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Target
G protein-activated inward rectifier potassium channel 1/2
Ligand
BDBM50437952
Substrate
n/a
Meas. Tech.
ChEMBL_972869 (CHEMBL2411646)
IC50
650±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 1/2
Synonyms:
Kir3.1/Kir3.2
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 972869
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
G protein-activated inward rectifier potassium channel 2
Synonyms:
BIR1 | GIRK-2 | GIRK2 | Inward rectifier K(+) channel Kir3.2 | KATP-2 | KATP2 | KCNJ6 | KCNJ6_HUMAN | KCNJ7 | Potassium channel, inwardly rectifying subfamily J member 6
Type:
PROTEIN
Mol. Mass.:
48440.73
Organism:
Homo sapiens (Human)
Description:
ChEMBL_107630
Residue:
423
Sequence:
MAKLTESMTNVLEGDSMDQDVESPVAIHQPKLPKQARDDLPRHISRDRTKRKIQRYVRKDGKCNVHHGNVRETYRYLTDIFTTLVDLKWRFNLLIFVMVYTVTWLFFGMIWWLIAYIRGDMDHIEDPSWTPCVTNLNGFVSAFLFSIETETTIGYGYRVITDKCPEGIILLLIQSVLGSIVNAFMVGCMFVKISQPKKRAETLVFSTHAVISMRDGKLCLMFRVGDLRNSHIVEASIRAKLIKSKQTSEGEFIPLNQTDINVGYYTGDDRLFLVSPLIISHEINQQSPFWEISKAQLPKEELEIVVILEGMVEATGMTCQARSSYITSEILWGYRFTPVLTLEDGFYEVDYNSFHETYETSTPSLSAKELAELASRAELPLSWSVSSKLNQHAELETEEEEKNLEEQTERNGDVANLENESKV
  
Inhibitor
Name:
BDBM50437952
Synonyms:
CHEMBL2409118
Type:
Small organic molecule
Emp. Form.:
C20H18F2N4O
Mol. Mass.:
368.3799
SMILES:
Fc1ccc(NC(=O)Nc2cc(CC3CC3)nn2-c2ccccc2)cc1F
Structure:
Search PDB for entries with ligand similarity: