Reaction Details
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ATP-sensitive inward rectifier potassium channel 1
Ligand
BDBM155928
Substrate
n/a
Meas. Tech.
ChEMBL_1515531 (CHEMBL3615712)
IC50
14±n/a nM
Citation
Walsh, SP; Shahripour, A; Tang, H; Teumelsan, N; Frie, J; Zhu, Y; Priest, BT; Swensen, AM; Liu, J; Margulis, M; Visconti, R; Weinglass, A; Felix, JP; Brochu, RM; Bailey, T; Thomas-Fowlkes, B; Alonso-Galicia, M; Zhou, X; Pai, LY; Corona, A; Hampton, C; Hernandez, M; Bentley, R; Chen, J; Shah, K; Metzger, J; Forrest, M; Owens, K; Tong, V; Ha, S; Roy, S; Kaczorowski, GJ; Yang, L; Parmee, E; Garcia, ML; Sullivan, K; Pasternak, A Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation. ACS Med Chem Lett 6:747-52 (2015) [PubMed] Article More Info.:
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:
BDBM155928
Synonyms:
US9018211, 52
Type:
Small organic molecule
Emp. Form.:
C24H28N4O5
Mol. Mass.:
452.5029
SMILES:
COc1cc(ncc1C#N)[C@@H](O)CN1CCN(C[C@H](O)c2ccc3C(=O)OCc3c2C)CC1 |r|
Structure:
