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TargetG protein-activated inward rectifier potassium channel 1/4
LigandBDBM585736
Substrate/Competitorn/a
Meas. Tech.IonWorks Quattro system
IC50 32.0±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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BDBM585736
n/a
NameBDBM585736
Synonyms:8-chloro-1-(2,6-dichlorophenyl)-5- ((2,2-dimethyl-1,3-dioxolan-4- yl)methoxy)-2-(hydroxymethyl)- 1,6-naphthyridin-4(1H)-one | US11530213, Example 57
TypeSmall organic molecule
Emp. Form.C21H19Cl3N2O5
Mol. Mass.485.745
SMILESCC1(C)OCC(COc2ncc(Cl)c3n(c(CO)cc(=O)c23)-c2c(Cl)cccc2Cl)O1 |(-2.21,-8.21,;-2.61,-6.72,;-1.12,-7.12,;-4.15,-6.72,;-4.62,-5.26,;-3.38,-4.35,;-3.38,-2.81,;-2.04,-2.04,;-2.04,-.5,;-3.38,.27,;-3.38,1.81,;-2.04,2.58,;-2.04,4.12,;-.71,1.81,;.62,2.58,;1.96,1.81,;3.29,2.58,;4.62,1.81,;1.96,.27,;.62,-.5,;.62,-2.04,;-.71,.27,;.62,5.13,;-.71,5.9,;-2.04,5.13,;-.71,7.44,;.62,8.21,;1.96,7.44,;1.96,5.9,;3.29,5.13,;-2.13,-5.26,)|
Structure
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