Target
G protein-activated inward rectifier potassium channel 1/4
Ligand
BDBM585732
Substrate
n/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 
Target
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:
MSALRRKFGDDYQVVTTSSSGSGLQPQGPGQDPQQQLVPKKKRQRFVDKNGRCNVQHGNLGSETSRYLSDLFTTLVDLKWRWNLFIFILTYTVAWLFMASMWWVIAYTRGDLNKAHVGNYTPCVANVYNFPSAFLFFIETEATIGYGYRYITDKCPEGIILFLFQSILGSIVDAFLIGCMFIKMSQPKKRAETLMFSEHAVISMRDGKLTLMFRVGNLRNSHMVSAQIRCKLLKSRQTPEGEFLPLDQLELDVGFSTGADQLFLVSPLTICHVIDAKSPFYDLSQRSMQTEQFEIVVILEGIVETTGMTCQARTSYTEDEVLWGHRFFPVISLEEGFFKVDYSQFHATFEVPTPPYSVKEQEEMLLMSSPLIAPAITNSKERHNSVECLDGLDDITTKLPSKLQKITGREDFPKKLLRMSSTTSEKAYSLGDLPMKLQRISSVPGNSEEKLVSKTTKMLSDPMSQSVADLPPKLQKMAGGAARMEGNLPAKLRKMNSDRFT
  
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:
MAGDSRNAMNQDMEIGVTPWDPKKIPKQARDYVPIATDRTRLLAEGKKPRQRYMEKSGKCNVHHGNVQETYRYLSDLFTTLVDLKWRFNLLVFTMVYTVTWLFFGFIWWLIAYIRGDLDHVGDQEWIPCVENLSGFVSAFLFSIETETTIGYGFRVITEKCPEGIILLLVQAILGSIVNAFMVGCMFVKISQPKKRAETLMFSNNAVISMRDEKLCLMFRVGDLRNSHIVEASIRAKLIKSRQTKEGEFIPLNQTDINVGFDTGDDRLFLVSPLIISHEINQKSPFWEMSQAQLHQEEFEVVVILEGMVEATGMTCQARSSYMDTEVLWGHRFTPVLTLEKGFYEVDYNTFHDTYETNTPSCCAKELAEMKREGRLLQYLPSPPLLGGCAEAGLDAEAEQNEEDEPKGLGGSREARGSV
  
Inhibitor
Name:
BDBM585732
Synonyms:
8-chloro-1-(2,6-dichlorophenyl)-5- (3-hydroxy-2- (hydroxymethyl)propoxy)-2- (methoxymethyl)-1,6-naphthyridin- 4(1H)-one | US11530213, Example 53
Type:
Small organic molecule
Emp. Form.:
C20H19Cl3N2O5
Mol. Mass.:
473.734
SMILES:
COCc1cc(=O)c2c(OCC(CO)CO)ncc(Cl)c2n1-c1c(Cl)cccc1Cl |(4.67,-.77,;4.67,.77,;3.33,1.54,;2,.77,;2,-.77,;.67,-1.54,;.67,-3.08,;-.67,-.77,;-2,-1.54,;-2,-3.08,;-3.33,-3.85,;-3.33,-5.39,;-2,-6.16,;-.67,-5.39,;-4.67,-6.16,;-6,-5.39,;-3.33,-.77,;-3.33,.77,;-2,1.54,;-2,3.08,;-.67,.77,;.67,1.54,;.67,3.08,;-.67,3.85,;-2,4.62,;-.67,5.39,;.67,6.16,;2,5.39,;2,3.85,;3.33,3.08,)|
Structure:
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