Therapeutic Targets Database
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Target Validation Information
TTD IDTTDS00403
Target NameGamma-aminobutyric acid receptor subunit alpha-1    
Type of TargetSuccessful target    
Drug Potency against TargetZK-93423IC50 = 1 nM[1]
CGS-9895IC50 = 100 nM[2]
3-(2,2-Dimethyl-propoxy)-9H-beta-carbolineIC50 = 104 nM[3]
3-demethoxy-3-L-fucopyranosylaminothiocolchicineIC50 = 10500 nM[4]
Benzyl-(9H-beta-carbolin-6-yl)-amineIC50 = 106 nM[5]
3-Propoxy-9H-beta-carbolineIC50 = 11 nM[5]
3-demethoxy-3-D-mannopyranosylaminothiocolchicineIC50 = 11300 nM[4]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-oneIC50 = 1140 nM[6]
3-Methoxy-9H-beta-carbolineIC50 = 124 nM[5]
3-Nitro-9H-beta-carbolineIC50 = 125 nM[5]
9H-beta-Carbolin-6-ylamineIC50 = 1300 nM[7]
Isoquinoline-3-carboxylic acid methyl esterIC50 = 13200 nM[5]
AMENTOFLAVONEIC50 = 14.9 nM[8]
(9H-beta-Carbolin-3-yl)-methanolIC50 = 1470 nM[7]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-oneIC50 = 16000 nM[9]
NORHARMANEIC50 = 1620 nM[5]
CGP-27492IC50 = 1700 nM[10]
3-demethoxy-3D-glucopyranosylaminothiocolchicineIC50 = 18000 nM[4]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluoreneIC50 = 1920 nM[5]
BETA-CCMIC50 = 2 nM[11]
1-(9H-beta-Carbolin-3-yl)-butan-1-oneIC50 = 2.8 nM[3]
3,3-Diisopropyl-dihydro-furan-2-oneIC50 = 220 nM[6]
3-Ethyl-3-methyl-dihydro-furan-2-oneIC50 = 2280 nM[6]
3-Ethoxy-9H-beta-carbolineIC50 = 24 nM[5]
GAMMA-AMINO-BUTANOIC ACIDIC50 = 24 nM[4]
RO-054520IC50 = 24 nM[12]
3-Ethyl-3-isopropyl-dihydro-furan-2-oneIC50 = 240 nM[6]
(4R)-4-ammoniopentanoateIC50 = 2500 nM[13]
(2E,4S)-4-ammoniopent-2-enoateIC50 = 2600 nM[13]
(4S)-4-ammoniopentanoateIC50 = 2900 nM[13]
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-oneIC50 = 300 nM[9]
3-tert-Butyl-3-ethyl-dihydro-furan-2-oneIC50 = 310 nM[6]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-oneIC50 = 3100 nM[9]
Pyrrolidin-3-yl-acetic acidIC50 = 330 nM[14]
THIOCOLCHICOSIDEIC50 = 3400 nM[4]
1-Methyl-5-oxa-spiro[2.4]heptan-4-oneIC50 = 3410 nM[6]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-oneIC50 = 360 nM[6]
3-Isothiocyanato-9H-beta-carbolineIC50 = 4 nM[15]
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluoreneIC50 = 4 nM[16]
CGS-13767IC50 = 4 nM[17]
9H-beta-Carbolin-3-olIC50 = 4000 nM[5]
N-(9H-beta-Carbolin-3-yl)-acetamideIC50 = 4000 nM[18]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carbolineIC50 = 43.2 nM[19]
3-Chloro-9H-beta-carbolineIC50 = 45 nM[5]
(9H-beta-Carbolin-3-yl)-ethyl-amineIC50 = 460 nM[18]
N-(9H-beta-Carbolin-3-yl)-formamideIC50 = 4700 nM[18]
3-sec-Butoxy-9H-beta-carbolineIC50 = 471 nM[3]
RWJ-16979IC50 = 5.9 nM[20]
(2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acidIC50 = 500 nM[21]
3-Isopropoxy-9H-beta-carbolineIC50 = 500 nM[3]
3-(3-Methyl-butoxy)-9H-beta-carbolineIC50 = 535 nM[3]
3-amino-3-demethoxythiocolchicineIC50 = 5400 nM[4]
DivaplonIC50 = 56 nM[22]
1-(9H-beta-Carbolin-3-yl)-ethanoneIC50 = 58 nM[7]
5-[(1S)-1-ammonioethyl]isoxazol-3-olateIC50 = 5800 nM[13]
RIPAZEPAMIC50 = 670 nM[23]
6-Methyl-2-oxa-spiro[4.4]nonan-1-oneIC50 = 680 nM[6]
3-demethoxy-3-D-xylopyranosylaminothiocolchicineIC50 = 7000 nM[4]
ELTANOLONEIC50 = 71 nM[24]
