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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM29865
Substrate/CompetitorBDBM13739
Meas. Tech.Measurement of 11beta-HSD1 Activity
pH8±n/a
Temperature295.15±n/a K
Ki 9.8±n/a nM
Citation Siu, MJohnson, TOWang, YNair, SKTaylor, WDCripps, SJMatthews, JJEdwards, MPPauly, TAErmolieff, JCastro, AHosea, NALaPaglia, AFanjul, ANVogel, JE N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett19:3493-7 (2009) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  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:
BDBM29865
BDBM13739
NameBDBM29865
Synonyms:N-(Pyridin-2-yl) arylsulfonamide, 27
TypeSmall organic molecule
Emp. Form.C19H16N4O2S
Mol. Mass.364.421
SMILESCNc1cccc(NS(=O)(=O)c2ccc(cc2)-c2ccc(cc2)C#N)n1
Structure
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