Target Validation Information
Target ID T51487
Target Name Gamma-aminobutyric acid receptor subunit alpha-1
Target Type
Successful
Drug Potency against Target NSC-93394 Drug Info Ki = 4500 nM
2-(3-Chloro-phenyl)-chromen-4-one Drug Info Ki = 614 nM
3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-ium Drug Info Ki = 1400 nM
6-Bromo-2-(3-bromo-phenyl)-chromen-4-one Drug Info Ki = 19 nM
6-Bromo-2-(2-nitro-phenyl)-chromen-4-one Drug Info Ki = 208 nM
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 17000 nM
4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol Drug Info IC50 = 78 nM [530818]
RO-054520 Drug Info IC50 = 24 nM [533368]
RY-066 Drug Info Ki = 83 nM [534718]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info Ki = 1120 nM [528080]
RO-145975 Drug Info Ki = 53 nM [534008]
Ro-154513 Drug Info Ki = 5.3 nM [534008]
Ro-4938581 Drug Info Ki = 174 nM [530391]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [528134]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info Ki = 92 nM [528134]
AMENTOFLAVONE Drug Info IC50 = 14.9 nM [526653]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 7000 nM [528408]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [533514]
L-655708 Drug Info Ki = 44 nM [527005]
3-ethoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 6.43 nM [531188]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 740 nM [533975]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone Drug Info Ki = 4200 nM [528134]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info Ki = 35 nM [528134]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 780 nM [533975]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info Ki = 0.54 nM [528134]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info Ki = 1870 nM [528034]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [533514]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info Ki = 4480 nM [528080]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 346 nM [528709]
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinoline Drug Info Ki = 270 nM [534155]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info Ki = 380 nM [526738]
GNF-PF-4421 Drug Info Ki = 20 nM [528134]
3-butoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 36.9 nM [531188]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide Drug Info Ki = 31.3 nM [528709]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 9700 nM [528408]
THIOCOLCHICOSIDE Drug Info IC50 = 3400 nM [528408]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 36 nM [527382]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 16000 nM [533354]
6-Chloro-2-phenyl-chromen-4-one Drug Info Ki = 164 nM
6-Chloro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 8 nM
2-(3-Bromo-phenyl)-6-nitro-chromen-4-one Drug Info Ki = 25 nM
GAMMA-AMINO-BUTANOIC ACID Drug Info IC50 = 24 nM [528408]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 18 nM [531188]
3-isobutoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 24.9 nM [531188]
MRK016 Drug Info Ki = 0.27 nM [527853]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 3800 nM [527382]
N-(9H-beta-Carbolin-3-yl)-acetamide Drug Info IC50 = 4000 nM [533400]
RO-145974 Drug Info Ki = 45 nM [534008]
RO-194603 Drug Info Ki = 0.2 nM [534008]
Ro-4938581 Drug Info Ki = 15 nM [530391]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info Ki = 214 nM [528134]
6-Bromo-2-phenyl-chromen-4-one Drug Info Ki = 75 nM
3-Propoxy-9H-beta-carboline Drug Info IC50 = 11 nM [533363]
Benzyl-(9H-beta-carbolin-6-yl)-amine Drug Info IC50 = 106 nM [533363]
3-Ethoxy-9H-beta-carboline Drug Info IC50 = 24 nM [533363]
3-Isopropoxy-9H-beta-carboline Drug Info IC50 = 500 nM [526755]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info IC50 = 535 nM [526755]
3-Butoxy-9H-beta-carboline Drug Info IC50 = 98 nM [526755]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 220 nM [527382]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 245 nM [531188]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info Ki = 440 nM [528034]
3-propoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 5.3 nM [531188]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester Drug Info IC50 = 80 nM [533400]
NORHARMANE Drug Info IC50 = 1620 nM [533363]
3-carboxy-6-ethyl-4-quinolone Drug Info Ki = 208 nM [528134]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info IC50 = 310 nM [533975]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 360 nM [533975]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 3410 nM [533975]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [528134]
1-(9H-beta-Carbolin-3-yl)-butan-1-one Drug Info IC50 = 2.8 nM [526755]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 0.6 nM [534155]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene Drug Info IC50 = 1920 nM [533363]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 19 nM [528134]
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 53 nM [534157]
RIPAZEPAM Drug Info IC50 = 670 nM [533397]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 59 nM [534157]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info Ki = 9100 nM [527382]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanol Drug Info IC50 = 76 nM [533414]
Isoquinoline-3-carboxylic acid methyl ester Drug Info IC50 = 13200 nM [533363]
N-(9H-beta-Carbolin-3-yl)-formamide Drug Info IC50 = 4700 nM [533400]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline Drug Info Ki = 6573 nM [534157]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 1175 nM [528709]
6-Nitro-2-phenyl-chromen-4-one Drug Info Ki = 275 nM
NSC-19028 Drug Info Ki = 1000 nM
3-(isopentyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 350.2 nM [531188]
CGS-13767 Drug Info IC50 = 4 nM [529466]
CGP-27492 Drug Info IC50 = 1700 nM [533678]
9H-beta-Carbolin-3-ol Drug Info IC50 = 4000 nM [533363]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info Ki = 1.2 nM [526738]
3-Nitro-9H-beta-carboline Drug Info IC50 = 125 nM [533363]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 180 nM
(9H-beta-Carbolin-3-yl)-ethyl-amine Drug Info IC50 = 460 nM [533400]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info IC50 = 220 nM [533975]
3-(2,2-Dimethyl-propoxy)-9H-beta-carboline Drug Info IC50 = 104 nM [526755]
9H-beta-Carbolin-6-ylamine Drug Info IC50 = 1300 nM [533414]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 1140 nM [533975]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 830 nM [531188]
3-Chloro-9H-beta-carboline Drug Info IC50 = 45 nM [533363]
3-Isobutoxy-9H-beta-carboline Drug Info IC50 = 93 nM [526755]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info Ki = 2600 nM [528134]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 2200 nM [528034]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [533514]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info Ki = 3290 nM [528080]
CGS-9896 Drug Info Ki = 2.4 nM [528080]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 300 nM [533354]
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info Ki = 17 nM [528134]
3-sec-Butoxy-9H-beta-carboline Drug Info IC50 = 471 nM [526755]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info Ki = 6580 nM [528134]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1 nM [534155]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 16 nM [534157]
3-Methoxy-9H-beta-carboline Drug Info IC50 = 124 nM [533363]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 13 nM [528134]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 0.17 nM [528134]
1-(9H-beta-Carbolin-3-yl)-ethanone Drug Info IC50 = 58 nM [533414]
2-Phenyl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 22 nM [534155]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 9500 nM [534157]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 10500 nM [528408]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 11300 nM [528408]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 3100 nM [533354]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 65 nM [528709]
U-78875 Drug Info Ki = 1.6 nM [525465]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 331 nM [528034]
3-Isothiocyanato-9H-beta-carboline Drug Info IC50 = 4 nM [531518]
3,3-Diethyl-dihydro-furan-2-one Drug Info IC50 = 750 nM [533975]
(2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acid Drug Info IC50 = 500 nM
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline Drug Info IC50 = 43.2 nM [534660]
ZK-93423 Drug Info IC50 = 1 nM [530319]
Ridine-5-carboxylic acid ethyl ester Drug Info IC50 = 79 nM [533164]
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluorene Drug Info IC50 = 4 nM [533412]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 225 nM [526094]
NSC-73613 Drug Info Ki = 285 nM
ELTANOLONE Drug Info IC50 = 71 nM [527511]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1.7 nM [534155]
CGS-9895 Drug Info IC50 = 100 nM [533348]
Pyrrolidin-3-yl-acetic acid Drug Info IC50 = 330 nM [533396]
6-Bromo-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 220 nM
3-Methyl-9H-beta-carboline Drug Info Ki = 1.1 nM [533745]
Divaplon Drug Info IC50 = 56 nM [533379]
BETA-CCM Drug Info IC50 = 2 nM [533763]
U-89267 Drug Info Ki = 0.65 nM [533912]
3-amino-3-demethoxythiocolchicine Drug Info IC50 = 5400 nM [528408]
Ro-151310 Drug Info Ki = 5.4 nM [534008]
CI-218872 Drug Info Ki = 160 nM [533745]
RO-147437 Drug Info Ki = 1.3 nM [534008]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 16 nM [528134]
ALLOPREGNANOLONE Drug Info IC50 = 74 nM [527511]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [533514]
RWJ-16979 Drug Info IC50 = 5.9 nM [533762]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 1.8 nM [528134]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info IC50 = 240 nM [533975]
GNF-PF-3645 Drug Info Ki = 15 nM [528134]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 1.4 nM [528134]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 2280 nM [533975]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 820 nM [527382]
2-Oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 810 nM [533975]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 680 nM [533975]
3-butoxycarbonyl-4-quinolone Drug Info Ki = 54 nM [528134]
(2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [533514]
3-ethoxycarbonyl-4-quinolone Drug Info Ki = 78 nM [528134]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info Ki = 0.26 nM [528134]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 18000 nM [528408]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 125 nM [528709]
6-Bromo-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 3.8 nM
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info Ki = 13000 nM [528295]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 12 nM
2-(3-Bromo-phenyl)-chromen-4-one Drug Info Ki = 413 nM
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 0.72 nM [531188]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 4.8 nM [531188]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 1.2 nM [531188]
(9H-beta-Carbolin-3-yl)-methanol Drug Info IC50 = 1470 nM [533414]
References
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Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
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Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
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Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
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Ref 527853J Med Chem. 2005 Nov 17;48(23):7089-92.7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
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Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 530391Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4. Epub 2009 Aug 15.The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
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Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 527382J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 528034J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 533400J Med Chem. 1985 Jun;28(6):824-8.3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 534155J Med Chem. 1996 Jul 5;39(14):2844-51.Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
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Ref 527382J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Ref 533414J Med Chem. 1987 Apr;30(4):750-3.Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 533400J Med Chem. 1985 Jun;28(6):824-8.3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam.
