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Target11-beta-hydroxysteroid dehydrogenase 1
LigandBDBM29833
Substrate/CompetitorBDBM13739
Meas. Tech.11beta-HSD1 Homogeneous Time-Resolved Fluorescence (HTRF) Assay
pH7.4±n/a
Temperature310.15±n/a K
IC50 6±n/a nM
Citation Lepifre, FChristmann-Franck, SRoche, DLeriche, CCarniato, DCharon, CBozec, SDoare, LSchmidlin, FLecomte, MValeur, E Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold. Bioorg Med Chem Lett19:3682-5 (2009) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   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:
BDBM29833
BDBM13739
NameBDBM29833
Synonyms:spiro-carboxamide scaffold, 6
TypeSmall organic molecule
Emp. Form.C19H24ClNO
Mol. Mass.317.853
SMILESClc1ccc(cc1)C1(CC1)C(=O)N1CCC2(C1)CCCCC2
Structure
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