Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E] |
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Ligand | BDBM32499 |
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Substrate/Competitor | BDBM13739 |
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Meas. Tech. | Scintillation Proximity Assay (SPA) |
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pH | 6.5±n/a |
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Temperature | 296.15±n/a K |
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IC50 | 35±n/a nM |
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Citation | Wang, H; Ruan, Z; Li, JJ; Simpkins, LM; Smirk, RA; Wu, SC; Hutchins, RD; Nirschl, DS; Van Kirk, K; Cooper, CB; Sutton, JC; Ma, Z; Golla, R; Seethala, R; Salyan, ME; Nayeem, A; Krystek, SR; Sheriff, S; Camac, DM; Morin, PE; Carpenter, B; Robl, JA; Zahler, R; Gordon, DA; Hamann, LG Pyridine amides as potent and selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1. Bioorg Med Chem Lett18:3168-72 (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 [23-292,A23S,F278E] |
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Name: | 11-beta-hydroxysteroid dehydrogenase 1 [23-292,A23S,F278E] |
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.: | 31315.06 |
Organism: | Homo sapiens (Human) |
Description: | P28845[23-292,A23S,F278E] |
Residue: | 286 |
Sequence: | GSHMASMTGGQQMGRGSNEEFRPEMLQGKKVIVTGASKGIGREMAYHLAKMGAHVVVTAR
SKETLQKVVSHCLELGAASAHYIAGTMEDMTFAEQFVAQAGKLMGGLDMLILNHITNTSL
NLFHDDIHHVRKSMEVNFLSYVVLTVAALPMLKQSNGSIVVVSSLAGKVAYPMVAAYSAS
KFALDGFFSSIRKEYSVSRVNVSITLCVLGLIDTETAMKAVSGIVHMQAAPKEECALEII
KGGALRQEEVYYDSSRWTTLLIRNPCRKILEELYSTSYNMDRFINK
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BDBM32499 |
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BDBM13739 |
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Name | BDBM32499 |
Synonyms: | pyridine amide, 8 |
Type | Small organic molecule |
Emp. Form. | C19H20Cl2N2O3S |
Mol. Mass. | 427.345 |
SMILES | CC1CCN(CC1)C(=O)c1cccc(CS(=O)(=O)c2c(Cl)cccc2Cl)n1 |
Structure |
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