Target
G protein-activated inward rectifier potassium channel 1/4
Ligand
BDBM585760
Substrate
n/a
Meas. Tech.
IonWorks Quattro system
IC50
23.0±n/a nM
Citation
 Barbe, GBebernitz, GRGeng, SGulgeze Efthymiou, HBLiao, LMa, FMo, RParker, DTPeng, YPeukert, SSmith, NYamada, KYasoshima, 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:
BDBM585760
Synonyms:
US11530213, Example 81
Type:
Small organic molecule
Emp. Form.:
C18H15Cl3N2O3
Mol. Mass.:
413.682
SMILES:
Cc1cc(=O)c2c(CC(O)CO)ncc(Cl)c2n1-c1c(Cl)cccc1Cl |(4,1.18,;2.67,.41,;2.67,-1.13,;1.33,-1.9,;1.33,-3.44,;,-1.13,;-1.33,-1.9,;-1.33,-3.44,;-2.67,-4.21,;-4,-3.44,;-2.67,-5.75,;-4,-6.52,;-2.67,-1.13,;-2.67,.41,;-1.33,1.18,;-1.33,2.72,;,.41,;1.33,1.18,;1.33,3.44,;2.67,4.21,;4,3.44,;2.67,5.75,;1.33,6.52,;,5.75,;,4.21,;-1.33,3.44,)|
Structure:
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