug Info | Patented | Osteoarthritis pain | [20] | |
106 | PMID25666693-Compound-65 | Drug Info | Patented | Osteoarthritis pain | [20] | |
107 | PMID25666693-Compound-66 | Drug Info | Patented | Osteoarthritis pain | [20] | |
108 | PMID25666693-Compound-69 | Drug Info | Patented | Osteoarthritis pain | [20] | |
109 | PMID25666693-Compound-7 | Drug Info | Patented | Osteoarthritis pain | [20] | |
110 | PMID25666693-Compound-70 | Drug Info | Patented | Osteoarthritis pain | [20] | |
111 | PMID25666693-Compound-71 | Drug Info | Patented | Osteoarthritis pain | [20] | |
112 | PMID25666693-Compound-72 | Drug Info | Patented | Osteoarthritis pain | [20] | |
113 | PMID25666693-Compound-73 | Drug Info | Patented | Osteoarthritis pain | [20] | |
114 | PMID25666693-Compound-74 | Drug Info | Patented | Osteoarthritis pain | [20] | |
115 | PMID25666693-Compound-75 | Drug Info | Patented | Osteoarthritis pain | [20] | |
116 | PMID25666693-Compound-76 | Drug Info | Patented | Osteoarthritis pain | [20] | |
117 | PMID25666693-Compound-77 | Drug Info | Patented | Osteoarthritis pain | [20] | |
118 | PMID25666693-Compound-78 | Drug Info | Patented | Osteoarthritis pain | [20] | |
119 | PMID25666693-Compound-79 | Drug Info | Patented | Osteoarthritis pain | [20] | |
120 | PMID25666693-Compound-8 | Drug Info | Patented | Osteoarthritis pain | [20] | |
121 | PMID25666693-Compound-80 | Drug Info | Patented | Osteoarthritis pain | [20] | |
122 | PMID25666693-Compound-81 | Drug Info | Patented | Osteoarthritis pain | [20] | |
123 | PMID25666693-Compound-82 | Drug Info | Patented | Osteoarthritis pain | [20] | |
124 | PMID25666693-Compound-84 | Drug Info | Patented | Osteoarthritis pain | [20] | |
125 | PMID25666693-Compound-85 | Drug Info | Patented | Osteoarthritis pain | [20] | |
126 | PMID25666693-Compound-86 | Drug Info | Patented | Osteoarthritis pain | [20] | |
127 | PMID25666693-Compound-87 | Drug Info | Patented | Osteoarthritis pain | [20] | |
128 | PMID25666693-Compound-88 | Drug Info | Patented | Osteoarthritis pain | [20] | |
129 | PMID25666693-Compound-9 | Drug Info | Patented | Osteoarthritis pain | [20] | |
130 | PMID25666693-Compound-90 | Drug Info | Patented | Osteoarthritis pain | [20] | |
131 | PMID25666693-Compound-92 | Drug Info | Patented | Osteoarthritis pain | [20] | |
132 | PMID25666693-Compound-93 | Drug Info | Patented | Osteoarthritis pain | [20] | |
133 | PMID25666693-Compound-94 | Drug Info | Patented | Osteoarthritis pain | [20] | |
134 | PMID25666693-Compound-95 | Drug Info | Patented | Osteoarthritis pain | [20] | |
135 | PMID25666693-Compound-97 | Drug Info | Patented | Osteoarthritis pain | [20] | |
136 | PMID25666693-Compound-98 | Drug Info | Patented | Osteoarthritis pain | [20] | |
137 | PMID25666693-Compound-99 | Drug Info | Patented | Osteoarthritis pain | [20] | |
Discontinued Drug(s) | [+] 7 Discontinued Drugs | + | ||||
1 | AZD1386 | Drug Info | Discontinued in Phase 2 | Gastroesophageal reflux disease | [22], [23] | |
2 | DA-5018 | Drug Info | Discontinued in Phase 2 | Postherpetic neuralgia | [10] | |
3 | JTS-653 | Drug Info | Discontinued in Phase 2 | Pain | [24] | |
4 | Nuvanil | Drug Info | Discontinued in Phase 2 | Pain | [25] | |
5 | AMG-517 | Drug Info | Discontinued in Phase 1 | Chronic pain | [26], [27] | |
6 | AMG-8562 | Drug Info | Terminated | Pain | [30] | |
7 | BL-1872 | Drug Info | Terminated | Pain | [31] | |
Preclinical Drug(s) | [+] 1 Preclinical Drugs | + | ||||
1 | A-425619 | Drug Info | Preclinical | Pain | [28], [29] | |
Mode of Action | [+] 7 Modes of Action | + | ||||
Antagonist | [+] 150 Antagonist drugs | + | ||||
1 | DWP-05195 | Drug Info | [32] | |||
2 | GRC-15300 | Drug Info | [33] | |||
3 | PAC-14028 | Drug Info | [34] | |||
4 | XEN-D0501 | Drug Info | [36] | |||
5 | GRC-6211 | Drug Info | [38] | |||
6 | JNJ-39439335 | Drug Info | [39] | |||
7 | MR-1817 | Drug Info | [40] | |||
8 | PF-3864086 | Drug Info | [41] | |||
9 | PHE-377 | Drug Info | [42] | |||
10 | PMID25666693-Compound-1 | Drug Info | [20] | |||
11 | PMID25666693-Compound-10 | Drug Info | [20] | |||
12 | PMID25666693-Compound-101 | Drug Info | [20] | |||
13 | PMID25666693-Compound-102 | Drug Info | [20] | |||
14 | PMID25666693-Compound-103 | Drug Info | [20] | |||
15 | PMID25666693-Compound-104 | Drug Info | [20] | |||
16 | PMID25666693-Compound-106 | Drug Info | [20] | |||
17 | PMID25666693-Compound-108 | Drug Info | [20] | |||
18 | PMID25666693-Compound-109 | Drug Info | [20] | |||
19 | PMID25666693-Compound-11 | Drug Info | [20] | |||
20 | PMID25666693-Compound-110 | Drug Info | [20] | |||
21 | PMID25666693-Compound-111 | Drug Info | [20] | |||
22 | PMID25666693-Compound-112 | Drug Info | [20] | |||
23 | PMID25666693-Compound-113 | Drug Info | [20] | |||
24 | PMID25666693-Compound-114 | Drug Info | [20] | |||
25 | PMID25666693-Compound-115 | Drug Info | [20] | |||
26 | PMID25666693-Compound-116 | Drug Info | [20] | |||
27 | PMID25666693-Compound-117 | Drug Info | [20] | |||
28 | PMID25666693-Compound-118 | Drug Info | [20] | |||
29 | PMID25666693-Compound-119 | Drug Info | [20] | |||
30 | PMID25666693-Compound-12 | Drug Info | [20] | |||
31 | PMID25666693-Compound-121 | Drug Info | [20] | |||
32 | PMID25666693-Compound-122 | Drug Info | [20] | |||
33 | PMID25666693-Compound-123 | Drug Info | [20] | |||
34 | PMID25666693-Compound-124 | Drug Info | [20] | |||
35 | PMID25666693-Compound-126 | Drug Info | [20] | |||
36 | PMID25666693-Compound-127 | Drug Info | [20] | |||
37 | PMID25666693-Compound-128 | Drug Info | [20] | |||
38 | PMID25666693-Compound-129 | Drug Info | [20] | |||
39 | PMID25666693-Compound-13 | Drug Info | [20] | |||
40 | PMID25666693-Compound-130 | Drug Info | [20] | |||
41 | PMID25666693-Compound-131 | Drug Info | [20] | |||
42 | PMID25666693-Compound-133 | Drug Info | [20] | |||
43 | PMID25666693-Compound-134 | Drug Info | [20] | |||
44 | PMID25666693-Compound-135 | Drug Info | [20] | |||
45 | PMID25666693-Compound-136 | Drug Info | [20] | |||
46 | PMID25666693-Compound-137 | Drug Info | [20] | |||
47 | PMID25666693-Compound-138 | Drug Info | [20] | |||
48 | PMID25666693-Compound-139 | Drug Info | [20] | |||
49 | PMID25666693-Compound-14 | Drug Info | [20] | |||
50 | PMID25666693-Compound-140 | Drug Info | [20] | |||
51 | PMID25666693-Compound-141 | Drug Info | [20] | |||
52 | PMID25666693-Compound-142 | Drug Info | [20] | |||
53 | PMID25666693-Compound-143 | Drug Info | [20] | |||
54 | PMID25666693-Compound-145 | Drug Info | [20] | |||
55 | PMID25666693-Compound-146 | Drug Info | [20] | |||
56 | PMID25666693-Compound-147 | Drug Info | [20] | |||
57 | PMID25666693-Compound-148 | Drug Info | [20] | |||
58 | PMID25666693-Compound-149 | Drug Info | [20] | |||
59 | PMID25666693-Compound-15 | Drug Info | [20] | |||
60 | PMID25666693-Compound-150 | Drug Info | [20] | |||
61 | PMID25666693-Compound-153 | Drug Info | [20] | |||
62 | PMID25666693-Compound-154 | Drug Info | [20] | |||
63 | PMID25666693-Compound-155 | Drug Info | [20] | |||
64 | PMID25666693-Compound-156 | Drug Info | [20] | |||
65 | PMID25666693-Compound-157 | Drug Info | [20] | |||
66 | PMID25666693-Compound-158 | Drug Info | [20] | |||
67 | PMID25666693-Compound-159 | Drug Info | [20] | |||
68 | PMID25666693-Compound-16 | Drug Info | [20] | |||
69 | PMID25666693-Compound-162 | Drug Info | [20] | |||
70 | PMID25666693-Compound-17 | Drug Info | [20] | |||
71 | PMID25666693-Compound-19 | Drug Info | [20] | |||
72 | PMID25666693-Compound-2 | Drug Info | [20] | |||
73 | PMID25666693-Compound-20 | Drug Info | [20] | |||
74 | PMID25666693-Compound-22 | Drug Info | [20] | |||
75 | PMID25666693-Compound-23 | Drug Info | [20] | |||
76 | PMID25666693-Compound-24 | Drug Info | [20] | |||
77 | PMID25666693-Compound-25 | Drug Info | [20] | |||
78 | PMID25666693-Compound-26 | Drug Info | [20] | |||
79 | PMID25666693-Compound-27 | Drug Info | [20] | |||
80 | PMID25666693-Compound-28 | Drug Info | [20] | |||
81 | PMID25666693-Compound-29 | Drug Info | [20] | |||
82 | PMID25666693-Compound-3 | Drug Info | [20] | |||
83 | PMID25666693-Compound-30 | Drug Info | [20] | |||
84 | PMID25666693-Compound-31 | Drug Info | [20] | |||
85 | PMID25666693-Compound-32 | Drug Info | [20] | |||
86 | PMID25666693-Compound-34 | Drug Info | [20] | |||
87 | PMID25666693-Compound-35 | Drug Info | [20] | |||
88 | PMID25666693-Compound-37 | Drug Info | [20] | |||
89 | PMID25666693-Compound-38 | Drug Info | [20] | |||
90 | PMID25666693-Compound-4 | Drug Info | [20] | |||
91 | PMID25666693-Compound-40 | Drug Info | [20] | |||
92 | PMID25666693-Compound-41 | Drug Info | [20] | |||
93 | PMID25666693-Compound-42 | Drug Info | [20] | |||
94 | PMID25666693-Compound-43 | Drug Info | [20] | |||
95 | PMID25666693-Compound-44 | Drug Info | [20] | |||
96 | PMID25666693-Compound-46 | Drug Info | [20] | |||
97 | PMID25666693-Compound-47 | Drug Info | [20] | |||
98 | PMID25666693-Compound-48 | Drug Info | [20] | |||
99 | PMID25666693-Compound-49 | Drug Info | [20] | |||
100 | PMID25666693-Compound-5 | Drug Info | [20] | |||
101 | PMID25666693-Compound-50 | Drug Info | [20] | |||
102 | PMID25666693-Compound-51 | Drug Info | [20] | |||
103 | PMID25666693-Compound-52 | Drug Info | [20] | |||
104 | PMID25666693-Compound-53 | Drug Info | [20] | |||
105 | PMID25666693-Compound-55 | Drug Info | [20] | |||
106 | PMID25666693-Compound-56 | Drug Info | [20] | |||
107 | PMID25666693-Compound-57 | Drug Info | [20] | |||
108 | PMID25666693-Compound-58 | Drug Info | [20] | |||
109 | PMID25666693-Compound-59 | Drug Info | [20] | |||
110 | PMID25666693-Compound-6 | Drug Info | [20] | |||
111 | PMID25666693-Compound-60 | Drug Info | [20] | |||
112 | PMID25666693-Compound-61 | Drug Info | [20] | |||
113 | PMID25666693-Compound-62 | Drug Info | [20] | |||
114 | PMID25666693-Compound-63 | Drug Info | [20] | |||
115 | PMID25666693-Compound-65 | Drug Info | [20] | |||
116 | PMID25666693-Compound-66 | Drug Info | [20] | |||
