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Target
G protein-activated inward rectifier potassium channel 1/4
Ligand
BDBM585716
Substrate
n/a
Meas. Tech.
IonWorks Quattro system
IC50
6.00±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:
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:
Human
Description:
ChEMBL_107914
Residue:
419
Sequence:
MAGDSRNAMNQDMEIGVTPWDPKKIPKQARDYVPIATDRTRLLAEGKKPRQRYMEKSGKCNVHHGNVQETYRYLSDLFTTLVDLKWRFNLLVFTMVYTVTWLFFGFIWWLIAYIRGDLDHVGDQEWIPCVENLSGFVSAFLFSIETETTIGYGFRVITEKCPEGIILLLVQAILGSIVNAFMVGCMFVKISQPKKRAETLMFSNNAVISMRDEKLCLMFRVGDLRNSHIVEASIRAKLIKSRQTKEGEFIPLNQTDINVGFDTGDDRLFLVSPLIISHEINQKSPFWEMSQAQLHQEEFEVVVILEGMVEATGMTCQARSSYMDTEVLWGHRFTPVLTLEKGFYEVDYNTFHDTYETNTPSCCAKELAEMKREGRLLQYLPSPPLLGGCAEAGLDAEAEQNEEDEPKGLGGSREARGSV
  
Inhibitor
Name:
BDBM585716
Synonyms:
8-chloro-1-(2,6-dichlorophenyl)-5- ((2-(2-(2-(2- hydroxyethoxy)ethoxy)ethoxy)eth- yl)amino)-2-methyl-1,6- naphthyridin-4(1H)-one | US11530213, Example 37
Type:
Small organic molecule
Emp. Form.:
C23H26Cl3N3O5
Mol. Mass.:
530.829
SMILES:
Cc1cc(=O)c2c(NCCOCCOCCOCCO)ncc(Cl)c2n1-c1c(Cl)cccc1Cl |(12.06,-4.58,;10.73,-3.81,;9.39,-4.58,;8.06,-3.81,;6.73,-4.58,;8.06,-2.27,;6.73,-1.5,;5.39,-2.27,;4.06,-1.5,;2.72,-2.27,;1.39,-1.5,;.06,-2.27,;-1.28,-1.5,;-2.61,-2.27,;-3.94,-1.5,;-5.28,-2.27,;-6.61,-1.5,;-7.94,-2.27,;-9.28,-1.5,;-10.61,-2.27,;6.73,.04,;8.06,.81,;9.39,.04,;10.73,.81,;9.39,-1.5,;10.73,-2.27,;12.06,-1.5,;13.39,-2.27,;13.39,-3.81,;14.73,-1.5,;14.73,.04,;13.39,.81,;12.06,.04,;11.43,1.45,)|
Structure:
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