Target
ATP-sensitive inward rectifier potassium channel 1
Ligand
BDBM290057
Substrate
n/a
Meas. Tech.
ChEMBL_1822312 (CHEMBL4322076)
IC50
60±n/a nM
Citation
 Aretz, CDVadukoot, AKHopkins, CR Discovery of Small Molecule Renal Outer Medullary Potassium (ROMK) Channel Inhibitors: A Brief History of Medicinal Chemistry Approaches To Develop Novel Diuretic Therapeutics. J Med Chem 62:8682-8694 (2019) [PubMed]  Article
Target
Name:
ATP-sensitive inward rectifier potassium channel 1
Synonyms:
ATP-regulated potassium channel ROM-K | ATP-regulated potassium channel ROMK | ATP-sensitive inward rectifier potassium channel 1 | Egl nine homolog 1 | KCNJ1 | KCNJ1_HUMAN | Potassium channel (ATP modulatory) | Potassium inwardly-rectifying channel, subfamily J, member 1 | ROMK1 | Renal Outer Medullary Potassium (ROMK1) | The Renal Outer Medullary Potassium (ROMK)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
44809.08
Organism:
Homo sapiens (Human)
Description:
gi_223460826
Residue:
391
Sequence:
MNASSRNVFDTLIRVLTESMFKHLRKWVVTRFFGHSRQRARLVSKDGRCNIEFGNVEAQSRFIFFVDIWTTVLDLKWRYKMTIFITAFLGSWFFFGLLWYAVAYIHKDLPEFHPSANHTPCVENINGLTSAFLFSLETQVTIGYGFRCVTEQCATAIFLLIFQSILGVIINSFMCGAILAKISRPKKRAKTITFSKNAVISKRGGKLCLLIRVANLRKSLLIGSHIYGKLLKTTVTPEGETIILDQININFVVDAGNENLFFISPLTIYHVIDHNSPFFHMAAETLLQQDFELVVFLDGTVESTSATCQVRTSYVPEEVLWGYRFAPIVSKTKEGKYRVDFHNFSKTVEVETPHCAMCLYNEKDVRARMKRGYDNPNFILSEVNETDDTKM
  
Inhibitor
Name:
BDBM290057
Synonyms:
US9573961, Example 42
Type:
Small organic molecule
Emp. Form.:
C24H25N7O2
Mol. Mass.:
443.501
SMILES:
Cc1c(cccc1[C@@H]1CN2CCN(C[C@H]2CO1)C(=O)Cc1ccc(cc1)-n1cnnn1)C#N |r|
Structure:
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