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Target
Gamma-aminobutyric acid receptor subunit alpha-3
Ligand
BDBM50120782
Substrate
n/a
Meas. Tech.
ChEMBL_68405 (CHEMBL678894)
EC50
23±n/a nM
Citation
 Albaugh, PA; Marshall, L; Gregory, J; White, G; Hutchison, A; Ross, PC; Gallagher, DW; Tallman, JF; Crago, M; Cassella, JV Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor. J Med Chem 45:5043-51 (2002) [PubMed]  Article 
Target
Name:
Gamma-aminobutyric acid receptor subunit alpha-3
Synonyms:
GABA A Alpha3Beta3Gamma2 | GABA A receptor alpha-3/beta-2/gamma-2 | GABA C | GABA receptor alpha-3 subunit | GABA-A receptor | GABRA3 | GBRA3_HUMAN | Gamma-aminobutyric acid receptor subunit alpha-3 | agonist GABA site
Type:
Enzyme Catalytic Domain
Mol. Mass.:
55175.47
Organism:
Homo sapiens (Human)
Description:
GABA A Alpha3Beta1Gamma2 0 HUMAN::P34903
Residue:
492
Sequence:
MIITQTSHCYMTSLGILFLINILPGTTGQGESRRQEPGDFVKQDIGGLSPKHAPDIPDDSTDNITIFTRILDRLLDGYDNRLRPGLGDAVTEVKTDIYVTSFGPVSDTDMEYTIDVFFRQTWHDERLKFDGPMKILPLNNLLASKIWTPDTFFHNGKKSVAHNMTTPNKLLRLVDNGTLLYTMRLTIHAECPMHLEDFPMDVHACPLKFGSYAYTTAEVVYSWTLGKNKSVEVAQDGSRLNQYDLLGHVVGTEIIRSSTGEYVVMTTHFHLKRKIGYFVIQTYLPCIMTVILSQVSFWLNRESVPARTVFGVTTVLTMTTLSISARNSLPKVAYATAMDWFIAVCYAFVFSALIEFATVNYFTKRSWAWEGKKVPEALEMKKKTPAAPAKKTSTTFNIVGTTYPINLAKDTEFSTISKGAAPSASSTPTIIASPKATYVQDSPTETKTYNSVSKVDKISRIIFPVLFAIFNLVYWATYVNRESAIKGMIRKQ
  
Inhibitor
Name:
BDBM50120782
Synonyms:
2-(2-Fluoro-phenyl)-8-pyridin-3-ylmethyl-6,7,8,9-tetrahydro-5H-1,3a,5,8-tetraaza-cyclopenta[a]naphthalen-4-one | CHEMBL146086
Type:
Small organic molecule
Emp. Form.:
C21H18FN5O
Mol. Mass.:
375.3989
SMILES:
Fc1ccccc1-c1cn2c(n1)c1CN(Cc3cccnc3)CCc1[nH]c2=O
Structure:
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