ALLOPREGNANOLONEIC50 = 74 nM[24]
3-Isopropyl-3-methyl-dihydro-furan-2-oneIC50 = 740 nM[6]
3,3-Diethyl-dihydro-furan-2-oneIC50 = 750 nM[6]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanolIC50 = 76 nM[7]
4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-olIC50 = 78 nM[25]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-oneIC50 = 780 nM[6]
ridine-5-carboxylic acid ethyl esterIC50 = 79 nM[26]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl esterIC50 = 80 nM[18]
2-Oxa-spiro[4.4]nonan-1-oneIC50 = 810 nM[6]
3-Isobutoxy-9H-beta-carbolineIC50 = 93 nM[3]
5-[(1R)-1-ammonioethyl]isoxazol-3-olateIC50 = 9500 nM[13]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicineIC50 = 9700 nM[4]
3-Butoxy-9H-beta-carbolineIC50 = 98 nM[3]
6-benzyl-3-propylaminocarbonyl-4-quinoloneKi = 0.048 nM[27]
6-benzyl-3-propoxycarbonyl-4-quinoloneKi = 0.17 nM[27]
RO-194603Ki = 0.2 nM[28]
6-ethyl-3-propylaminocarbonyl-4-quinoloneKi = 0.26 nM[27]
TPA-023Ki = 0.27 nM[29]
3-butylaminocarbonyl-6-ethyl-4-quinoloneKi = 0.54 nM[27]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinolineKi = 0.6 nM[30]
U-89267Ki = 0.65 nM[31]
beta-Carboline-3-carboxylic acid t-butyl esterKi = 0.72 nM[32]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinolineKi = 1 nM[30]
PNU-91571Ki = 1 nM[33]
3-Methyl-9H-beta-carbolineKi = 1.1 nM[34]
(beta-CCE)9H-beta-Carboline-3-carboxylic acidKi = 1.2 nM[35]
Ethyl 9H-pyrido[3,4-b]indole-3-carboxylateKi = 1.2 nM[32]
RO-147437Ki = 1.3 nM[28]
6-benzyl-3-ethoxycarbonyl-4-quinoloneKi = 1.4 nM[27]
U-78875Ki = 1.6 nM[33]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinolineKi = 1.7 nM[30]
6-ethyl-3-propoxycarbonyl-4-quinoloneKi = 1.8 nM[27]
NSC-19028Ki = 1000 nM[36]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-oneKi = 1120 nM[37]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamideKi = 1175 nM[38]
6-Nitro-2-(3-nitro-phenyl)-chromen-4-oneKi = 12 nM[39]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamideKi = 125 nM[38]
3-butoxycarbonyl-6-ethyl-4-quinoloneKi = 13 nM[27]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-olKi = 13000 nM[40]
3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-iumKi = 1400 nM[41]
GNF-PF-3645Ki = 15 nM[27]
Ro-4882224Ki = 15 nM[42]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-oneKi = 16 nM[43]
6-bromo-3-ethoxycarbonyl-4-quinoloneKi = 16 nM[27]
CI-218872Ki = 160 nM[34]
6-Chloro-2-phenyl-chromen-4-oneKi = 164 nM[36]
3-ethoxycarbonyl-6-propyl-4-quinoloneKi = 17 nM[27]
6-Nitro-2-(4-nitro-phenyl)-chromen-4-oneKi = 17000 nM[39]
Ro-4938581Ki = 174 nM[42]
sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylateKi = 18 nM[32]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-oneKi = 180 nM[36]
5-(piperidin-4-yl)isothiazol-3-olKi = 1870 nM[44]
3-cyclopentoxycarbonyl-6-ethyl-4-quinoloneKi = 19 nM[27]
6-Bromo-2-(3-bromo-phenyl)-chromen-4-oneKi = 19 nM[36]
CGS-9896Ki = 2.4 nM[37]
GNF-PF-4421Ki = 20 nM[27]
3-carboxy-6-ethyl-4-quinoloneKi = 208 nM[27]
6-Bromo-2-(2-nitro-phenyl)-chromen-4-oneKi = 208 nM[45]
6-ethyl-3-i-propoxycarbonyl-4-quinoloneKi = 214 nM[27]
2-Phenyl-3H-imidazo[4,5-c]quinolineKi = 22 nM[30]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-olKi = 220 nM[46]
