Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50243672
Substrate
n/a
Meas. Tech.
ChEMBL_487343 (CHEMBL1021869)
IC50
2.1±n/a nM
Citation
 Julian, LDWang, ZBostick, TCaille, SChoi, RDeGraffenreid, MDi, YHe, XHungate, RWJaen, JCLiu, JMonshouwer, MMcMinn, DRew, YSudom, ASun, DTu, HUrsu, SWalker, NYan, XYe, QPowers, JP Discovery of novel, potent benzamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model. J Med Chem 51:3953-60 (2008) [PubMed]  Article
Target
Name:
11-beta-hydroxysteroid dehydrogenase 1
Synonyms:
11-DH | 11-beta-HSD1 | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | 11-beta-hydroxysteroid dehydrogenase | 11-beta-hydroxysteroid dehydrogenase 1 (11HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11beta-HSD1) | DHI1_HUMAN | HSD11 | HSD11B1 | HSD11L | SDR26C1
Type:
Enzyme
Mol. Mass.:
32409.16
Organism:
Homo sapiens (Human)
Description:
P28845
Residue:
292
Sequence:
MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
  
Inhibitor
Name:
BDBM50243672
Synonyms:
1,1,1-trifluoro-2-(4-((S)-2-methylpiperidin-1-ylsulfonyl)phenyl)propan-2-ol | CHEMBL472116
Type:
Small organic molecule
Emp. Form.:
C15H20F3NO3S
Mol. Mass.:
351.384
SMILES:
C[C@H]1CCCCN1S(=O)(=O)c1ccc(cc1)C(C)(O)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: