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Target
ATP-sensitive inward rectifier potassium channel 1
Ligand
BDBM194954
Substrate
n/a
Meas. Tech.
ChEMBL_2155251 (CHEMBL5039911)
IC50
2.8±n/a nM
Citation
 Jiang, J; Ding, FX; Zhou, X; Bateman, TJ; Dong, S; Gu, X; Keh deJesus, R; Pio, B; Tang, H; Chobanian, HR; Levorse, D; Hu, M; Thomas-Fowlkes, B; Margulis, M; Koehler, M; Weinglass, A; Gibson, J; Houle, K; Yudkovitz, J; Hampton, C; Pai, LY; Samuel, K; Cutarelli, T; Sullivan, K; Parmee, ER; Davies, I; Pasternak, A Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic. J Med Chem 64:7691-7701 (2021) [PubMed]  Article 
Target
Name:
ATP-sensitive inward rectifier potassium channel 1
Synonyms:
ATP-regulated potassium channel ROM-K | ATP-sensitive inward rectifier potassium channel 1 | Inward rectifier K(+) channel Kir1.1 | KAB-1 | KCNJ1_RAT | Kcnj1 | Potassium channel (ATP modulatory) | Potassium channel, inwardly rectifying subfamily J member 1 | Renal Outer Medullary Potassium (ROMK) | Renal Outer Medullary Potassium (ROMK1) | Romk1 | The Renal Outer Medullary Potassium (ROMK) channel (Kir1.1)
Type:
Enzyme
Mol. Mass.:
44976.27
Organism:
Rattus norvegicus (Rat)
Description:
P35560
Residue:
391
Sequence:
MGASERSVFRVLIRALTERMFKHLRRWFITHIFGRSRQRARLVSKEGRCNIEFGNVDAQSRFIFFVDIWTTVLDLKWRYKMTVFITAFLGSWFLFGLLWYVVAYVHKDLPEFYPPDNRTPCVENINGMTSAFLFSLETQVTIGYGFRFVTEQCATAIFLLIFQSILGVIINSFMCGAILAKISRPKKRAKTITFSKNAVISKRGGKLCLLIRVANLRKSLLIGSHIYGKLLKTTITPEGETIILDQTNINFVVDAGNENLFFISPLTIYHIIDHNSPFFHMAAETLSQQDFELVVFLDGTVESTSATCQVRTSYVPEEVLWGYRFVPIVSKTKEGKYRVDFHNFGKTVEVETPHCAMCLYNEKDARARMKRGYDNPNFVLSEVDETDDTQM
  
Inhibitor
Name:
BDBM194954
Synonyms:
US9206198, 7
Type:
Small organic molecule
Emp. Form.:
C24H28N2O6
Mol. Mass.:
440.4889
SMILES:
CC1=C(COC1=O)N1CCC2(CCN(C[C@H](O)c3ccc4C(=O)OCc4c3C)CC2)C1=O |r,t:1|
Structure:
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