6-Bromo-2-(4-nitro-phenyl)-chromen-4-oneKi = 220 nM[45]
4-Methyl-5-(4-piperidyl)isothiazol-3-olKi = 2200 nM[44]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamideKi = 225 nM[47]
3-isobutoxy-9H-pyrido[3,4-b]indoleKi = 24.9 nM[32]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indoleKi = 245 nM[32]
2-(3-Bromo-phenyl)-6-nitro-chromen-4-oneKi = 25 nM[36]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinoloneKi = 2600 nM[27]
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinolineKi = 270 nM[30]
6-Nitro-2-phenyl-chromen-4-oneKi = 275 nM[36]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinoloneKi = 28 nM[27]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinoloneKi = 28 nM[27]
NSC-73613Ki = 285 nM[36]
6-Bromo-2-(3-nitro-phenyl)-chromen-4-oneKi = 3.8 nM[45]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamideKi = 31.3 nM[38]
1-(4-chlorophenyl)-4-phenyl-1H-imidazoleKi = 3290 nM[37]
4-benzyl-5-(4-piperidyl)isothiazol-3-olKi = 331 nM[44]
N-benzyl-2-(1H-indol-3-yl)-2-oxoacetamideKi = 346 nM[38]
6-ethyl-3-pentoxycarbonyl-4-quinoloneKi = 35 nM[27]
3-(isopentyloxy)-9H-pyrido[3,4-b]indoleKi = 350.2 nM[32]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-olKi = 36 nM[46]
3-butoxy-9H-pyrido[3,4-b]indoleKi = 36.9 nM[32]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamideKi = 380 nM[35]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-olKi = 3800 nM[46]
ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylateKi = 4.8 nM[32]
2-(3-Bromo-phenyl)-chromen-4-oneKi = 413 nM[36]
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinoloneKi = 4200 nM[27]
L-655708;NCGC00025115-02Ki = 44 nM[48]
5-(4-piperidyl)-4-propylisothiazol-3-olKi = 440 nM[44]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazoleKi = 4480 nM[37]
RO-145974Ki = 45 nM[28]
NSC-93394Ki = 4500 nM[36]
3-propoxy-9H-pyrido[3,4-b]indoleKi = 5.3 nM[32]
Ro-154513Ki = 5.3 nM[28]
Ro-151310Ki = 5.4 nM[28]
RO-145975Ki = 53 nM[28]
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-oneKi = 53 nM[43]
3-butoxycarbonyl-4-quinoloneKi = 54 nM[27]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-oneKi = 59 nM[43]
3-ethoxy-9H-pyrido[3,4-b]indoleKi = 6.43 nM[32]
2-(3-Chloro-phenyl)-chromen-4-oneKi = 614 nM[36]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamideKi = 65 nM[38]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazolineKi = 6573 nM[43]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinoloneKi = 6580 nM[27]
GABAZINEKi = 74 nM[44]
GABAZINEKi = 74 nM[46]
6-Bromo-2-phenyl-chromen-4-oneKi = 75 nM[36]
3-ethoxycarbonyl-4-quinoloneKi = 78 nM[27]
6-Chloro-2-(3-nitro-phenyl)-chromen-4-oneKi = 8 nM[36]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-olKi = 820 nM[46]
RY-066Ki = 83 nM[49]
3-(benzyloxy)-9H-pyrido[3,4-b]indoleKi = 830 nM[32]
5-Piperidin-4-yl-isoxazol-3-olKi = 9100 nM[46]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinoloneKi = 92 nM[27]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-oneKi = 9500 nM[43]
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Professor in Department of Pharmacy
National University of Singapore, Singapore


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