Reaction Details Report a problem with these data
Target
Gamma-aminobutyric acid receptor subunit alpha-3
Ligand
BDBM50120773
Substrate
n/a
Meas. Tech.
ChEMBL_68405 (CHEMBL678894)
EC50
242±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:
BDBM50120773
Synonyms:
8-(2-Fluoro-benzoyl)-2-(2-fluoro-phenyl)-6,7,8,9-tetrahydro-5H-1,3a,5,8-tetraaza-cyclopenta[a]naphthalen-4-one | CHEMBL146302
Type:
Small organic molecule
Emp. Form.:
C22H16F2N4O2
Mol. Mass.:
406.3848
SMILES:
Fc1ccccc1C(=O)N1CCc2[nH]c(=O)n3cc(nc3c2C1)-c1ccccc1F
Structure:
Search PDB for entries with ligand similarity: