| Reaction Details |
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 | Report a problem with these data |
| Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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| Ligand | BDBM29843 |
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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 | 169±n/a nM |
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| Comments | 55% 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 |
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| 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 |
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| Type: | Enzyme |
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| Mol. Mass.: | 32409.16 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P28845 |
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| Residue: | 292 |
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| Sequence: | MAFMKKYLLPILGLFMAYYYYSANEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAH
VVVTARSKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNH
ITNTSLNLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMV
AAYSASKFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEE
CALEIIKGGALRQEEVYYDSSLWTTLLIRNPCRKILEFLYSTSYNMDRFINK
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| BDBM29843 |
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| BDBM13739 |
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| Name | BDBM29843 |
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| Synonyms: | N-(Pyridin-2-yl) arylsulfonamide, 3 |
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| Type | Small organic molecule |
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| Emp. Form. | C19H22ClN3O3S |
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| Mol. Mass. | 407.914 |
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| SMILES | Cc1c(Cl)cccc1S(=O)(=O)Nc1cccc(CC(=O)N2CCCCC2)n1 |
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| Structure | 
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