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Target
G protein-activated inward rectifier potassium channel 4
Ligand
BDBM585727
Substrate
n/a
Meas. Tech.
ChEMBL_2295208
IC50
9.0±n/a nM
Citation
 Peukert, S; Gulgeze Efthymiou, HB; Mo, R; Peng, Y; Ma, F; Barbe, G; Bebernitz, G; Fridrich, C; Buono, C; Williams, ET; Daniels, T; Li, L; Zhang, X; Adachi, Y; Abe, M; Taggart, AKP Discovery of a brain-sparing GIRK1/4 inhibitor for pharmacological cardioversion of atrial fibrillation. Bioorg Med Chem Lett 85:0 (2023) [PubMed]
Target
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:
BDBM585727
Synonyms:
8-chloro-1-(2,6-dichlorophenyl)-5- (2-hydroxyethoxy)-2-methyl-1,6- naphthyridin-4(1H)-one | US11530213, Example 48
Type:
Small organic molecule
Emp. Form.:
C17H13Cl3N2O3
Mol. Mass.:
399.656
SMILES:
Cc1cc(=O)c2c(OCCO)ncc(Cl)c2n1-c1c(Cl)cccc1Cl |(4,1.07,;2.67,.3,;2.67,-1.24,;1.33,-2.01,;1.33,-3.55,;,-1.24,;-1.33,-2.01,;-1.33,-3.55,;-2.67,-4.32,;-2.67,-5.86,;-4,-6.63,;-2.67,-1.24,;-2.67,.3,;-1.33,1.07,;-1.33,2.61,;,.3,;1.33,1.07,;1.33,3.55,;2.67,4.32,;4,3.55,;2.67,5.86,;1.33,6.63,;,5.86,;,4.32,;-1.33,3.55,)|
Structure:
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