Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50193783
Substrate
n/a
Meas. Tech.
ChEMBL_424105 (CHEMBL856751)
IC50
518±n/a nM
Citation
 Yeh, VSKurukulasuriya, RFung, SMonzon, KChiou, WWang, JStolarik, DImade, HShapiro, RKnourek-Segel, VBush, EWilcox, DNguyen, PTBrune, MJacobson, PLink, JT Discovery of orally active butyrolactam 11beta-HSD1 inhibitors. Bioorg Med Chem Lett 16:5555-60 (2006) [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:
BDBM50193783
Synonyms:
(1R,7S,8r)-ethyl 4-(4-((5-cyanopyridin-2-yloxy)methyl)-3,3-dimethyl-2-oxopyrrolidin-1-yl)bicyclo[5.1.0]octane-8-carboxylate | CHEMBL218943
Type:
Small organic molecule
Emp. Form.:
C24H31N3O4
Mol. Mass.:
425.5206
SMILES:
CCOC(=O)[C@@H]1[C@H]2CCC(CC[C@@H]12)N1CC(COc2ccc(cn2)C#N)C(C)(C)C1=O
Structure:
Search PDB for entries with ligand similarity: