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Target
G protein-activated inward rectifier potassium channel 1
Ligand
BDBM50437956
Substrate
n/a
Meas. Tech.
ChEMBL_972869 (CHEMBL2411646)
IC50
3900±n/a nM
Citation
 Wen, W; Wu, W; Romaine, IM; Kaufmann, K; Du, Y; Sulikowski, GA; Weaver, CD; Lindsley, CW Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg Med Chem Lett 23:4562-6 (2013) [PubMed]  Article 
Target
Name:
G protein-activated inward rectifier potassium channel 1
Synonyms:
GIRK-1 | GIRK1 | Inward rectifier K(+) channel Kir3.1 | KCNJ3 | KCNJ3_HUMAN | Potassium channel, inwardly rectifying subfamily J member 3
Type:
PROTEIN
Mol. Mass.:
56610.74
Organism:
Homo sapiens (Human)
Description:
ChEMBL_107915
Residue:
501
Sequence:
MSALRRKFGDDYQVVTTSSSGSGLQPQGPGQDPQQQLVPKKKRQRFVDKNGRCNVQHGNLGSETSRYLSDLFTTLVDLKWRWNLFIFILTYTVAWLFMASMWWVIAYTRGDLNKAHVGNYTPCVANVYNFPSAFLFFIETEATIGYGYRYITDKCPEGIILFLFQSILGSIVDAFLIGCMFIKMSQPKKRAETLMFSEHAVISMRDGKLTLMFRVGNLRNSHMVSAQIRCKLLKSRQTPEGEFLPLDQLELDVGFSTGADQLFLVSPLTICHVIDAKSPFYDLSQRSMQTEQFEIVVILEGIVETTGMTCQARTSYTEDEVLWGHRFFPVISLEEGFFKVDYSQFHATFEVPTPPYSVKEQEEMLLMSSPLIAPAITNSKERHNSVECLDGLDDITTKLPSKLQKITGREDFPKKLLRMSSTTSEKAYSLGDLPMKLQRISSVPGNSEEKLVSKTTKMLSDPMSQSVADLPPKLQKMAGGAARMEGNLPAKLRKMNSDRFT
  
Inhibitor
Name:
BDBM50437956
Synonyms:
CHEMBL2409126
Type:
Small organic molecule
Emp. Form.:
C20H22N4O
Mol. Mass.:
334.4149
SMILES:
CC(C)c1cc(NC(=O)Nc2ccc(C)cc2)n(n1)-c1ccccc1
Structure:
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