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TargetG protein-activated inward rectifier potassium channel 1/4
LigandBDBM585741
Substrate/Competitorn/a
Meas. Tech.IonWorks Quattro system
IC50 13.0±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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BDBM585741
n/a
NameBDBM585741
Synonyms:US11530213, Example 62
TypeSmall organic molecule
Emp. Form.C18H13Cl3F2N2O4
Mol. Mass.465.663
SMILESOCC(O)COc1ncc(Cl)c2n(c(cc(=O)c12)C(F)F)-c1c(Cl)cccc1Cl |(-4.27,-7.27,;-4.67,-5.78,;-3.33,-5.01,;-2.25,-6.1,;-3.33,-3.47,;-2,-2.7,;-2,-1.16,;-3.33,-.39,;-3.33,1.15,;-2,1.92,;-2,3.46,;-.67,1.15,;.67,1.92,;2,1.15,;2,-.39,;.67,-1.16,;.67,-2.7,;-.67,-.39,;3.33,1.92,;4.67,1.15,;4.1,3.25,;.67,4.19,;-.67,4.96,;-2,4.19,;-.67,6.5,;.67,7.27,;2,6.5,;2,4.96,;3.33,4.19,)|
Structure
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