Reaction Details |
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Target | 11-beta-hydroxysteroid dehydrogenase 1 |
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Ligand | BDBM107487 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1685710 (CHEMBL4036189) |
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IC50 | 0.800000±n/a nM |
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Citation | Zhuang, L; Tice, CM; Xu, Z; Zhao, W; Cacatian, S; Ye, YJ; Singh, SB; Lindblom, P; McKeever, BM; Krosky, PM; Zhao, Y; Lala, D; Kruk, BA; Meng, S; Howard, L; Johnson, JA; Bukhtiyarov, Y; Panemangalore, R; Guo, J; Guo, R; Himmelsbach, F; Hamilton, B; Schuler-Metz, A; Schauerte, H; Gregg, R; McGeehan, GM; Leftheris, K; Claremon, DA Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11? hydroxysteroid dehydrogenase type 1 inhibitor. Bioorg Med Chem25:3649-3657 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, 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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BDBM107487 |
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n/a |
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Name | BDBM107487 |
Synonyms: | US8575157, 201 | US8592410, Comparator 13 | US8598163, 71 |
Type | Small organic molecule |
Emp. Form. | C22H25BrFNO3 |
Mol. Mass. | 450.341 |
SMILES | C[C@H](N1CC[C@@](CC(C)(C)O)(OC1=O)c1ccc(F)cc1)c1ccc(Br)cc1 |r| |
Structure |
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