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TargetG protein-activated inward rectifier potassium channel 1/4
LigandBDBM585720
Substrate/Competitorn/a
Meas. Tech.IonWorks Quattro system
IC50 28.0±n/a nM
Citation Barbe, GBebernitz, GRGeng, SGulgeze Efthymiou, HBLiao, LMa, FMo, RParker, DTPeng, YPeukert, SSmith, NYamada, KYasoshima, K Naphthyridinone derivatives and their use in the treatment of arrhythmia US Patent US11530213 Publication Date 12/20/2022
More Info.:Get all data from this article,  Assay Method
 
G protein-activated inward rectifier potassium channel 1/4
Name:G protein-activated inward rectifier potassium channel 1/4
Synonyms:GIRK1/4 channels | Kir3.1/Kir3.4
Type:PROTEIN
Mol. Mass.:n/a
Description:n/a
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:
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 | KCNJ5_HUMAN | 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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BDBM585720
n/a
NameBDBM585720
Synonyms:8-chloro-1-(2,6-dichlorophenyl)-5- (3-hydroxy-2-(hydroxymethyl)-2- methylpropoxy)-2-methyl-1,6- naphthyridin-4(1H)-one | US11530213, Example 41
TypeSmall organic molecule
Emp. Form.C20H19Cl3N2O4
Mol. Mass.457.735
SMILESCc1cc(=O)c2c(OCC(C)(CO)CO)ncc(Cl)c2n1-c1c(Cl)cccc1Cl |(4.67,2.31,;3.33,1.54,;3.33,,;2,-.77,;2,-2.31,;.67,,;-.67,-.77,;-.67,-2.31,;-2,-3.08,;-2,-4.62,;-.67,-3.85,;-.67,-5.39,;-.67,-6.93,;-3.33,-5.39,;-4.67,-4.62,;-2,,;-2,1.54,;-.67,2.31,;-.67,3.85,;.67,1.54,;2,2.31,;2,3.85,;.67,4.62,;-.67,5.39,;.67,6.16,;2,6.93,;3.33,6.16,;3.33,4.62,;4.67,3.85,)|
Structure
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