Target Validation Information
TTD ID T08910
Target Name GABA(A) receptor gamma-2 (GABRG2)
Type of Target
Successful
Drug Potency against Target (2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [24]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [24]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [24]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info Ki = 1.2 nM [3]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 1140 nM [27]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 16000 nM [23]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info Ki = 3290 nM [10]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 3410 nM [27]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info Ki = 380 nM [3]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info Ki = 1120 nM [10]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1 nM [29]
2-Oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 810 nM [27]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1.7 nM [29]
3,3-Diethyl-dihydro-furan-2-one Drug Info IC50 = 750 nM [27]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info IC50 = 220 nM [27]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info Ki = 10000 nM [19]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [19]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [19]
3-amino-3-demethoxythiocolchicine Drug Info IC50 = 5400 nM [13]
3-Butoxy-9H-beta-carboline Drug Info Ki = 1000 nM [19]
3-butoxycarbonyl-4-quinolone Drug Info Ki = 54 nM [11]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 13 nM [11]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info Ki = 0.54 nM [11]
3-carboxy-6-ethyl-4-quinolone Drug Info Ki = 208 nM [11]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 19 nM [11]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 9700 nM [13]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 11300 nM [13]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 7000 nM [13]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 10500 nM [13]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 18000 nM [13]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 1000 nM [19]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 25.1 nM [31]
3-ethoxycarbonyl-4-quinolone Drug Info Ki = 78 nM [11]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info Ki = 6580 nM [11]
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info Ki = 17 nM [11]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info IC50 = 240 nM [27]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 2280 nM [27]
3-Isobutoxy-9H-beta-carboline Drug Info Ki = 10000 nM [19]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 740 nM [27]
3-Isothiocyanato-9H-beta-carboline Drug Info IC50 = 4 nM [20]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 300 nM [23]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 3100 nM [23]
3-Methyl-9H-beta-carboline Drug Info Ki = 1.1 nM [25]
3-Propoxy-9H-beta-carboline Drug Info Ki = 1000 nM [19]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info IC50 = 310 nM [27]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info Ki = 13000 nM [12]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info Ki = 4480 nM [10]
4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol Drug Info IC50 = 78 nM [18]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 331 nM [9]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 3800 nM [6]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 2200 nM [9]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 820 nM [6]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 36 nM [6]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 220 nM [6]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info Ki = 440 nM [9]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info Ki = 1870 nM [9]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info Ki = 9100 nM [6]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [24]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [24]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 360 nM [27]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 780 nM [27]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 1.4 nM [11]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 0.17 nM [11]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone Drug Info Ki = 4200 nM [11]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 16 nM [11]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info Ki = 92 nM [11]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [11]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [11]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info Ki = 2600 nM [11]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info Ki = 214 nM [11]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info Ki = 35 nM [11]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 1.8 nM [11]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info Ki = 0.26 nM [11]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 680 nM [27]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 12 nM
6-Nitro-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 17000 nM
9H-beta-Carboline-3-carboxylic acid ethyl ester Drug Info Ki = 2700 nM [19]
Allopregnanolone Drug Info IC50 = 74 nM [7]
AMENTOFLAVONE Drug Info IC50 = 14.9 nM [2]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 1000 nM [19]
CGS-13767 Drug Info IC50 = 4 nM [15]
CGS-17867A Drug Info Ki = 0.77 nM [5]
CGS-9895 Drug Info IC50 = 100 nM [22]
CGS-9896 Drug Info Ki = 2.4 nM [10]
CI-218872 Drug Info Ki = 160 nM [25]
ELTANOLONE Drug Info IC50 = 71 nM [7]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 1000 nM [19]
GNF-PF-3645 Drug Info Ki = 15 nM [11]
GNF-PF-4421 Drug Info Ki = 20 nM [11]
GSK683699 Drug Info IC50 = 24 nM [13]
L-655708 Drug Info Ki = 0.4 nM [4]
MRK016 Drug Info Ki = 0.2 nM [8]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide Drug Info Ki = 31.3 nM [14]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 346 nM [14]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 65 nM [14]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 1175 nM [14]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 943 nM [14]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 2160 nM [1]
Ridine-5-carboxylic acid ethyl ester Drug Info IC50 = 79 nM [21]
RO-145974 Drug Info Ki = 45 nM [28]
RO-145975 Drug Info Ki = 53 nM [28]
RO-147437 Drug Info Ki = 1.3 nM [28]
Ro-15-3505 Drug Info Ki = 5.4 nM [28]
RO-194603 Drug Info Ki = 0.2 nM [28]
Ro-4938581 Drug Info Ki = 14 nM [17]
Ro-4938581 Drug Info Ki = 80 nM [17]
RY-066 Drug Info Ki = 48 nM [32]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 216 nM [19]
THIOCOLCHICOSIDE Drug Info IC50 = 3400 nM [13]
U-78875 Drug Info Ki = 1.6 nM [30]
U-89267 Drug Info Ki = 0.65 nM [26]
ZK-93423 Drug Info IC50 = 1 nM [16]
[3H]Ro154513 Drug Info Ki = 15 nM [26]
References
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