Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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Ligand | BDBM29857 |
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Substrate/Competitor | BDBM13739 |
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Meas. Tech. | Measurement of 11beta-HSD1 Activity |
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pH | 8±n/a |
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Temperature | 295.15±n/a K |
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Ki | 20±n/a nM |
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Comments | 87% inhibition @ 0.1 uM. |
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Citation | Siu, M; Johnson, TO; Wang, Y; Nair, SK; Taylor, WD; Cripps, SJ; Matthews, JJ; Edwards, MP; Pauly, TA; Ermolieff, J; Castro, A; Hosea, NA; LaPaglia, A; Fanjul, AN; Vogel, 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 |
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More Info.: | Get all data from this article, 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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BDBM29857 |
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BDBM13739 |
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Name | BDBM29857 |
Synonyms: | N-(Pyridin-2-yl) arylsulfonamide, 19 |
Type | Small organic molecule |
Emp. Form. | C18H15FN2O2S |
Mol. Mass. | 342.387 |
SMILES | Cc1cccc(NS(=O)(=O)c2ccc(cc2)-c2ccc(F)cc2)n1 |
Structure |
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