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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM50248469
Substrate/Competitorn/a
Meas. Tech.ChEMBL_543009 (CHEMBL1018625)
IC50 0.9±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 Lett19:1522-7 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
11-beta-hydroxysteroid dehydrogenase 1
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:
MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAH
VVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNH
ITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMV
AAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEE
CALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
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  Blast E-value cutoff:
BDBM50248469
n/a
NameBDBM50248469
Synonyms:2-(4-((R)-4-(2,2-difluoro-2-(pyridin-4-yl)ethyl)-2-methylpiperazin-1-ylsulfonyl)phenyl)-1,1,1-trifluoropropan-2-ol | CHEMBL491489
TypeSmall organic molecule
Emp. Form.C21H24F5N3O3S
Mol. Mass.493.491
SMILESC[C@@H]1CN(CC(F)(F)c2ccncc2)CCN1S(=O)(=O)c1ccc(cc1)C(C)(O)C(F)(F)F |r|
Structure
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