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Target
G protein-activated inward rectifier potassium channel 1/4
Ligand
BDBM585711
Substrate
n/a
Meas. Tech.
IonWorks Quattro system
IC50
33.0±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:
BDBM585711
Synonyms:
8-chloro-1-(2,6-dichloro-4- fluorophenyl)-5-(2-(2-(2-(2- hydroxyethoxy)ethoxy)ethoxy)eth- oxy)-2-methyl-1,6-naphthyridin- 4(1H)-one | US11530213, Example 32
Type:
Small organic molecule
Emp. Form.:
C23H24Cl3FN2O6
Mol. Mass.:
549.804
SMILES:
Cc1cc(=O)c2c(OCCOCCOCCOCCO)ncc(Cl)c2n1-c1c(Cl)cc(F)cc1Cl |(11.85,-4.94,;10.52,-4.17,;9.18,-4.94,;7.85,-4.17,;6.51,-4.94,;7.85,-2.63,;6.51,-1.86,;5.18,-2.63,;3.85,-1.86,;2.51,-2.63,;1.18,-1.86,;-.15,-2.63,;-1.49,-1.86,;-2.82,-2.63,;-4.15,-1.86,;-5.49,-2.63,;-6.82,-1.86,;-8.16,-2.63,;-9.49,-1.86,;-10.82,-2.63,;6.51,-.32,;7.85,.45,;9.18,-.32,;10.52,.45,;9.18,-1.86,;10.52,-2.63,;11.85,-1.86,;13.18,-2.63,;13.18,-4.17,;14.52,-1.86,;14.52,-.32,;15.85,.45,;13.18,.45,;11.85,-.32,;11.22,1.09,)|
Structure:
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