Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 [24-292,C272S] |
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Ligand | BDBM32550 |
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Substrate/Competitor | BDBM13739 |
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Meas. Tech. | Human 11beta-HSD1 SPA Assay |
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pH | 7.2±n/a |
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Temperature | 295.15±n/a K |
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IC50 | 7±n/a nM |
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EC50 | 241±n/a nM |
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Citation | Sun, D; Wang, Z; Di, Y; Jaen, JC; Labelle, M; Ma, J; Miao, S; Sudom, A; Tang, L; Tomooka, CS; Tu, H; Ursu, S; Walker, N; Yan, X; Ye, Q; Powers, JP Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). Bioorg Med Chem Lett18:3513-6 (2008) [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 [24-292,C272S] |
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Name: | 11-beta-hydroxysteroid dehydrogenase 1 [24-292,C272S] |
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.: | 31804.08 |
Organism: | Homo sapiens (Human) |
Description: | Purified recombinant human 11beta-HSD1. |
Residue: | 286 |
Sequence: | MKHQHQHQHQHQHQQPLNEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTAR
SKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSL
NLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSAS
KFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEII
KGGALRQEEVYYDSSLWTTLLIRNPSRKILEFLYSTSYNMDRFINK
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BDBM32550 |
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BDBM13739 |
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Name | BDBM32550 |
Synonyms: | arylsulfonylpiperazine, 22 |
Type | Small organic molecule |
Emp. Form. | C16H14Cl2F3N3O2S |
Mol. Mass. | 440.267 |
SMILES | FC(F)(F)c1cccnc1N1CCN(CC1)S(=O)(=O)c1ccc(Cl)cc1Cl |
Structure |
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