Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50252368
Substrate
n/a
Meas. Tech.
ChEMBL_487981 (CHEMBL1013112)
IC50
41±n/a nM
Citation
 Xiang, JWan, ZKLi, HQIpek, MBinnun, ENunez, JChen, LMcKew, JCMansour, TSXu, XSuri, VTam, MXing, YLi, XHahm, STobin, JSaiah, E Piperazine sulfonamides as potent, selective, and orally available 11beta-hydroxysteroid dehydrogenase type 1 inhibitors with efficacy in the rat cortisone-induced hyperinsulinemia model. J Med Chem 51:4068-71 (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 1 | 11beta-HSD1A | Corticosteroid 11-beta-dehydrogenase isozyme 1 | Corticosteroid 11-beta-dehydrogenase isozyme 1 (11-beta-HSD-1) | DHI1_MOUSE | Hsd11 | Hsd11b1
Type:
Enzyme
Mol. Mass.:
32369.70
Organism:
Mus musculus (mouse)
Description:
P50172
Residue:
292
Sequence:
MAVMKNYLLPILVLFLAYYYYSTNEEFRPEMLQGKKVIVTGASKGIGREMAYHLSKMGAHVVLTARSEEGLQKVVSRCLELGAASAHYIAGTMEDMTFAEQFIVKAGKLMGGLDMLILNHITQTSLSLFHDDIHSVRRVMEVNFLSYVVMSTAALPMLKQSNGSIAVISSLAGKMTQPMIAPYSASKFALDGFFSTIRTELYITKVNVSITLCVLGLIDTETAMKEISGIINAQASPKEECALEIIKGTALRKSEVYYDKSPLTPILLGNPGRKIMEFFSLRYYNKDMFVSN
  
Inhibitor
Name:
BDBM50252368
Synonyms:
(3S)-1-[3-({(2R)-4-[4-fluoro-2-(trifluoromethyl)phenyl]-2-methylpiperazin-1-yl}sulfonyl)phenyl]pyrrolidin-3-ol | CHEMBL519623
Type:
Small organic molecule
Emp. Form.:
C22H25F4N3O3S
Mol. Mass.:
487.511
SMILES:
C[C@@H]1CN(CCN1S(=O)(=O)c1cccc(c1)N1CC[C@H](O)C1)c1ccc(F)cc1C(F)(F)F |r|
Structure:
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