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TargetKir3.1/Kir3.4
LigandBDBM50437968
Substrate/Competitorn/a
Meas. Tech.ChEMBL_972874
EC50 3500±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/Kir3.4
Name:Kir3.1/Kir3.4
Synonyms:n/a
Type:n/a
Mol. Mass.:n/a
Description:ASSAY_ID of ChEMBL is 972874
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 4
Synonyms:CIR | Cardiac inward rectifier | GIRK-4 | GIRK4 | Heart KATP channel | IRK-4 | Inward rectifier K(+) channel Kir3.4 | KATP-1 | KCNJ5 | Potassium channel, inwardly rectifying subfamily J member 5
Type:PROTEIN
Mol. Mass.:47658.06
Organism:Homo sapiens (Human)
Description:ChEMBL_107914
Residue:419
Sequence:
MAGDSRNAMNQDMEIGVTPWDPKKIPKQARDYVPIATDRTRLLAEGKKPRQRYMEKSGKC
NVHHGNVQETYRYLSDLFTTLVDLKWRFNLLVFTMVYTVTWLFFGFIWWLIAYIRGDLDH
VGDQEWIPCVENLSGFVSAFLFSIETETTIGYGFRVITEKCPEGIILLLVQAILGSIVNA
FMVGCMFVKISQPKKRAETLMFSNNAVISMRDEKLCLMFRVGDLRNSHIVEASIRAKLIK
SRQTKEGEFIPLNQTDINVGFDTGDDRLFLVSPLIISHEINQKSPFWEMSQAQLHQEEFE
VVVILEGMVEATGMTCQARSSYMDTEVLWGHRFTPVLTLEKGFYEVDYNTFHDTYETNTP
SCCAKELAEMKREGRLLQYLPSPPLLGGCAEAGLDAEAEQNEEDEPKGLGGSREARGSV
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BDBM50437968
n/a
NameBDBM50437968
Synonyms:CHEMBL2409134
TypeSmall organic molecule
Emp. Form.C21H21F3N4O
Mol. Mass.402.4128
SMILESCC(C)c1cc(NC(=O)Nc2cccc(c2)C(F)(F)F)n(Cc2ccccc2)n1
Structure
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