Target Validation Information
Target ID T64382
Target Name Gamma-aminobutyric acid receptor
Target Type
Successful
Drug Potency against Target 6-Chloro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 8 nM
NSC-93394 Drug Info Ki = 4500 nM
2-(3-Chloro-phenyl)-chromen-4-one Drug Info Ki = 614 nM
6-Isopropyl-2-phenyl-chromen-4-one Drug Info Ki = 720 nM [526416]
NSC-19028 Drug Info Ki = 4200 nM [526416]
WEDELOLACTONE Drug Info IC50 = 2000 nM [525981]
Benzoic acid 2,6-diisopropyl-phenyl ester Drug Info IC50 = 15200 nM [534629]
2-(3-Bromo-phenyl)-6-nitro-chromen-4-one Drug Info Ki = 25 nM
3-Isopropoxy-9H-beta-carboline Drug Info IC50 = 500 nM [526755]
RY-066 Drug Info Ki = 48 nM [534718]
Toluene-1-diazonium-3-sulfonic acid anion Drug Info IC50 = 5000 nM [533352]
RO-147437 Drug Info Ki = 1.3 nM [534008]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 780 nM [533975]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info Ki = 6580 nM [528134]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info Ki = 0.26 nM [528134]
3-butoxycarbonyl-4-quinolone Drug Info Ki = 54 nM [528134]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 36 nM [527382]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 1000 nM [531188]
3-Isothiocyanato-9H-beta-carboline Drug Info IC50 = 4 nM [531518]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info IC50 = 310 nM [533975]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info Ki = 0.54 nM [528134]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 1.4 nM [528134]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info Ki = 1870 nM [528034]
2-Oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 810 nM [533975]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 740 nM [533975]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene Drug Info IC50 = 1920 nM [533363]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info Ki = 380 nM [526738]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 19 nM [528134]
6-Nitro-2-phenyl-chromen-4-one Drug Info Ki = 275 nM
4-(5-tert-Butyl-[1,3]dithian-2-yl)-benzonitrile Drug Info Ki = 240 nM [533668]
BL-1020 Drug Info Ki = 3740 nM [552862]
2-(4-Amino-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 2600 nM [526416]
6-Bromo-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 220 nM
6-Bromo-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 3.8 nM
3-Ethoxy-9H-beta-carboline Drug Info Ki = 25.1 nM [534660]
3-amino-3-demethoxythiocolchicine Drug Info IC50 = 5400 nM [528408]
3-Methyl-9H-beta-carboline Drug Info Ki = 1.1 nM [533745]
Phenobarbital Drug Info IC50 = 100000 nM [552210]
6-Bromo-2-phenyl-chromen-4-one Drug Info Ki = 75 nM
PITRAZEPINE Drug Info IC50 = 240 nM [526735]
(2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [533514]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 1000 nM [531188]
3-(isopentyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
(R)-4-amino-2-methylbutanoic acid Drug Info IC50 = 16000 nM [529135]
Ro-154513 Drug Info Ki = 3.8 nM [534122]
U-78875 Drug Info Ki = 1.6 nM [525465]
7-Diazonium-naphthalene-1-sulfonic acid anion Drug Info IC50 < 10000 nM [533352]
BETA-CCM Drug Info IC50 = 2 nM [533763]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 16 nM [528134]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [533514]
THIOCOLCHICOSIDE Drug Info IC50 = 3400 nM [528408]
3-Propoxy-9H-beta-carboline Drug Info IC50 = 11 nM [533363]
3-Nitro-9H-beta-carboline Drug Info IC50 = 125 nM [533363]
Benzyl-(9H-beta-carbolin-6-yl)-amine Drug Info IC50 = 106 nM [533363]
RIPAZEPAM Drug Info IC50 = 670 nM [533397]
GNF-PF-3645 Drug Info Ki = 15 nM [528134]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 360 nM [533975]
3-ethoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 1000 nM [531188]
1-(9H-beta-Carbolin-3-yl)-ethanone Drug Info IC50 = 58 nM [533414]
3-butoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 1000 nM [531188]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 18000 nM [528408]
9H-beta-Carbolin-6-ylamine Drug Info IC50 = 1300 nM [533414]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 9500 nM [534157]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester Drug Info IC50 = 80 nM [533400]
2,4-Diamino-butyric acid(GABA) Drug Info IC50 = 33 nM [533404]
3,3-Diethyl-dihydro-furan-2-one Drug Info IC50 = 750 nM [533975]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [528134]
3-Isobutoxy-9H-beta-carboline Drug Info IC50 = 93 nM [526755]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info Ki = 230 nM [528034]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 2280 nM [533975]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 1.8 nM [528134]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [533514]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 3410 nM [533975]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info Ki = 3290 nM [528080]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [528134]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 680 nM [533975]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info Ki = 2600 nM [528134]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1.7 nM [534155]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 0.6 nM [534155]
3-Chloro-9H-beta-carboline Drug Info IC50 = 45 nM [533363]
3-sec-Butoxy-9H-beta-carboline Drug Info IC50 = 471 nM [526755]
3-Methoxy-9H-beta-carboline Drug Info IC50 = 124 nM [533363]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info Ki = 214 nM [528134]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info Ki = 92 nM [528134]
3-carboxy-6-ethyl-4-quinolone Drug Info Ki = 208 nM [528134]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info Ki = 1.2 nM [526738]
(9H-beta-Carbolin-3-yl)-methanol Drug Info IC50 = 1470 nM [533414]
((E)-3-Amino-propenyl)-methyl-phosphinic acid Drug Info IC50 = 5500 nM [529517]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline Drug Info IC50 = 43.2 nM [534660]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 7000 nM [528408]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 943 nM [528709]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 3800 nM [527382]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 300 nM [533354]
GAMMA-AMINO-BUTANOIC ACID Drug Info IC50 = 24 nM [528408]
RWJ-16979 Drug Info IC50 = 5.9 nM [533762]
3-Amino-propane-1-sulfonic acid Drug Info IC50 = 300 nM
MRK016 Drug Info Ki = 0.2 nM [527853]
8-Diazonium-naphthalene-1-sulfonic acid anion Drug Info IC50 = 10000 nM [533352]
2-(3-Methoxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 99 nM [526416]
RO-194603 Drug Info Ki = 0.2 nM [534008]
N-(9H-beta-Carbolin-3-yl)-formamide Drug Info IC50 = 4700 nM [533400]
RO-145974 Drug Info Ki = 45 nM [534008]
ETIOCHOLANOLONE Drug Info IC50 = 4140 nM [528321]
Ro-4938581 Drug Info Ki = 14 nM [530391]
6-Chloro-2-phenyl-chromen-4-one Drug Info Ki = 164 nM
RO-054520 Drug Info IC50 = 24 nM [533368]
1-(9H-beta-Carbolin-3-yl)-butan-1-one Drug Info IC50 = 2.8 nM [526755]
Isoquinoline-3-carboxylic acid methyl ester Drug Info IC50 = 13200 nM [533363]
9H-beta-Carbolin-3-ol Drug Info IC50 = 4000 nM [533363]
3-Hydroxy-piperidine-4-carboxylic acid Drug Info IC50 = 12000 nM [533544]
ALFAXALONE Drug Info IC50 = 300 nM [534629]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info IC50 = 535 nM [526755]
4-Hydroxy-3,5-diisopropyl-benzaldehyde Drug Info IC50 = 5800 nM [534629]
2-(3-Amino-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 1200 nM [526416]
6-Ethyl-2-phenyl-chromen-4-one Drug Info Ki = 180 nM [526416]
2-(3-Butoxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 710 nM [526416]
(9H-beta-Carbolin-3-yl)-ethyl-amine Drug Info IC50 = 460 nM [533400]
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinoline Drug Info Ki = 270 nM [534155]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info IC50 = 220 nM [533975]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 120 nM [534710]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone Drug Info Ki = 4200 nM [528134]
6-Methyl-2-p-tolyl-chromen-4-one Drug Info Ki = 4400 nM [526416]
3,3-Dimethyl-dihydro-furan-2-one Drug Info IC50 = 9200 nM [533975]
3-(2,2-Dimethyl-propoxy)-9H-beta-carboline Drug Info IC50 = 104 nM [526755]
2,6-Diisopropyl-4-nitro-phenol Drug Info IC50 = 1950 nM [534629]
4-Chloro-2,6-diisopropyl-phenol Drug Info IC50 = 1440 nM [534629]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 2880 nM [528034]
4-Dimethylamino-2,6-diisopropyl-phenol Drug Info IC50 = 5700 nM [534629]
4-Iodo-2,6-diisopropyl-phenol Drug Info IC50 = 1200 nM [534629]
2-(2-Hydroxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 6.2 nM [526416]
2-(2-Methoxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 820 nM [526416]
6-Methyl-2-phenyl-chromen-4-one Drug Info Ki = 180 nM [526416]
2-Phenyl-6-propyl-chromen-4-one Drug Info Ki = 480 nM [526416]
ANDROSTERONE Drug Info IC50 = 410 nM [528321]
2-(2-Amino-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 700 nM [526416]
6-Methyl-2-pyridin-3-yl-chromen-4-one Drug Info Ki = 130 nM [526416]
2-(3-Hydroxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 390 nM [526416]
2-(3-Bromo-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 12 nM [526416]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 3100 nM [533354]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 16 nM [534157]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 16000 nM [533354]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 216 nM [531188]
NORHARMANE Drug Info IC50 = 1620 nM [533363]
3-Butoxy-9H-beta-carboline Drug Info IC50 = 98 nM [526755]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 59 nM [534157]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanol Drug Info IC50 = 76 nM [533414]
3-isobutoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
N-(9H-beta-Carbolin-3-yl)-acetamide Drug Info IC50 = 4000 nM [533400]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline Drug Info Ki = 6573 nM [534157]
4-Bromo-2,6-diisopropyl-phenol Drug Info IC50 = 1070 nM [534629]
Acetic acid 2,6-diisopropyl-phenyl ester Drug Info IC50 = 8500 nM [534629]
4-Methyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 10000 nM [525949]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 465 nM [528034]
Ridine-5-carboxylic acid ethyl ester Drug Info IC50 = 79 nM [533164]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1 nM [534155]
L-655708 Drug Info Ki = 0.4 nM [527005]
5-tert-Butyl-2-(4-ethynyl-phenyl)-[1,3]dithiane Drug Info Ki = 85 nM [533668]
CGS-17867A Drug Info Ki = 0.77 nM [527100]
Piperidine-4-carboxylic acid Drug Info IC50 = 330 nM [533544]
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluorene Drug Info IC50 = 4 nM [533412]
Piperazine Drug Info EC50 = 22 nM [552483]
U-89267 Drug Info Ki = 0.65 nM [533912]
ZK-93423 Drug Info IC50 = 1 nM [530319]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 180 nM
CGP-27492 Drug Info IC50 = 1700 nM [533678]
Ro-4938581 Drug Info Ki = 80 nM [530391]
3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-ium Drug Info Ki = 1400 nM
Ro-16-6028 Drug Info IC50 = 6.1 nM [534316]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 2160 nM [526094]
5-tert-Butyl-2-(4-fluoro-phenyl)-[1,3]dithiane Drug Info Ki = 1100 nM [533668]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 10500 nM [528408]
NSC-73613 Drug Info Ki = 285 nM
BRL-54504AX Drug Info IC50 = 950 nM
Dextofisopam Drug Info IC50 < 100 nM [553160]
Divaplon Drug Info IC50 = 56 nM [533379]
(2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acid Drug Info IC50 = 500 nM
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info Ki = 17 nM [528134]
6-Bromo-2-(3-bromo-phenyl)-chromen-4-one Drug Info Ki = 19 nM
Pyrrolidin-3-yl-acetic acid Drug Info IC50 = 330 nM [533396]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 9700 nM [528408]
RO-145975 Drug Info Ki = 53 nM [534008]
AMENTOFLAVONE Drug Info IC50 = 14.9 nM [526653]
3-ethoxycarbonyl-4-quinolone Drug Info Ki = 78 nM [528134]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 11300 nM [528408]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 1140 nM [533975]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info Ki = 35 nM [528134]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 0.17 nM [528134]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info IC50 = 240 nM [533975]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 13 nM [528134]
GNF-PF-4421 Drug Info Ki = 20 nM [528134]
2-Phenyl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 22 nM [534155]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [531188]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [533514]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info Ki = 4480 nM [528080]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 820 nM [527382]
Clonazepam Drug Info IC50 = 5 nM [552214]
3-ammoniopropane-1-sulfinate Drug Info IC50 = 470 nM
Ro-151310 Drug Info Ki = 0.85 nM [531044]
ELTANOLONE Drug Info IC50 = 71 nM [528321]
CGS-9895 Drug Info IC50 = 100 nM [533348]
CGS-13767 Drug Info IC50 = 4 nM [529466]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 159 nM [528744]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info Ki = 11000 nM [528744]
ALPIDEM Drug Info IC50 = 26 nM [534470]
4-Ethyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info IC50 = 10300 nM [525949]
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 17000 nM
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info Ki = 13000 nM [528295]
AFLATREME Drug Info IC50 = 4300 nM
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [533514]
CI-218872 Drug Info Ki = 561 nM [531188]
3-propoxy-9H-pyrido[3,4-b]indole Drug Info Ki = 1000 nM [531188]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 2700 nM [531188]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info Ki = 1120 nM [528080]
CGS-9896 Drug Info Ki = 2.4 nM [528080]
6-Bromo-2-(2-nitro-phenyl)-chromen-4-one Drug Info Ki = 208 nM
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 53 nM [534157]
2-(3-Bromo-phenyl)-chromen-4-one Drug Info Ki = 413 nM
ALLOPREGNANOLONE Drug Info IC50 = 74 nM [528321]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 12 nM
Ro-15-3505 Drug Info Ki = 20 nM [533721]
References
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