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TargetKir3.1/Kir3.2
LigandBDBM50437952
Substrate/Competitorn/a
Meas. Tech.ChEMBL_972869
IC50 650±n/a nM
Citation Wen WWu WRomaine IMKaufmann KDu YSulikowski GAWeaver CDLindsley 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
More Info.:Get all data from this article,  Assay Method
 
Kir3.1/Kir3.2
Name:Kir3.1/Kir3.2
Synonyms:n/a
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 | Potassium channel, inwardly rectifying subfamily J member 3
Type:PROTEIN
Mol. Mass.:56610.74
Organism:Homo sapiens (Human)
Description:ChEMBL_107915
Residue:501
Sequence:
MSALRRKFGDDYQVVTTSSSGSGLQPQGPGQDPQQQLVPKKKRQRFVDKNGRCNVQHGNL
GSETSRYLSDLFTTLVDLKWRWNLFIFILTYTVAWLFMASMWWVIAYTRGDLNKAHVGNY
TPCVANVYNFPSAFLFFIETEATIGYGYRYITDKCPEGIILFLFQSILGSIVDAFLIGCM
FIKMSQPKKRAETLMFSEHAVISMRDGKLTLMFRVGNLRNSHMVSAQIRCKLLKSRQTPE
GEFLPLDQLELDVGFSTGADQLFLVSPLTICHVIDAKSPFYDLSQRSMQTEQFEIVVILE
GIVETTGMTCQARTSYTEDEVLWGHRFFPVISLEEGFFKVDYSQFHATFEVPTPPYSVKE
QEEMLLMSSPLIAPAITNSKERHNSVECLDGLDDITTKLPSKLQKITGREDFPKKLLRMS
STTSEKAYSLGDLPMKLQRISSVPGNSEEKLVSKTTKMLSDPMSQSVADLPPKLQKMAGG
AARMEGNLPAKLRKMNSDRFT
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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 | 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:
MAKLTESMTNVLEGDSMDQDVESPVAIHQPKLPKQARDDLPRHISRDRTKRKIQRYVRKD
GKCNVHHGNVRETYRYLTDIFTTLVDLKWRFNLLIFVMVYTVTWLFFGMIWWLIAYIRGD
MDHIEDPSWTPCVTNLNGFVSAFLFSIETETTIGYGYRVITDKCPEGIILLLIQSVLGSI
VNAFMVGCMFVKISQPKKRAETLVFSTHAVISMRDGKLCLMFRVGDLRNSHIVEASIRAK
LIKSKQTSEGEFIPLNQTDINVGYYTGDDRLFLVSPLIISHEINQQSPFWEISKAQLPKE
ELEIVVILEGMVEATGMTCQARSSYITSEILWGYRFTPVLTLEDGFYEVDYNSFHETYET
STPSLSAKELAELASRAELPLSWSVSSKLNQHAELETEEEEKNLEEQTERNGDVANLENE
SKV
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BDBM50437952
n/a
NameBDBM50437952
Synonyms:CHEMBL2409118
TypeSmall organic molecule
Emp. Form.C20H18F2N4O
Mol. Mass.368.3799
SMILESFc1ccc(NC(=O)Nc2cc(CC3CC3)nn2-c2ccccc2)cc1F
Structure
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