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Target11-beta-hydroxysteroid dehydrogenase 1 [24-292,C272S]
LigandBDBM32534
Substrate/CompetitorBDBM13739
Meas. Tech.Human 11beta-HSD1 SPA Assay
pH7.2±n/a
Temperature295.15±n/a K
IC50 20±n/a nM
EC50 574±n/a nM
Citation Sun, DWang, ZDi, YJaen, JCLabelle, MMa, JMiao, SSudom, ATang, LTomooka, CSTu, HUrsu, SWalker, NYan, XYe, QPowers, JP Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). Bioorg Med Chem Lett18:3513-6 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
11-beta-hydroxysteroid dehydrogenase 1 [24-292,C272S]
Name:11-beta-hydroxysteroid dehydrogenase 1 [24-292,C272S]
Synonyms:11-DH | 11-beta-Hydroxysteroid Dehydrogenase 1 (11-beta-HSD1) | Corticosteroid 11-beta-dehydrogenase isozyme 1 | DHI1_HUMAN | HSD11 | HSD11B1 | HSD11L | SDR26C1
Type:Homodimer
Mol. Mass.:31804.08
Organism:Homo sapiens (Human)
Description:Purified recombinant human 11beta-HSD1.
Residue:286
Sequence:
MKHQHQHQHQHQHQQPLNEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTAR
SKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSL
NLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSAS
KFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEII
KGGALRQEEVYYDSSLWTTLLIRNPSRKILEFLYSTSYNMDRFINK
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BDBM32534
BDBM13739
NameBDBM32534
Synonyms:arylsulfonylpiperazine, 6
TypeSmall organic molecule
Emp. Form.C17H18F3N3O2S
Mol. Mass.385.404
SMILESFC(F)(F)c1cccnc1N1CCN(CC1)S(=O)(=O)Cc1ccccc1
Structure
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