Target
11-beta-hydroxysteroid dehydrogenase 1
Ligand
BDBM50248471
Substrate
n/a
Meas. Tech.
ChEMBL_543009 (CHEMBL1018625)
IC50
0.4±n/a nM
Citation
 Sun, DWang, ZCardozo, MChoi, RDegraffenreid, MDi, YHe, XJaen, JCLabelle, MLiu, JMa, JMiao, SSudom, ATang, LTu, HUrsu, SWalker, NYan, XYe, QPowers, JP Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). Bioorg Med Chem Lett 19:1522-7 (2009) [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:
BDBM50248471
Synonyms:
1,1,1-trifluoro-2-(4-((R)-2-methyl-4-((1-(pyridin-4-yl)cyclopropyl)methyl)piperazin-1-ylsulfonyl)phenyl)propan-2-ol | CHEMBL522964
Type:
Small organic molecule
Emp. Form.:
C23H28F3N3O3S
Mol. Mass.:
483.547
SMILES:
C[C@@H]1CN(CC2(CC2)c2ccncc2)CCN1S(=O)(=O)c1ccc(cc1)C(C)(O)C(F)(F)F |r|
Structure:
Search PDB for entries with ligand similarity: