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Target
G protein-activated inward rectifier potassium channel 1/4
Ligand
BDBM585710
Substrate
n/a
Meas. Tech.
IonWorks Quattro system
IC50
100.0±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:
BDBM585710
Synonyms:
8-chloro-1-(2,6-dichlorophenyl)-5- ((2R,4S)-4-hydroxy-2- (hydroxymethyl)pyrrolidin-1-yl)-2- methyl-1,6-naphthyridin-4(1H)-one | US11530213, Example 31
Type:
Small organic molecule
Emp. Form.:
C20H18Cl3N3O3
Mol. Mass.:
454.734
SMILES:
Cc1cc(=O)c2c(cnc(Cl)c2n1-c1c(Cl)cccc1Cl)N1C[C@@H](O)C[C@@H]1CO |r,wU:23.26,wD:26.30,(4.62,1.32,;3.29,.55,;3.29,-.99,;1.96,-1.76,;1.96,-3.3,;.62,-.99,;-.71,-1.76,;-2.04,-.99,;-2.04,.55,;-.71,1.32,;-.71,2.86,;.62,.55,;1.96,1.32,;1.96,3.92,;.62,4.69,;-.71,3.92,;.62,6.23,;1.96,7,;3.29,6.23,;3.29,4.69,;4.62,3.92,;-.71,-3.3,;.54,-4.2,;.06,-5.67,;.83,-7,;-1.48,-5.67,;-1.96,-4.2,;-3.29,-3.43,;-4.62,-4.2,)|
Structure:
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