117 | PMID25666693-Compound-69 | Drug Info | [20] | |||
118 | PMID25666693-Compound-7 | Drug Info | [20] | |||
119 | PMID25666693-Compound-70 | Drug Info | [20] | |||
120 | PMID25666693-Compound-71 | Drug Info | [20] | |||
121 | PMID25666693-Compound-72 | Drug Info | [20] | |||
122 | PMID25666693-Compound-73 | Drug Info | [20] | |||
123 | PMID25666693-Compound-74 | Drug Info | [20] | |||
124 | PMID25666693-Compound-75 | Drug Info | [20] | |||
125 | PMID25666693-Compound-76 | Drug Info | [20] | |||
126 | PMID25666693-Compound-77 | Drug Info | [20] | |||
127 | PMID25666693-Compound-78 | Drug Info | [20] | |||
128 | PMID25666693-Compound-79 | Drug Info | [20] | |||
129 | PMID25666693-Compound-8 | Drug Info | [20] | |||
130 | PMID25666693-Compound-80 | Drug Info | [20] | |||
131 | PMID25666693-Compound-81 | Drug Info | [20] | |||
132 | PMID25666693-Compound-82 | Drug Info | [20] | |||
133 | PMID25666693-Compound-84 | Drug Info | [20] | |||
134 | PMID25666693-Compound-85 | Drug Info | [20] | |||
135 | PMID25666693-Compound-86 | Drug Info | [20] | |||
136 | PMID25666693-Compound-87 | Drug Info | [20] | |||
137 | PMID25666693-Compound-88 | Drug Info | [20] | |||
138 | PMID25666693-Compound-9 | Drug Info | [20] | |||
139 | PMID25666693-Compound-90 | Drug Info | [20] | |||
140 | PMID25666693-Compound-92 | Drug Info | [20] | |||
141 | PMID25666693-Compound-93 | Drug Info | [20] | |||
142 | PMID25666693-Compound-94 | Drug Info | [20] | |||
143 | PMID25666693-Compound-95 | Drug Info | [20] | |||
144 | PMID25666693-Compound-97 | Drug Info | [20] | |||
145 | PMID25666693-Compound-98 | Drug Info | [20] | |||
146 | PMID25666693-Compound-99 | Drug Info | [20] | |||
147 | JTS-653 | Drug Info | [35] | |||
148 | ABT-116 | Drug Info | [35] | |||
149 | ASP-8370 | Drug Info | [35] | |||
150 | KMJ-372 | Drug Info | [35] | |||
Activator | [+] 10 Activator drugs | + | ||||
1 | Resiniferatoxin | Drug Info | [10], [35] | |||
2 | 12S-HPETE | Drug Info | [53] | |||
3 | 15S-HPETE | Drug Info | [53] | |||
4 | 2-APB | Drug Info | [55] | |||
5 | 5S-HETE | Drug Info | [35] | |||
6 | 5S-HPETE | Drug Info | [53] | |||
7 | arvanil | Drug Info | [62] | |||
8 | diphenylboronic anhydride | Drug Info | [35] | |||
9 | phenylacetylrinvanil | Drug Info | [68] | |||
10 | PPAHV | Drug Info | [69] | |||
Blocker | [+] 8 Blocker drugs | + | ||||
1 | ABT-102 | Drug Info | [37] | |||
2 | AZD1386 | Drug Info | [43] | |||
3 | AMG-517 | Drug Info | [37], [46] | |||
4 | A-425619 | Drug Info | [37] | |||
5 | AMG-8562 | Drug Info | [37] | |||
6 | A-993610 | Drug Info | [37] | |||
7 | AMG-8563 | Drug Info | [37] | |||
8 | BCTC | Drug Info | [37] | |||
Agonist | [+] 3 Agonist drugs | + | ||||
1 | CA-011 | Drug Info | [4] | |||
2 | Nuvanil | Drug Info | [45] | |||
3 | LASSBio-881 | Drug Info | [35] | |||
Modulator | [+] 3 Modulator drugs | + | ||||
1 | DA-5018 | Drug Info | [44] | |||
2 | BL-1872 | Drug Info | [47] | |||
3 | NE-28345 | Drug Info | [67] | |||
Inhibitor | [+] 41 Inhibitor drugs | + | ||||
1 | (5E,8E,11E,14E)-Icosa-5,8,11,14-tetraenal | Drug Info | [48] | |||
2 | (E)-Octadec-9-enal | Drug Info | [48] | |||
3 | (R)-1-(1H-indazol-4-yl)-3-(1-p-tolylethyl)urea | Drug Info | [49] | |||
4 | (S)-1-(1H-indazol-4-yl)-3-(1-p-tolylethyl)urea | Drug Info | [49] | |||
5 | 1,3-dibenzyl urea | Drug Info | [50] | |||
6 | 1-(4-Bromo-benzyl)-3-quinazolin-8-yl-urea | Drug Info | [51] | |||
7 | 1-(isoquinolin-5-yl)-3-(4-morpholinobenzyl)urea | Drug Info | [52] | |||
8 | 1-benzhydryl-3-(isoquinolin-5-yl)urea | Drug Info | [49] | |||
9 | 2-(4-pentylphenyl)-N-(pyridin-3-yl)acetamide | Drug Info | [54] | |||
10 | 4-(3-methylpyridin-2-yl)-N-p-tolylbenzamide | Drug Info | [56] | |||
11 | 4-(butyl(methyl)amino)-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
12 | 4-(cyclohexylamino)-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
13 | 4-(hexyl(methyl)amino)-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
14 | 4-(methyl(octyl)amino)-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
15 | 4-butyl-N-(7-hydroxynaphthalen-1-yl)benzamide | Drug Info | [54] | |||
16 | 4-butyl-N-(isoquinolin-5-yl)benzamide | Drug Info | [54] | |||
17 | 4-butyl-N-(pyridin-3-yl)benzamide | Drug Info | [54] | |||
18 | 4-butyl-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
19 | 4-butyl-N-phenylbenzamide | Drug Info | [54] | |||
20 | 4-decyl-N-(pyridin-3-yl)benzamide | Drug Info | [54] | |||
21 | 4-heptyl-N-(pyridin-3-yl)benzamide | Drug Info | [54] | |||
22 | 4-hexyl-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
23 | 4-nonyl-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
24 | 4-octyl-N-(pyridin-3-yl)benzamide | Drug Info | [54] | |||
25 | 4-octyl-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
26 | 4-pentyl-N-pyridin-3-yl benzamide | Drug Info | [54] | |||
27 | 4-propyl-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
28 | 4-Pyridin-2-yl-piperazine-1-carboxylic acid amide | Drug Info | [57] | |||
29 | 4-tert-butyl-N-(quinolin-3-yl)benzamide | Drug Info | [54] | |||
30 | 6'-Iodononivamide | Drug Info | [58] | |||
31 | A-795614 | Drug Info | [59] | |||
32 | ATC-120 | Drug Info | [63] | |||
33 | CAPSAZEPINE | Drug Info | [64] | |||
34 | JNJ-17203212 | Drug Info | [64] | |||
35 | N-(4-iodophenyl)-4-(trifluoromethyl)benzamide | Drug Info | [65] | |||
36 | N-methyl-4-pentyl-N-(pyridin-3-yl)benzamide | Drug Info | [54] | |||
37 | N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]lauramide | Drug Info | [66] | |||
38 | N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]linoleamide | Drug Info | [66] | |||
39 | N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]undecanamide | Drug Info | [66] | |||
40 | Pyrrolidin-1-yl-thiourea | Drug Info | [57] | |||
41 | SB-782443 | Drug Info | [70] | |||
Blocker (channel blocker) | [+] 6 Blocker (channel blocker) drugs | + | ||||
1 | 6-iodo-nordihydrocapsaicin | Drug Info | [35] | |||
2 | A778317 | Drug Info | [60] | |||
3 | agatoxin 489 | Drug Info | [61] | |||
4 | NADA | Drug Info | [35] | |||
5 | [125I]resiniferatoxin | Drug Info | [71] | |||
6 | [3H]A778317 | Drug Info | [60] |
Cell-based Target Expression Variations | Top | |||||
---|---|---|---|---|---|---|
Cell-based Target Expression Variations |
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 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 Pathway Affiliation
Biological Network Descriptors
|
Protein Name | Pfam ID | Percentage of Identity (%) | E value |
---|---|---|---|
Ankyrin repeat domain-containing protein 62 (ANKRD62) | 29.851 (40/134) | 3.00E-03 |
KEGG Pathway | Pathway ID | Affiliated Target | Pathway Map |
---|---|---|---|
Neuroactive ligand-receptor interaction | hsa04080 | Affiliated Target |
|
Class: Environmental Information Processing => Signaling molecules and interaction | Pathway Hierarchy | ||
Inflammatory mediator regulation of TRP channels | hsa04750 | Affiliated Target |
|
Class: Organismal Systems => Sensory system | Pathway Hierarchy |
Degree | 4 | Degree centrality | 4.30E-04 | Betweenness centrality | 4.12E-04 |
---|---|---|---|---|---|
Closeness centrality | 1.80E-01 | Radiality | 1.30E+01 | Clustering coefficient | 1.67E-01 |
Neighborhood connectivity | 6.25E+00 | Topological coefficient | 2.74E-01 | Eccentricity | 13 |
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 |
Target Poor or Non Binders | Top | |||||
---|---|---|---|---|---|---|
Target Poor or Non Binders |
Target Affiliated Biological Pathways | Top | |||||
---|---|---|---|---|---|---|
KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
1 | Neuroactive ligand-receptor interaction | |||||
2 | Inflammatory mediator regulation of TRP channels | |||||
NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
1 | IL2 Signaling Pathway | |||||
PID Pathway | [+] 2 PID Pathways | + | ||||
1 | Trk receptor signaling mediated by the MAPK pathway | |||||
2 | Trk receptor signaling mediated by PI3K and PLC-gamma | |||||
Reactome | [+] 1 Reactome Pathways | + | ||||
1 | TRP channels |
Target-Related Models and Studies | Top | |||||
---|---|---|---|---|---|---|
Target Validation | ||||||
Target QSAR Model |
References | Top | |||||
---|---|---|---|---|---|---|
REF 1 | Capsaicin receptor: TRPV1 a promiscuous TRP channel. Handb Exp Pharmacol. 2007;(179):155-71. | |||||
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: 2486). | |||||
REF 3 | ClinicalTrials.gov (NCT00771511) Cervical Capsaicin for Labor Induction and Pain Relief. U.S. National Institutes of Health. | |||||
REF 4 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 5 | ClinicalTrials.gov (NCT01424514) SB705498 Proof of Concept Chamber Challenge in Subjects With Non Allergic Rhinitis. U.S. National Institutes of Health. | |||||
REF 6 | ClinicalTrials.gov (NCT01557010) Evaluate the Efficacy and Safety of DWP05195 in Subjects With Post-Herpetic Neuralgia. U.S. National Institutes of Health. | |||||
REF 7 | ClinicalTrials.gov (NCT01463397) Efficacy and Safety of SAR292833 Administration for 4 Weeks in Patients With Chronic Peripheral Neuropathic Pain. U.S. National Institutes of Health. | |||||
REF 8 | ClinicalTrials.gov (NCT02052531) Efficacy and Safety Study of PAC-14028 Cream in Dermal Pruritus. U.S. National Institutes of Health. | |||||
REF 9 | 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: 2491). | |||||
REF 10 | Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26. | |||||
REF 11 | ClinicalTrials.gov (NCT02233699) A Study to Assess the Efficacy of XEN-D0501 in Reducing the Cough Frequency in Patients With Chronic Idiopathic Cough. U.S. National Institutes of Health. | |||||
REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025854) | |||||
REF 13 | Clinical pipeline report, company report or official report of Biom Therapeutics | |||||
REF 14 | ClinicalTrials.gov (NCT00854659) A Safety, Tolerability and Pharmacokinetic Study of ABT-102 in Healthy Subjects. U.S. National Institutes of Health. | |||||
REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024886) | |||||
