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Target
G protein-activated inward rectifier potassium channel 4
Ligand
BDBM50613997
Substrate
n/a
Meas. Tech.
ChEMBL_2295208
IC50
11±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:
BDBM50613997
Synonyms:
CHEMBL5280047
Type:
Small organic molecule
Emp. Form.:
C18H15Cl2FN2O4
Mol. Mass.:
413.227
SMILES:
Cc1cc(=O)c2c(F)cncc2n1-c1c(Cl)cc(OCC(O)CO)cc1Cl |(3.33,-3.08,;2,-3.85,;2,-5.39,;.66,-6.16,;.66,-7.7,;-.67,-5.39,;-2,-6.16,;-2,-7.7,;-3.33,-5.4,;-3.33,-3.85,;-2,-3.08,;-.67,-3.85,;.66,-3.08,;.66,-1.54,;-.67,-.77,;-2.01,-1.54,;-.67,.77,;.66,1.54,;.66,3.08,;-.67,3.85,;-.67,5.39,;.66,6.16,;-2,6.16,;-2,7.7,;1.99,.77,;2,-.76,;3.33,-1.53,)|
Structure:
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