Target Validation Information
TTD ID T64382
Target Name Gamma-aminobutyric acid receptor (GAR)
Type of Target
Successful
Drug Potency against Target Clonazepam Drug Info IC50 = 5 nM [64]
Phenobarbital Drug Info IC50 = 100000 nM [63]
Piperazine Drug Info EC50 = 22 nM [65]
Dextofisopam Drug Info IC50 < 100 nM [67]
BL-1020 Drug Info Ki = 3740 nM [66]
Drug Info IC50 = 300 nM
((E)-3-Amino-propenyl)-methyl-phosphinic acid Drug Info IC50 = 5500 nM [24]
(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 [43]
(4R)-4-ammoniopentanoate Drug Info IC50 = 2500 nM [43]
(4S)-4-ammoniopentanoate Drug Info IC50 = 2900 nM [43]
(6-Benzylamino-9H-beta-carbolin-3-yl)-methanol Drug Info IC50 = 76 nM [42]
(9H-beta-Carbolin-3-yl)-carbamic acid ethyl ester Drug Info IC50 = 80 nM [39]
(9H-beta-Carbolin-3-yl)-ethyl-amine Drug Info IC50 = 460 nM [39]
(9H-beta-Carbolin-3-yl)-methanol Drug Info IC50 = 1470 nM [42]
(beta-CCE)9H-beta-Carboline-3-carboxylic acid Drug Info Ki = 1.2 nM [8]
(R)-4-amino-2-methylbutanoic acid Drug Info IC50 = 16000 nM [22]
1,1-Dimethyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 1140 nM [52]
1,3-Diphenyl-1H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 16000 nM [33]
1-(4-chlorophenyl)-4-phenyl-1H-imidazole Drug Info Ki = 3290 nM [15]
1-(9H-beta-Carbolin-3-yl)-butan-1-one Drug Info IC50 = 2.8 nM [9]
1-(9H-beta-Carbolin-3-yl)-ethanone Drug Info IC50 = 58 nM [42]
1-Methyl-5-oxa-spiro[2.4]heptan-4-one Drug Info IC50 = 3410 nM [52]
2,4-Diamino-butyric acid(GABA) Drug Info IC50 = 33 nM [40]
2,6-Diisopropyl-4-nitro-phenol Drug Info IC50 = 1950 nM [59]
2-(1H-Indol-3-yl)-2-oxo-N-phenethyl-acetamide Drug Info Ki = 380 nM [8]
2-(2-Amino-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 700 nM [5]
2-(2-Hydroxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 6.2 nM [5]
2-(2-Methoxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 820 nM [5]
2-(3-Amino-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 1200 nM [5]
2-(3-Bromo-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 12 nM [5]
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-Butoxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 710 nM [5]
2-(3-Chloro-phenyl)-chromen-4-one Drug Info Ki = 614 nM
2-(3-Hydroxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 390 nM [5]
2-(3-Methoxy-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 99 nM [5]
2-(4-Amino-phenyl)-6-methyl-chromen-4-one Drug Info Ki = 2600 nM [5]
2-(4-Chloro-phenyl)-3H-imidazo[4,5-c]quinoline Drug Info Ki = 270 nM [55]
2-(4-chlorophenyl)-5-phenyl-4-isoxazolin-3-one Drug Info Ki = 1120 nM [15]
2-Furan-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 16 nM [56]
2-Isoxazol-3-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 0.6 nM [55]
2-Isoxazol-5-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1 nM [55]
2-Oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 810 nM [52]
2-p-Tolyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 9500 nM [56]
2-Phenyl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 22 nM [55]
2-Phenyl-5,6-dihydro-pyrazolo[1,5-c]quinazoline Drug Info Ki = 6573 nM [56]
2-Phenyl-6-propyl-chromen-4-one Drug Info Ki = 480 nM [5]
2-Phenyl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 59 nM [56]
2-Pyridin-2-yl-6H-pyrazolo[1,5-c]quinazolin-5-one Drug Info Ki = 53 nM [56]
2-Thiophen-2-yl-3H-imidazo[4,5-c]quinoline Drug Info Ki = 1.7 nM [55]
3,3-Diethyl-dihydro-furan-2-one Drug Info IC50 = 750 nM [52]
3,3-Diisopropyl-dihydro-furan-2-one Drug Info IC50 = 220 nM [52]
3,3-Dimethyl-dihydro-furan-2-one Drug Info IC50 = 9200 nM [52]
3-(2,2-Dimethyl-propoxy)-9H-beta-carboline Drug Info IC50 = 104 nM [9]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info Ki = 10000 nM [28]
3-(3-Methyl-butoxy)-9H-beta-carboline Drug Info IC50 = 535 nM [9]
3-(benzyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [28]
3-(hexa-1,3-dienyloxy)-9H-pyrido[3,4-b]indole Drug Info Ki = 10000 nM [28]
3-amino-3-demethoxythiocolchicine Drug Info IC50 = 5400 nM [19]
3-ammoniopropane-1-sulfinate Drug Info IC50 = 470 nM
3-Butoxy-9H-beta-carboline Drug Info Ki = 1000 nM [28]
3-Butoxy-9H-beta-carboline Drug Info IC50 = 98 nM [9]
3-butoxycarbonyl-4-quinolone Drug Info Ki = 54 nM [16]
3-butoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 13 nM [16]
3-butylaminocarbonyl-6-ethyl-4-quinolone Drug Info Ki = 0.54 nM [16]
3-carboxy-6-ethyl-4-quinolone Drug Info Ki = 208 nM [16]
3-Chloro-9H-beta-carboline Drug Info IC50 = 45 nM [34]
3-cyclopentoxycarbonyl-6-ethyl-4-quinolone Drug Info Ki = 19 nM [16]
3-demethoxy-3-D-lyxopyranosylaminothiocolchicine Drug Info IC50 = 9700 nM [19]
3-demethoxy-3-D-mannopyranosylaminothiocolchicine Drug Info IC50 = 11300 nM [19]
3-demethoxy-3-D-xylopyranosylaminothiocolchicine Drug Info IC50 = 7000 nM [19]
3-demethoxy-3-L-fucopyranosylaminothiocolchicine Drug Info IC50 = 10500 nM [19]
3-demethoxy-3D-glucopyranosylaminothiocolchicine Drug Info IC50 = 18000 nM [19]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 1000 nM [28]
3-Ethoxy-9H-beta-carboline Drug Info Ki = 25.1 nM [60]
3-ethoxycarbonyl-4-quinolone Drug Info Ki = 78 nM [16]
3-ethoxycarbonyl-6-ethyl-2-methyl-4-quinolone Drug Info Ki = 6580 nM [16]
3-ethoxycarbonyl-6-propyl-4-quinolone Drug Info Ki = 17 nM [16]
3-Ethyl-3-isopropyl-dihydro-furan-2-one Drug Info IC50 = 240 nM [52]
3-Ethyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 2280 nM [52]
3-Hydroxy-piperidine-4-carboxylic acid Drug Info IC50 = 12000 nM [44]
3-Isobutoxy-9H-beta-carboline Drug Info Ki = 10000 nM [28]
3-Isobutoxy-9H-beta-carboline Drug Info IC50 = 93 nM [9]
3-Isopropoxy-9H-beta-carboline Drug Info IC50 = 500 nM [9]
3-Isopropyl-3-methyl-dihydro-furan-2-one Drug Info IC50 = 740 nM [52]
3-Isothiocyanato-9H-beta-carboline Drug Info IC50 = 4 nM [29]
3-Methoxy-9H-beta-carboline Drug Info IC50 = 124 nM [34]
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 [33]
3-Methyl-2-phenyl-2H-chromeno[4,3-c]pyrazol-4-one Drug Info IC50 = 3100 nM [33]
3-Methyl-9H-beta-carboline Drug Info Ki = 1.1 nM [48]
3-Nitro-9H-beta-carboline Drug Info IC50 = 125 nM [34]
