Reaction Details
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Aldo-keto reductase family 1 member B1
Ligand
BDBM16452
Substrate
BDBM16443
Meas. Tech.
In Vitro Aldose Reductase Inhibition Assay
pH
7.0000±n/a
Temperature
297.1500±n/a K
IC50
4±n/a nM
Citation
Mylari, BL; Armento, SJ; Beebe, DA; Conn, EL; Coutcher, JB; Dina, MS; O'Gorman, MT; Linhares, MC; Martin, WH; Oates, PJ; Tess, DA; Withbroe, GJ; Zembrowski, WJ A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one. J Med Chem 46:2283-6 (2003) [PubMed] Article Target
Name:
Aldo-keto reductase family 1 member B1
Synonyms:
AR | Aldose reductase | Aldose Reductase (ALR2) | Aldo-keto reductase family 1 member B1 (AKR1B1) | ALDR_HUMAN | AKR1B1 | ALDR1 | ALR2 | Aldose reductase (AR)
Type:
Protein
Mol. Mass.:
35855.50
Organism:
Human
Description:
P15121. 4LAU; 2IKI; 4LB4; 2FZD; 2FZ8; 1US0
Residue:
316
Sequence:
MASRLLLNNGAKMPILGLGTWKSPPGQVTEAVKVAIDVGYRHIDCAHVYQNENEVGVAIQEKLREQVVKREELFIVSKLWCTYHEKGLVKGACQKTLSDLKLDYLDLYLIHWPTGFKPGKEFFPLDESGNVVPSDTNILDTWAAMEELVDEGLVKAIGISNFNHLQVEMILNKPGLKYKPAVNQIECHPYLTQEKLIQYCQSKGIVVTAYSPLGSPDRPWAKPEDPSLLEDPRIKAIAAKHNKTTAQVLIRFPMQRNLVVIPKSVTPERIAENFKVFDFELSSQDMTTLLSYNRNWRVCALLSCTSHKDYPFHEEF
Inhibitor
Name:
BDBM16452
Synonyms:
(4-oxo-3-{[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl}-3,4-dihydrophthalazin-1-yl)acetic acid | 2-(4-oxo-3-{[5-(trifluoromethyl)-1,3-benzothiazol-2-yl]methyl}-3,4-dihydrophthalazin-1-yl)acetic acid | Xedia | CHEMBL10372 | Alond | Zopolrestat
Type:
Small organic molecule
Emp. Form.:
TBD
Mol. Mass.:
TBD
SMILES:
TBD

