Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50193795
Substrate
n/a
Meas. Tech.
ChEMBL_424105 (CHEMBL856751)
IC50
500±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:
BDBM50193795
Synonyms:
34-(4-((5-cyanopyridin-2-yloxy)methyl)-3,3-dimethyl-2-oxopyrrolidin-1-yl)bicyclo[2.2.2]octane-1-carboxamide | CHEMBL218569
Type:
Small organic molecule
Emp. Form.:
C22H28N4O3
Mol. Mass.:
396.4827
SMILES:
CC1(C)C(COc2ccc(cn2)C#N)CN(C1=O)C12CCC(CC1)(CC2)C(N)=O
Structure:
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