3-Propoxy-9H-beta-carboline Drug Info Ki = 1000 nM [28]
3-Propoxy-9H-beta-carboline Drug Info IC50 = 11 nM [34]
3-sec-Butoxy-9H-beta-carboline Drug Info IC50 = 471 nM [9]
3-tert-Butyl-3-ethyl-dihydro-furan-2-one Drug Info IC50 = 310 nM [52]
4-(2-aminoethyl)-1,2,5-oxadiazol-3-ol Drug Info Ki = 13000 nM [17]
4-(4-chlorophenyl)-1-pyrid-2-yl-pyrazole Drug Info Ki = 4480 nM [15]
4-(5-tert-Butyl-[1,3]dithian-2-yl)-benzonitrile Drug Info Ki = 240 nM [45]
4-benzyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 465 nM [14]
4-Benzyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 3800 nM [12]
4-Bromo-2,6-diisopropyl-phenol Drug Info IC50 = 1070 nM [59]
4-Chloro-2,6-diisopropyl-phenol Drug Info IC50 = 1440 nM [59]
4-Dimethylamino-2,6-diisopropyl-phenol Drug Info IC50 = 5700 nM [59]
4-Ethyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info IC50 = 10300 nM [2]
4-Hydroxy-3,5-diisopropyl-benzaldehyde Drug Info IC50 = 5800 nM [59]
4-Iodo-2,6-diisopropyl-phenol Drug Info IC50 = 1200 nM [59]
4-Methoxymethyl-3,6-dipropoxy-9H-beta-carboline Drug Info IC50 = 43.2 nM [60]
4-Methyl-5-(4-piperidyl)isothiazol-3-ol Drug Info Ki = 2880 nM [14]
4-Methyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 10000 nM [2]
4-Naphthalen-1-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 820 nM [12]
4-Naphthalen-2-yl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 36 nM [12]
4-Phenyl-5-piperidin-4-yl-isoxazol-3-ol Drug Info Ki = 159 nM [21]
5-(4-piperidyl)-4-propylisothiazol-3-ol Drug Info Ki = 230 nM [14]
5-(piperidin-4-yl)isothiazol-3-ol Drug Info Ki = 1870 nM [14]
5-(piperidin-4-yl)isoxazol-3-ol Drug Info Ki = 11000 nM [21]
5-tert-Butyl-2-(4-ethynyl-phenyl)-[1,3]dithiane Drug Info Ki = 85 nM [45]
5-tert-Butyl-2-(4-fluoro-phenyl)-[1,3]dithiane Drug Info Ki = 1100 nM [45]
5-[(1R)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 9500 nM [43]
5-[(1S)-1-ammonioethyl]isoxazol-3-olate Drug Info IC50 = 5800 nM [43]
6,6-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 360 nM [52]
6,9-Dimethyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 780 nM [52]
6-benzyl-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 1.4 nM [16]
6-benzyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 0.17 nM [16]
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 [16]
6-bromo-3-ethoxycarbonyl-4-quinolone Drug Info Ki = 16 nM [16]
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-2-phenyl-chromen-4-one Drug Info Ki = 180 nM [5]
6-ethyl-3-(2-ethylbutoxycarbonyl)-4-quinolone Drug Info Ki = 92 nM [16]
6-ethyl-3-(2-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [16]
6-ethyl-3-(3-methylbutoxycarbonyl)-4-quinolone Drug Info Ki = 28 nM [16]
6-ethyl-3-(3-pentoxycarbonyl)-4-quinolone Drug Info Ki = 2600 nM [16]
6-ethyl-3-i-propoxycarbonyl-4-quinolone Drug Info Ki = 214 nM [16]
6-ethyl-3-pentoxycarbonyl-4-quinolone Drug Info Ki = 35 nM [16]
6-ethyl-3-propoxycarbonyl-4-quinolone Drug Info Ki = 1.8 nM [16]
6-ethyl-3-propylaminocarbonyl-4-quinolone Drug Info Ki = 0.26 nM [16]
6-Fluoro-2-(3-nitro-phenyl)-chromen-4-one Drug Info Ki = 180 nM
6-Isopropyl-2-phenyl-chromen-4-one Drug Info Ki = 720 nM [5]
6-Methyl-2-oxa-spiro[4.4]nonan-1-one Drug Info IC50 = 680 nM [52]
6-Methyl-2-p-tolyl-chromen-4-one Drug Info Ki = 4400 nM [5]
6-Methyl-2-phenyl-chromen-4-one Drug Info Ki = 180 nM [5]
6-Methyl-2-pyridin-3-yl-chromen-4-one Drug Info Ki = 130 nM [5]
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 [41]
7,12-Dihydro-7,12-diaza-indeno[1,2-a]fluorene Drug Info IC50 = 1920 nM [34]
7-Diazonium-naphthalene-1-sulfonic acid anion Drug Info IC50 < 10000 nM [32]
8-Diazonium-naphthalene-1-sulfonic acid anion Drug Info IC50 = 10000 nM [32]
9H-beta-Carbolin-3-ol Drug Info IC50 = 4000 nM [34]
9H-beta-Carbolin-6-ylamine Drug Info IC50 = 1300 nM [42]
9H-beta-Carboline-3-carboxylic acid ethyl ester Drug Info Ki = 2700 nM [28]
Acetic acid 2,6-diisopropyl-phenyl ester Drug Info IC50 = 8500 nM [59]
AFLATREME Drug Info IC50 = 4300 nM
ALFAXALONE Drug Info IC50 = 300 nM [59]
Allopregnanolone Drug Info IC50 = 74 nM [18]
Alpidem Drug Info IC50 = 26 nM [58]
AMENTOFLAVONE Drug Info IC50 = 14.9 nM [6]
ANDROSTERONE Drug Info IC50 = 410 nM [18]
Benzoic acid 2,6-diisopropyl-phenyl ester Drug Info IC50 = 15200 nM [59]
Benzyl-(9H-beta-carbolin-6-yl)-amine Drug Info IC50 = 106 nM [34]
Beta-Carboline-3-carboxylic acid t-butyl ester Drug Info Ki = 1000 nM [28]
BETA-CCM Drug Info IC50 = 2 nM [50]
BRL-54504AX Drug Info IC50 = 950 nM
CGS-13767 Drug Info IC50 = 4 nM [23]
CGS-17867A Drug Info Ki = 0.77 nM [11]
CGS-9895 Drug Info IC50 = 100 nM [31]
CGS-9896 Drug Info Ki = 2.4 nM [15]
CI-218872 Drug Info Ki = 561 nM [28]
Divaplon Drug Info IC50 = 56 nM [36]
ELTANOLONE Drug Info IC50 = 71 nM [18]
Ethyl 6-iodo-9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 1000 nM [28]
ETIOCHOLANOLONE Drug Info IC50 = 4140 nM [18]
flavone Drug Info Ki = 4200 nM [5]
GNF-PF-3645 Drug Info Ki = 15 nM [16]
GNF-PF-4421 Drug Info Ki = 20 nM [16]
GSK683699 Drug Info IC50 = 24 nM [19]
isonipecotic acid Drug Info IC50 = 330 nM [44]
Isoquinoline-3-carboxylic acid methyl ester Drug Info IC50 = 13200 nM [34]
L-655708 Drug Info Ki = 0.4 nM [10]
MRK016 Drug Info Ki = 0.2 nM [13]
N-(9H-beta-Carbolin-3-yl)-acetamide Drug Info IC50 = 4000 nM [39]
N-(9H-beta-Carbolin-3-yl)-formamide Drug Info IC50 = 4700 nM [39]
N-Benzyl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 120 nM [61]
N-butyl-2-(5-nitro-1H-indol-3-yl)-2-oxoacetamide Drug Info Ki = 943 nM [20]
N-Indan-1-yl-2-(1H-indol-3-yl)-2-oxo-acetamide Drug Info Ki = 2160 nM [4]
NORHARMANE Drug Info IC50 = 1620 nM [34]
NSC-73613 Drug Info Ki = 285 nM
NSC-93394 Drug Info Ki = 4500 nM
Pitrazepine Drug Info IC50 = 240 nM [7]
Pyrrolidin-3-yl-acetic acid Drug Info IC50 = 330 nM [37]
Ridine-5-carboxylic acid ethyl ester Drug Info IC50 = 79 nM [30]
RIPAZEPAM Drug Info IC50 = 670 nM [38]
RO-054520 Drug Info IC50 = 24 nM [35]
RO-145974 Drug Info Ki = 45 nM [53]
RO-145975 Drug Info Ki = 53 nM [53]
RO-147437 Drug Info Ki = 1.3 nM [53]
Ro-15-3505 Drug Info Ki = 0.85 nM [27]
Ro-15-3505 Drug Info Ki = 20 nM [47]
Ro-16-6028 Drug Info IC50 = 6.1 nM [57]
RO-194603 Drug Info Ki = 0.2 nM [53]
Ro-4938581 Drug Info Ki = 14 nM [26]
Ro-4938581 Drug Info Ki = 80 nM [26]
RWJ-16979 Drug Info IC50 = 5.9 nM [49]
RY-066 Drug Info Ki = 48 nM [62]
Sec-butyl 9H-pyrido[3,4-b]indole-3-carboxylate Drug Info Ki = 216 nM [28]
THIOCOLCHICOSIDE Drug Info IC50 = 3400 nM [19]
Toluene-1-diazonium-3-sulfonic acid anion Drug Info IC50 = 5000 nM [32]
U-78875 Drug Info Ki = 1.6 nM [1]
U-89267 Drug Info Ki = 0.65 nM [51]
WEDELOLACTONE Drug Info IC50 = 2000 nM [3]
ZK-93423 Drug Info IC50 = 1 nM [25]
[3H]CGP27492 Drug Info IC50 = 1700 nM [46]
[3H]Ro154513 Drug Info Ki = 3.8 nM [54]
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 A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology. J Med Chem. 2000 Dec 28;43(26):4930-3.
REF 3 Synthesis and preliminary pharmacological evaluation of coumestans with different patterns of oxygenation. Bioorg Med Chem Lett. 2001 Feb 12;11(3):283-6.
REF 4 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 5 Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor. J Med Chem. 2002 Sep 12;45(19):4188-201.
REF 6 Semisynthetic preparation of amentoflavone: A negative modulator at GABA(A) receptors. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2281-4.
REF 7 Structure and molecular modeling of GABAA receptor antagonists. J Med Chem. 1992 May 29;35(11):1969-77.
REF 8 Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives. J Med Chem. 1992 Jun 12;35(12):2214-20.
REF 9 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 10 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 11 2,5-Dihydropyrazolo[4,3-c]pyridin-3-ones: functionally selective benzodiazepine binding site ligands on the GABAA receptor. Bioorg Med Chem Lett. 2004 Jul 5;14(13):3441-4.
REF 12 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 13 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 14 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 15 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 16 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 17 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 18 Neurosteroid analogues. 11. Alternative ring system scaffolds: gamma-aminobutyric acid receptor modulation and anesthetic actions of benz[f]indenes. J Med Chem. 2006 Jul 27;49(15):4595-605.
REF 19 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 20 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 21 4-aryl-5-(4-piperidyl)-3-isoxazolol GABAA antagonists: synthesis, pharmacology, and structure-activity relationships. J Med Chem. 2007 Apr 19;50(8):1988-92.
REF 22 Enantioselective actions of 4-amino-3-hydroxybutanoic acid and (3-amino-2-hydroxypropyl)methylphosphinic acid at recombinant GABA(C) receptors. Bioorg Med Chem Lett. 2008 Jan 1;18(1):402-4.
REF 23 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 24 Novel gamma-aminobutyric acid rho1 receptor antagonists; synthesis, pharmacological activity and structure-activity relationships. J Med Chem. 2008 Jul 10;51(13):3825-40.
REF 25 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 26 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 27 The GABA(A) receptor as a target for photochromic molecules. Bioorg Med Chem. 2010 Nov 15;18(22):7731-8.
REF 28 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 29 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 30 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 31 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 32 Aryl diazo compounds and diazonium salts as potential irreversible probes of the gamma-aminobutyric acid receptor. J Med Chem. 1987 Dec;30(12):2222-7.
REF 33 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 34 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 35 Methods for drug discovery: development of potent, selective, orally effective cholecystokinin antagonists. J Med Chem. 1988 Dec;31(12):2235-46.
REF 36 (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 37 Orally active and potent inhibitors of gamma-aminobutyric acid uptake. J Med Chem. 1985 May;28(5):653-60.
REF 38 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 39 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 40 Glycine antagonists. Synthesis, structure, and biological effects of some bicyclic 5-isoxazolol zwitterions. J Med Chem. 1986 Feb;29(2):224-9.
REF 41 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 42 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 43 gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects. J Med Chem. 1981 Dec;24(12):1377-83.
REF 44 Hydroxy- and amino-substituted piperidinecarboxylic acids as gamma-aminobutyric acid agonists and uptake inhibitors. J Med Chem. 1982 Oct;25(10):1157-62.
REF 45 Synthesis of carbon-11-, fluorine-18-, and iodine-125-labeled GABAA-gated chloride ion channel blockers: substituted 5-tert-butyl-2-phenyl-1,3-dith... J Med Chem. 1995 Jul 7;38(14):2663-71.
REF 46 Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists. J Med Chem. 1995 Aug 18;38(17):3297-312.
REF 47 Synthesis of novel imidazobenzodiazepines as probes of the pharmacophore for "diazepam-insensitive" GABAA receptors. J Med Chem. 1995 May 12;38(10):1679-88.
REF 48 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 49 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 50 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 51 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 52 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 53 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 54 Synthesis and pharmacological properties of novel 8-substituted imidazobenzodiazepines: high-affinity, selective probes for alpha 5-containing GABA... J Med Chem. 1996 Apr 26;39(9):1928-34.
REF 55 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 56 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 57 Synthesis and in vitro activity of 3 beta-substituted-3 alpha-hydroxypregnan-20-ones: allosteric modulators of the GABAA receptor. J Med Chem. 1997 Jan 3;40(1):61-72.
REF 58 Synthesis and binding affinity of 2-phenylimidazo[1,2-alpha]pyridine derivatives for both central and peripheral benzodiazepine receptors. A new se... J Med Chem. 1997 Sep 12;40(19):3109-18.
REF 59 Propofol analogues. Synthesis, relationships between structure and affinity at GABAA receptor in rat brain, and differential electrophysiological p... J Med Chem. 1998 May 21;41(11):1846-54.
REF 60 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 61 N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological acti... J Med Chem. 1998 Sep 24;41(20):3821-30.
REF 62 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.
REF 63 Effects of anticonvulsants on veratridine- and KCl-evoked glutamate release from rat cortical synaptosomes. Neurosci Lett. 1999 Dec 3;276(2):127-30.
REF 64 Subunit composition and pharmacological characterization of gamma-aminobutyric acid type A receptors in frog pituitary melanotrophs. Endocrinology. 2000 Mar;141(3):1083-92.
REF 65 Serotonergic 5-HT2C receptors as a potential therapeutic target for the design antiepileptic drugs. Curr Top Med Chem. 2005;5(1):59-67.
REF 66 BL-1020: a novel antipsychotic drug with GABAergic activity and low catalepsy, is efficacious in a rat model of schizophrenia. Eur Neuropsychopharmacol. 2009 Jan;19(1):1-13.
REF 67 Tofizopam affects binding of [3H]muscimol to gamma-amino-butyric acid receptors in rat and mouse brains. Pharmacol Res Commun. 1982 Sep;14(8):745-57.

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