Target Validation Information
TTD ID T51487
Target Name GABA(A) receptor alpha-1 (GABRA1)
Type of Target
Successful
Drug Potency against Target (2-Amino-4,5-dihydro-thiazol-4-yl)-acetic acid Drug Info IC50 = 500 nM
(2E,4S)-4-ammoniopent-2-enoate Drug Info IC50 = 2600 nM [33]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [33]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [33]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanol Drug Info IC50 = 76 nM [32]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester Drug Info IC50 = 80 nM [30]
(9H-beta-Carbolin-3-yl)-ethyl-amine Drug Info IC50 = 460 nM [30]
(9H-beta-Carbolin-3-yl)-methanol Drug Info IC50 = 1470 nM [32]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info Ki = 1.2 nM [4]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 1140 nM [39]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 16000 nM [24]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info Ki = 3290 nM [11]
1-(9H-beta-Carbolin-3-yl)-butan-1-one Drug Info IC50 = 2.8 nM [5]
1-(9H-beta-Carbolin-3-yl)-ethanone Drug Info IC50 = 58 nM [32]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 3410 nM [39]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info Ki = 380 nM [4]
2-(3-Bromo-phenyl)-6-nitro-chromen-4-one Drug Info Ki = 25 nM
2-(3-Bromo-phenyl)-chromen-4-one Drug Info Ki = 413 nM
2-(3-Chloro-phenyl)-chromen-4-one Drug Info Ki = 614 nM
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinoline Drug Info Ki = 270 nM [41]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info Ki = 1120 nM [11]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 16 nM [42]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 0.6 nM [41]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1 nM [41]
2-Oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 810 nM [39]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 9500 nM [42]
2-Phenyl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 22 nM [41]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline Drug Info Ki = 6573 nM [42]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 59 nM [42]
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 53 nM [42]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1.7 nM [41]
3,3-Diethyl-dihydro-furan-2-one Drug Info IC50 = 750 nM [39]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info IC50 = 220 nM [39]
3-(2,2-Dimethyl-propoxy)-9H-beta-carboline Drug Info IC50 = 104 nM [5]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info Ki = 350.2 nM [20]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info IC50 = 535 nM [5]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 830 nM [20]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 245 nM [20]
3-amino-3-demethoxythiocolchicine Drug Info IC50 = 5400 nM [14]
3-Butoxy-9H-beta-carboline Drug Info Ki = 36.9 nM [20]
3-Butoxy-9H-beta-carboline Drug Info IC50 = 98 nM [5]
3-butoxycarbonyl-4-quinolone Drug Info Ki = 54 nM [12]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 13 nM [12]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info Ki = 0.54 nM [12]
3-carboxy-6-ethyl-4-quinolone Drug Info Ki = 208 nM [12]
3-Chloro-9H-beta-carboline Drug Info IC50 = 45 nM [25]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 19 nM [12]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 9700 nM [14]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 11300 nM [14]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 7000 nM [14]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 10500 nM [14]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 18000 nM [14]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 6.43 nM [20]
3-Ethoxy-9H-beta-carboline Drug Info IC50 = 24 nM [25]
3-ethoxycarbonyl-4-quinolone Drug Info Ki = 78 nM [12]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info Ki = 6580 nM [12]
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info Ki = 17 nM [12]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info IC50 = 240 nM [39]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 2280 nM [39]
3-Isobutoxy-9H-beta-carboline Drug Info Ki = 24.9 nM [20]
3-Isobutoxy-9H-beta-carboline Drug Info IC50 = 93 nM [5]
3-Isopropoxy-9H-beta-carboline Drug Info IC50 = 500 nM [5]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 740 nM [39]
3-Isothiocyanato-9H-beta-carboline Drug Info IC50 = 4 nM [21]
3-Methoxy-9H-beta-carboline Drug Info IC50 = 124 nM [25]
3-Methoxycarbonyl-2-methyl-9H-beta-carbolin-2-ium Drug Info Ki = 1400 nM
3-Methyl-1-phenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 300 nM [24]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 3100 nM [24]
3-Methyl-9H-beta-carboline Drug Info Ki = 1.1 nM [35]
3-Nitro-9H-beta-carboline Drug Info IC50 = 125 nM [25]
3-Propoxy-9H-beta-carboline Drug Info Ki = 5.3 nM [20]
3-Propoxy-9H-beta-carboline Drug Info IC50 = 11 nM [25]
3-sec-Butoxy-9H-beta-carboline Drug Info IC50 = 471 nM [5]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info IC50 = 310 nM [39]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info Ki = 13000 nM [13]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info Ki = 4480 nM [11]
4-(biphenyl-3-yl)-5-(piperidin-4-yl)isoxazol-3-ol Drug Info IC50 = 78 nM [19]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 331 nM [10]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 3800 nM [7]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline Drug Info IC50 = 43.2 nM [43]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 2200 nM [10]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 820 nM [7]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 36 nM [7]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 220 nM [7]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info Ki = 440 nM [10]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info Ki = 1870 nM [10]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info Ki = 9100 nM [7]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [33]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [33]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 360 nM [39]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 780 nM [39]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 1.4 nM [12]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 0.17 nM [12]
6-Bromo-2-(2-nitro-phenyl)-chromen-4-one Drug Info Ki = 208 nM
6-Bromo-2-(3-bromo-phenyl)-chromen-4-one Drug Info Ki = 19 nM
6-Bromo-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 3.8 nM
6-Bromo-2-(4-nitro-phenyl)-chromen-4-one Drug Info Ki = 220 nM
6-Bromo-2-phenyl-chromen-4-one Drug Info Ki = 75 nM
6-bromo-3-ethoxycarbonyl-2-methyl-4-quinolone Drug Info Ki = 4200 nM [12]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 16 nM [12]
6-Chloro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 8 nM
6-Chloro-2-phenyl-chromen-4-one Drug Info Ki = 164 nM
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info Ki = 92 nM [12]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [12]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [12]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info Ki = 2600 nM [12]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info Ki = 214 nM [12]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info Ki = 35 nM [12]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 1.8 nM [12]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info Ki = 0.26 nM [12]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 180 nM
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 680 nM [39]
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
6-Nitro-2-phenyl-chromen-4-one Drug Info Ki = 275 nM
7,12-Dihydro-5,7,12-triaza-indeno[1,2-a]fluorene Drug Info IC50 = 4 nM [31]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene Drug Info IC50 = 1920 nM [25]
9H-beta-Carbolin-3-ol Drug Info IC50 = 4000 nM [25]
9H-beta-Carbolin-6-ylamine Drug Info IC50 = 1300 nM [32]
9H-beta-Carboline-3-carboxylic acid ethyl ester Drug Info Ki = 1.2 nM [20]
Allopregnanolone Drug Info IC50 = 74 nM [8]
AMENTOFLAVONE Drug Info IC50 = 14.9 nM [3]
Benzyl-(9H-beta-carbolin-6-yl)-amine Drug Info IC50 = 106 nM [25]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 0.72 nM [20]
BETA-CCM Drug Info IC50 = 2 nM [37]
CGS-13767 Drug Info IC50 = 4 nM [16]
CGS-9895 Drug Info IC50 = 100 nM [23]
CGS-9896 Drug Info Ki = 2.4 nM [11]
CI-218872 Drug Info Ki = 160 nM [35]
Divaplon Drug Info IC50 = 56 nM [27]
ELTANOLONE Drug Info IC50 = 71 nM [8]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 4.8 nM [20]
flavone Drug Info Ki = 1000 nM
GNF-PF-3645 Drug Info Ki = 15 nM [12]
GNF-PF-4421 Drug Info Ki = 20 nM [12]
GSK683699 Drug Info IC50 = 24 nM [14]
Isoquinoline-3-carboxylic acid methyl ester Drug Info IC50 = 13200 nM [25]
L-655708 Drug Info Ki = 44 nM [6]
MRK016 Drug Info Ki = 0.27 nM [9]
N-(9H-beta-Carbolin-3-yl)-acetamide Drug Info IC50 = 4000 nM [30]
N-(9H-beta-Carbolin-3-yl)-formamide Drug Info IC50 = 4700 nM [30]
N-(p-methylbenzyl)-5-nitroindol-3-ylglyoxylamide Drug Info Ki = 31.3 nM [15]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 346 nM [15]
N-benzyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 65 nM [15]
N-butyl-2-(1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 1175 nM [15]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 125 nM [15]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 225 nM [2]
NORHARMANE Drug Info IC50 = 1620 nM [25]
NSC-73613 Drug Info Ki = 285 nM
NSC-93394 Drug Info Ki = 4500 nM
Pyrrolidin-3-yl-acetic acid Drug Info IC50 = 330 nM [28]
Ridine-5-carboxylic acid ethyl ester Drug Info IC50 = 79 nM [22]
RIPAZEPAM Drug Info IC50 = 670 nM [29]
RO-054520 Drug Info IC50 = 24 nM [26]
RO-145974 Drug Info Ki = 45 nM [40]
RO-145975 Drug Info Ki = 53 nM [40]
RO-147437 Drug Info Ki = 1.3 nM [40]
Ro-15-3505 Drug Info Ki = 5.4 nM [40]
RO-194603 Drug Info Ki = 0.2 nM [40]
Ro-4938581 Drug Info Ki = 174 nM [18]
Ro-4938581 Drug Info Ki = 15 nM [18]
RWJ-16979 Drug Info IC50 = 5.9 nM [36]
RY-066 Drug Info Ki = 83 nM [44]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 18 nM [20]
THIOCOLCHICOSIDE Drug Info IC50 = 3400 nM [14]
U-78875 Drug Info Ki = 1.6 nM [1]
U-89267 Drug Info Ki = 0.65 nM [38]
ZK-93423 Drug Info IC50 = 1 nM [17]
[3H]CGP27492 Drug Info IC50 = 1700 nM [34]
[3H]Ro154513 Drug Info Ki = 5.3 nM [40]
References
REF 1 Piperazine imidazo[1,5-a]quinoxaline ureas as high-affinity GABAA ligands of dual functionality. J Med Chem. 1999 Apr 8;42(7):1123-44.
REF 2 Novel N-(arylalkyl)indol-3-ylglyoxylylamides targeted as ligands of the benzodiazepine receptor: synthesis, biological evaluation, and molecular mo... J Med Chem. 2001 Jul 5;44(14):2286-97.
REF 3 Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
REF 4 Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. J Med Chem. 1992 Jun 12;35(12):2214-20.
REF 5 Predictive binding of beta-carboline inverse agonists and antagonists via the CoMFA/GOLPE approach. J Med Chem. 1992 Oct 30;35(22):4001-10.
REF 6 3-phenyl-6-(2-pyridyl)methyloxy-1,2,4-triazolo[3,4-a]phthalazines and analogues: high-affinity gamma-aminobutyric acid-A benzodiazepine receptor li... J Med Chem. 2004 Mar 25;47(7):1807-22.
REF 7 Potent 4-aryl- or 4-arylalkyl-substituted 3-isoxazolol GABA(A) antagonists: synthesis, pharmacology, and molecular modeling. J Med Chem. 2005 Jan 27;48(2):427-39.
REF 8 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 (... J Med Chem. 2005 Apr 21;48(8):3051-9.
REF 9 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-a... J Med Chem. 2005 Nov 17;48(23):7089-92.
REF 10 Potent 4-arylalkyl-substituted 3-isothiazolol GABA(A) competitive/noncompetitive antagonists: synthesis and pharmacology. J Med Chem. 2006 Feb 23;49(4):1388-96.
REF 11 Synthesis, pharmacology, and structure-activity relationships of novel imidazolones and pyrrolones as modulators of GABAA receptors. J Med Chem. 2006 Mar 23;49(6):1855-66.
REF 12 4-quinolone derivatives: high-affinity ligands at the benzodiazepine site of brain GABA A receptors. synthesis, pharmacology, and pharmacophore mod... J Med Chem. 2006 Apr 20;49(8):2526-33.
REF 13 Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of ga... J Med Chem. 2006 Jul 13;49(14):4442-6.
REF 14 3-demethoxy-3-glycosylaminothiocolchicines: Synthesis of a new class of putative muscle relaxant compounds. J Med Chem. 2006 Sep 7;49(18):5571-7.
REF 15 Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-... J Med Chem. 2007 Apr 5;50(7):1627-34.
REF 16 Synthesis and benzodiazepine binding activity of a series of novel [1,2,4]triazolo[1,5-c]quinazolin-5(6H)-ones. J Med Chem. 1991 Jan;34(1):281-90.
REF 17 Structural requirements for agonist actions at the benzodiazepine receptor: studies with analogues of 6-(benzyloxy)-4-(methoxymethyl)-beta-carbolin... J Med Chem. 1990 Mar;33(3):1062-9.
REF 18 The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment... Bioorg Med Chem Lett. 2009 Oct 15;19(20):5940-4.
REF 19 Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relatio... J Med Chem. 2010 Apr 22;53(8):3417-21.
REF 20 Design, synthesis, and subtype selectivity of 3,6-disubstituted -carbolines at Bz/GABA(A)ergic receptors. SAR and studies directed toward agents f... Bioorg Med Chem. 2010 Nov 1;18(21):7548-64.
REF 21 Synthetic and computer-assisted analyses of the pharmacophore for the benzodiazepine receptor inverse agonist site. J Med Chem. 1990 Sep;33(9):2343-57.
REF 22 Synthesis and structure-activity relationships of a series of anxioselective pyrazolopyridine ester and amide anxiolytic agents. J Med Chem. 1989 Dec;32(12):2561-73.
REF 23 1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding. J Med Chem. 1987 Oct;30(10):1737-42.
REF 24 Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ... J Med Chem. 1988 Jan;31(1):1-3.
REF 25 Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore. J Med Chem. 1988 Sep;31(9):1854-61.
REF 26 Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem. 1988 Dec;31(12):2235-46.
REF 27 (Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics. J Med Chem. 1988 Jun;31(6):1220-6.
REF 28 Orally active and potent inhibitors of gamma-aminobutyric acid uptake. J Med Chem. 1985 May;28(5):653-60.
REF 29 Synthesis and interaction of 5-(substituted-phenyl)-3-methyl-6,7-dihydropyrazolo[4,3-e] [1,4]diazepin-8(7H)-ones with benzodiazepine receptors in r... J Med Chem. 1985 May;28(5):683-5.
REF 30 3-Amino-beta-carboline derivatives and the benzodiazepine receptor. Synthesis of a selective antagonist of the sedative action of diazepam. J Med Chem. 1985 Jun;28(6):824-8.
REF 31 Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands. J Med Chem. 1987 Mar;30(3):456-8.
REF 32 Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists. J Med Chem. 1987 Apr;30(4):750-3.
REF 33 gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83.
REF 34 Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.
REF 35 Four amino acid exchanges convert a diazepam-insensitive, inverse agonist-preferring GABAA receptor into a diazepam-preferring GABAA receptor. J Med Chem. 1994 Dec 23;37(26):4576-80.
REF 36 Potential anxiolytic agents. Pyrido[1,2-a]benzimidazoles: a new structural class of ligands for the benzodiazepine binding site on GABA-A receptors. J Med Chem. 1995 Jan 6;38(1):16-20.
REF 37 Synthetic routes to 4-amino-3-carboxy-beta-carboline derivatives: incidental formation of novel furo[3,4-c]-beta-carbolin-2-ones displaying high af... J Med Chem. 1995 Jan 6;38(1):189-98.
REF 38 Antagonist, partial agonist, and full agonist imidazo[1,5-a]quinoxaline amides and carbamates acting through the GABAA/benzodiazepine receptor. J Med Chem. 1994 Mar 18;37(6):758-68.
REF 39 Alpha-spirocyclopentyl- and alpha-spirocyclopropyl-gamma-butyrolactones: conformationally constrained derivatives of anticonvulsant and convulsant ... J Med Chem. 1994 Jan 21;37(2):275-86.
REF 40 Synthesis and evaluation of imidazo[1,5-a][1,4]benzodiazepine esters with high affinities and selectivities at "diazepam-insensitive" benzodiazepin... J Med Chem. 1993 Apr 16;36(8):1001-6.
REF 41 Synthesis and structure--activity relationships of fused imidazopyridines: a new series of benzodiazepine receptor ligands. J Med Chem. 1996 Jul 5;39(14):2844-51.
REF 42 Synthesis and binding activity of some pyrazolo[1,5-c]quinazolines as tools to verify an optional binding site of a benzodiazepine receptor ligand. J Med Chem. 1996 Jul 19;39(15):2915-21.
REF 43 Synthesis and evaluation of analogues of the partial agonist 6-(propyloxy)-4-(methoxymethyl)-beta-carboline-3-carboxylic acid ethyl ester (6-PBC) a... J Med Chem. 1998 Jul 2;41(14):2537-52.
REF 44 Predictive models for GABAA/benzodiazepine receptor subtypes: studies of quantitative structure-activity relationships for imidazobenzodiazepines a... J Med Chem. 1998 Oct 8;41(21):4130-42.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.