Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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Ligand | BDBM29833 |
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Substrate/Competitor | BDBM13739 |
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Meas. Tech. | 11beta-HSD1 Homogeneous Time-Resolved Fluorescence (HTRF) Assay |
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pH | 7.4±n/a |
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Temperature | 310.15±n/a K |
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IC50 | 6±n/a nM |
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Citation | Lepifre, F; Christmann-Franck, S; Roche, D; Leriche, C; Carniato, D; Charon, C; Bozec, S; Doare, L; Schmidlin, F; Lecomte, M; Valeur, 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 |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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11-beta-hydroxysteroid dehydrogenase 1 |
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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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BDBM29833 |
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BDBM13739 |
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Name | BDBM29833 |
Synonyms: | spiro-carboxamide scaffold, 6 |
Type | Small organic molecule |
Emp. Form. | C19H24ClNO |
Mol. Mass. | 317.853 |
SMILES | Clc1ccc(cc1)C1(CC1)C(=O)N1CCC2(C1)CCCCC2 |
Structure |
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