REF 16 | ClinicalTrials.gov (NCT01631487) A Study to Investigate the Safety, Tolerability, and Pharmacokinetics of JNJ-39439335 in Healthy Japanese and Caucasian Adult Male Participants. U.S. National Institutes of Health. | |||||
REF 17 | ClinicalTrials.gov (NCT00960180) Study Evaluating Single Ascending Doses of MR1817. U.S. National Institutes of Health. | |||||
REF 18 | ClinicalTrials.gov (NCT00747058) A Study To Investigate The Safety, Toleration And Pharmacokinetics Of Single Oral Doses Of PF-03864086 In Healthy Male Subjects. U.S. National Institutes of Health. | |||||
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 800031648) | |||||
REF 20 | Transient receptor potential vanilloid type 1 antagonists: a patent review (2011 - 2014).Expert Opin Ther Pat. 2015 Mar;25(3):291-318. | |||||
REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023970) | |||||
REF 22 | 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: 7820). | |||||
REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027672) | |||||
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 800028532) | |||||
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 800003434) | |||||
REF 26 | 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: 4129). | |||||
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 800021804) | |||||
REF 28 | 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: 4117). | |||||
REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800023258) | |||||
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 800020509) | |||||
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 800015962) | |||||
REF 32 | TRPV1 Antagonists as Analgesic Agents. The Open Pain Journal, 2013, 6, (Suppl 1: M11), 108-118 . | |||||
REF 33 | The discovery and development of analgesics: new mechanisms, new modalities. J Clin Invest. 2010 November 1; 120(11): 3753-3759. | |||||
REF 34 | Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6. | |||||
REF 35 | 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. (Target id: 507). | |||||
REF 36 | An investigation of the safety and pharmacokinetics of the novel TRPV1 antagonist XEN-D0501 in healthy subjects. Br J Clin Pharmacol. 2011 Dec;72(6):921-31. | |||||
REF 37 | Analgesic potential of TRPV1 antagonists. Biochem Pharmacol. 2009 Aug 1;78(3):211-6. | |||||
REF 38 | GRC-6211, a new oral specific TRPV1 antagonist, decreases bladder overactivity and noxious bladder input in cystitis animal models. J Urol. 2009 Jan;181(1):379-86. | |||||
REF 39 | Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1H-benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep). J Med Chem. 2015 May 14;58(9):3859-74. | |||||
REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030745) | |||||
REF 41 | Clinical pipeline report, company report or official report of pfizer. | |||||
REF 42 | Clinical pipeline report, company report or official report of Pharmeste. | |||||
REF 43 | Clinical pipeline report, company report or official report of AstraZeneca (2009). | |||||
REF 44 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
REF 45 | TRPV1: ON THE ROAD TO PAIN RELIEF. Curr Mol Pharmacol. 2008 November; 1(3): 255-269. | |||||
REF 46 | The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat Rev Drug Discov. 2007 May;6(5):357-72. | |||||
REF 47 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | |||||
REF 48 | The taming of capsaicin. Reversal of the vanilloid activity of N-acylvanillamines by aromatic iodination. J Med Chem. 2005 Jul 14;48(14):4663-9. | |||||
REF 49 | Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher effic... Bioorg Med Chem Lett. 2007 Jul 15;17(14):3894-9. | |||||
REF 50 | Rare dipeptide and urea derivatives from roots of Moringa oleifera as potential anti-inflammatory and antinociceptive agents. Eur J Med Chem. 2009 Jan;44(1):432-6. | |||||
REF 51 | Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quin... J Med Chem. 2005 Feb 10;48(3):744-52. | |||||
REF 52 | In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 ... J Med Chem. 2007 Jul 26;50(15):3651-60. | |||||
REF 53 | Direct activation of capsaicin receptors by products of lipoxygenases: endogenous capsaicin-like substances. Proc Natl Acad Sci U S A. 2000 May 23;97(11):6155-60. | |||||
REF 54 | N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1). Bioorg Med Chem Lett. 2008 Apr 15;18(8):2730-4. | |||||
REF 55 | 2-aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2, and TRPV3. J Biol Chem. 2004 Aug 20;279(34):35741-8. | |||||
REF 56 | From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. | |||||
REF 57 | N-4-methansulfonamidobenzyl-N'-2-substituted-4-tert-butyl-benzyl thioureas as potent vanilloid receptor antagonistic ligands. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1693-6. | |||||
REF 58 | Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin. Bioorg Med Chem. 2010 Nov 15;18(22):8092-105. | |||||
REF 59 | Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists. Bioorg Med Chem. 2008 Sep 15;16(18):8516-25. | |||||
REF 60 | [3H]A-778317 [1-((R)-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand ... J Pharmacol Exp Ther. 2007 Oct;323(1):285-93. | |||||
REF 61 | An inhibitor of TRPV1 channels isolated from funnel Web spider venom. Biochemistry. 2005 Nov 29;44(47):15544-9. | |||||
REF 62 | Cloning and pharmacological characterization of mouse TRPV1. Neurosci Lett. 2004 Nov 3;370(1):55-60. | |||||
REF 63 | Silicon switch approach in TRPV1 antagonist MK-056 and its analogues. Bioorg Med Chem. 2010 Jan 1;18(1):111-6. | |||||
REF 64 | The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain. J Med Chem. 2007 May 31;50(11):2589-96. | |||||
REF 65 | Synthesis of benzamide derivatives as TRPV1 antagonists. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1072-8. | |||||
REF 66 | New N-arachidonoylserotonin analogues with potential "dual" mechanism of action against pain. J Med Chem. 2007 Dec 27;50(26):6554-69. | |||||
REF 67 | The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954. | |||||
REF 68 | Development of the first ultra-potent "capsaicinoid" agonist at transient receptor potential vanilloid type 1 (TRPV1) channels and its therapeutic ... J Pharmacol Exp Ther. 2005 Feb;312(2):561-70. | |||||
REF 69 | Pharmacological differences between the human and rat vanilloid receptor 1 (VR1). Br J Pharmacol. 2001 Mar;132(5):1084-94. | |||||
REF 70 | Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5609-13. | |||||
REF 71 | Iodo-resiniferatoxin, a new potent vanilloid receptor antagonist. Mol Pharmacol. 2001 Jan;59(1):9-15. |
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