Ref 534157J Med Chem. 1996 Jul 19;39(15):2915-21.Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand.
Ref 528709J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 529466J Med Chem. 1991 Jan;34(1):281-90.Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones.
Ref 533678J Med Chem. 1995 Aug 18;38(17):3297-312.Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 526738J Med Chem. 1992 Jun 12;35(12):2214-20.Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 533400J Med Chem. 1985 Jun;28(6):824-8.3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 533414J Med Chem. 1987 Apr;30(4):750-3.Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528034J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 528080J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
Ref 528080J Med Chem. 2006 Mar 23;49(6):1855-66.Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors.
Ref 533354J Med Chem. 1988 Jan;31(1):1-3.Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 526755J Med Chem. 1992 Oct 30;35(22):4001-10.Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 534155J Med Chem. 1996 Jul 5;39(14):2844-51.Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Ref 534157J Med Chem. 1996 Jul 19;39(15):2915-21.Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand.
Ref 533363J Med Chem. 1988 Sep;31(9):1854-61.Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533414J Med Chem. 1987 Apr;30(4):750-3.Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Ref 534155J Med Chem. 1996 Jul 5;39(14):2844-51.Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Ref 534157J Med Chem. 1996 Jul 19;39(15):2915-21.Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 533354J Med Chem. 1988 Jan;31(1):1-3.Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
Ref 528709J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Ref 525465J Med Chem. 1999 Apr 8;42(7):1123-44.Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality.
Ref 528034J Med Chem. 2006 Feb 23;49(4):1388-96.Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology.
Ref 531518J Med Chem. 1990 Sep;33(9):2343-57.Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 534660J Med Chem. 1998 Jul 2;41(14):2537-52.Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) and the full agonist 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (Zk 93423) at wild type and recombinant GABAA receptors.
Ref 530319J Med Chem. 1990 Mar;33(3):1062-9.Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester.
Ref 533164J Med Chem. 1989 Dec;32(12):2561-73.Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents.
Ref 533412J Med Chem. 1987 Mar;30(3):456-8.Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands.
Ref 526094J Med Chem. 2001 Jul 5;44(14):2286-97.Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular modeling analysis of the structure-activity relationships.
Ref 527511J Med Chem. 2005 Apr 21;48(8):3051-9.Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)-and (3alpha,5beta)-3-hydroxypregnan-20-one.
Ref 534155J Med Chem. 1996 Jul 5;39(14):2844-51.Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands.
Ref 533348J Med Chem. 1987 Oct;30(10):1737-42.1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding.
Ref 533396J Med Chem. 1985 May;28(5):653-60.Orally active and potent inhibitors of gamma-aminobutyric acid uptake.
Ref 533745J Med Chem. 1994 Dec 23;37(26):4576-80.Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
Ref 533379J Med Chem. 1988 Jun;31(6):1220-6.(Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics.
Ref 533763J Med Chem. 1995 Jan 6;38(1):189-98.Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high affinities for thebenzodiazepine receptor.
Ref 533912J Med Chem. 1994 Mar 18;37(6):758-68.Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 533745J Med Chem. 1994 Dec 23;37(26):4576-80.Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor.
Ref 534008J Med Chem. 1993 Apr 16;36(8):1001-6.Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepine receptors.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 527511J Med Chem. 2005 Apr 21;48(8):3051-9.Neurosteroid analogues. 10. The effect of methyl group substitution at the C-6 and C-7 positions on the GABA modulatory and anesthetic actions of (3alpha,5alpha)-and (3alpha,5beta)-3-hydroxypregnan-20-one.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 533762J Med Chem. 1995 Jan 6;38(1):16-20.Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 527382J Med Chem. 2005 Jan 27;48(2):427-39.Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 533975J Med Chem. 1994 Jan 21;37(2):275-86.Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant alpha,alpha-disubstituted gamma-butyrolactones.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 533514J Med Chem. 1981 Dec;24(12):1377-83.gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528134J Med Chem. 2006 Apr 20;49(8):2526-33.4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore modeling.
Ref 528408J Med Chem. 2006 Sep 7;49(18):5571-7.3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds.
Ref 528709J Med Chem. 2007 Apr 5;50(7):1627-34. Epub 2007 Mar 3.Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Ref 528295J Med Chem. 2006 Jul 13;49(14):4442-6.Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 531188Bioorg Med Chem. 2010 Nov 1;18(21):7548-64. Epub 2010 Sep 29.Design, synthesis, and subtype selectivity of 3,6-disubstituted |A-carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents for treatment of alcohol abuse.
Ref 533414J Med Chem. 1987 Apr;30(4):750-3.Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.

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