Target
11-beta-hydroxysteroid dehydrogenase type 2
Ligand
BDBM50273454
Substrate
n/a
Meas. Tech.
ChEMBL_561274 (CHEMBL1016222)
IC50
>10000±n/a nM
Citation
 Fotsch, CBartberger, MDBercot, EAChen, MCupples, REmery, MFretland, JGuram, AHale, CHan, NHickman, DHungate, RWHayashi, MKomorowski, RLiu, QMatsumoto, GSt Jean, DJUrsu, SVéniant, MXu, GYe, QYuan, CZhang, JZhang, XTu, HWang, M Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model. J Med Chem 51:7953-67 (2008) [PubMed]  Article 
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:
Human
Description:
Purified recombinant human 11beta-HSD2.
Residue:
405
Sequence:
MERWPWPSGGAWLLVAARALLQLLRSDLRLGRPLLAALALLAALDWLCQRLLPPPAALAVLAAAGWIALSRLARPQRLPVATRAVLITGCDSGFGKETAKKLDSMGFTVLATVLELNSPGAIELRTCCSPRLRLLQMDLTKPGDISRVLEFTKAHTTSTGLWGLVNNAGHNEVVADAELSPVATFRSCMEVNFFGALELTKGLLPLLRSSRGRIVTVGSPAGDMPYPCLGAYGTSKAAVALLMDTFSCELLPWGVKVSIIQPGCFKTESVRNVGQWEKRKQLLLANLPQELLQAYGKDYIEHLHGQFLHSLRLAMSDLTPVVDAITDALLAARPRRRYYPGQGLGLMYFIHYYLPEGLRRRFLQAFFISHCLPRALQPGQPGTTPPQDAAQDPNLSPGPSPAVAR
  
Inhibitor
Name:
BDBM50273454
Synonyms:
2-[(S)-1-(2-Fluorophenyl)ethylamino]-5-(2-hydroxypropan-2-yl)-5-methylthiazol-4(5H)-one | CHEMBL456537
Type:
Small organic molecule
Emp. Form.:
C15H19FN2O2S
Mol. Mass.:
310.387
SMILES:
C[C@H](NC1=NC(=O)C(C)(S1)C(C)(C)O)c1ccccc1F |r,t:3|
Structure:
Search PDB for entries with ligand similarity: