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Target11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E]
LigandBDBM32499
Substrate/CompetitorBDBM13739
Meas. Tech.Scintillation Proximity Assay (SPA)
pH6.5±n/a
Temperature296.15±n/a K
IC50 35±n/a nM
Citation Wang, HRuan, ZLi, JJSimpkins, LMSmirk, RAWu, SCHutchins, RDNirschl, DSVan Kirk, KCooper, CBSutton, JCMa, ZGolla, RSeethala, RSalyan, MENayeem, AKrystek, SRSheriff, SCamac, DMMorin, PECarpenter, BRobl, JAZahler, RGordon, DAHamann, LG Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem Lett18:3168-72 (2008) [PubMed]  Article
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11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E]
Name:11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E]
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.:31315.06
Organism:Homo sapiens (Human)
Description:P28845[23-292,A23S,F278E]
Residue:286
Sequence:
GSHMASMTGGQQMGRGSNEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTAR
SKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSL
NLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSAS
KFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEII
KGGALRQEEVYYDSSRWTTLLIRNPCRKILEELYSTSYNMDRFINK
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BDBM32499
BDBM13739
NameBDBM32499
Synonyms:pyridine amide, 8
TypeSmall organic molecule
Emp. Form.C19H20Cl2N2O3S
Mol. Mass.427.345
SMILESCC1CCN(CC1)C(=O)c1cccc(CS(=O)(=O)c2c(Cl)cccc2Cl)n1
Structure
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