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Target
G protein-activated inward rectifier potassium channel 1/4
Ligand
BDBM585714
Substrate
n/a
Meas. Tech.
IonWorks Quattro system
IC50
35.0±n/a nM
Citation
 Barbe, G; Bebernitz, GR; Geng, S; Gulgeze Efthymiou, HB; Liao, L; Ma, F; Mo, R; Parker, DT; Peng, Y; Peukert, S; Smith, N; Yamada, K; Yasoshima, 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:
BDBM585714
Synonyms:
5-((2-(1H-imidazol-4- yl)ethyl)amino)-8-chloro-1-(2,6- dichlorophenyl)-2-methyl-1,6- naphthyridin-4(1H)-one | US11530213, Example 35
Type:
Small organic molecule
Emp. Form.:
C20H16Cl3N5O
Mol. Mass.:
448.733
SMILES:
Cc1cc(=O)c2c(NCCc3c[nH]cn3)ncc(Cl)c2n1-c1c(Cl)cccc1Cl |(5.19,2.55,;3.85,1.78,;3.85,.24,;2.52,-.53,;2.52,-2.07,;1.18,.24,;-.15,-.53,;-.15,-2.07,;-1.48,-2.84,;-1.48,-4.38,;-2.82,-5.15,;-4.28,-4.68,;-5.19,-5.92,;-4.28,-7.17,;-2.82,-6.69,;-1.48,.24,;-1.48,1.78,;-.15,2.55,;-.15,4.09,;1.18,1.78,;2.52,2.55,;2.52,4.09,;1.18,4.86,;-.15,5.63,;1.18,6.4,;2.52,7.17,;3.85,6.4,;3.85,4.86,;5.19,4.09,)|
Structure:
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