Reaction Details
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11-beta-hydroxysteroid dehydrogenase type 2
Ligand
BDBM50348309
Substrate
n/a
Meas. Tech.
ChEMBL_757492 (CHEMBL1804464)
IC50
2520±n/a nM
Citation
Wang, H; Robl, JA; Hamann, LG; Simpkins, L; Golla, R; Li, YX; Seethala, R; Zvyaga, T; Gordon, DA; Li, JJ Generation of 3,8-substituted 1,2,4-triazolopyridines as potent inhibitors of human 11ß-hydroxysteroid dehydrogenase type 1 (11ß-HSD-1). Bioorg Med Chem Lett 21:4146-9 (2011) [PubMed] Article More Info.:
Target
Name:
11-beta-hydroxysteroid dehydrogenase type 2
Synonyms:
11-DH2 | 11-beta-HSD2 | 11-beta-Hydroxysteroid Dehydrogenase 2 (11-beta-HSD2) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 2 | 11-beta-hydroxysteroid dehydrogenase type 2 | 11-beta-hydroxysteroid dehydrogenase type 2 (11-beta-HSD2) | Corticosteroid 11-beta-dehydrogenase isozyme 2 | DHI2_HUMAN | HSD11B2 | HSD11K | NAD-dependent 11-beta-hydroxysteroid dehydrogenase | SDR9C3
Type:
Enzyme
Mol. Mass.:
44141.72
Organism:
Homo sapiens (Human)
Description:
Purified recombinant human 11beta-HSD2.
Residue:
405
Sequence:
MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAVLAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPGAIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELSPVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVALLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYIEHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRRRFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR
Inhibitor
Name:
BDBM50348309
Synonyms:
CHEMBL1800134
Type:
Small organic molecule
Emp. Form.:
C21H22ClN3O2
Mol. Mass.:
383.871
SMILES:
Cc1c(Cl)cccc1Oc1cccn2c(nnc12)C12CCC(O)(CC1)CC2
Structure:
