Reaction Details |
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Target | Nuclear receptor ROR-gamma |
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Ligand | BDBM190300 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Assay of Co-Activator Recruitment by TR-FRET |
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IC50 | 9.70±n/a nM |
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Citation | Schnute, ME; Flick, AC; Jones, P; Kaila, N; Mente, SR; Trzupek, JD; Vazquez, ML; Wennerstal, GM; Xing, L; Zamaratski, E; Zhang, L; Unwalla, RJ Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use therof US Patent US10227346 Publication Date 3/12/2019 |
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More Info.: | Get all data from this article, Assay Method |
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Nuclear receptor ROR-gamma |
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Name: | Nuclear receptor ROR-gamma |
Synonyms: | NR1F3 | Nuclear receptor ROR-gamma | Nuclear receptor ROR-gamma (RORC) | Nuclear receptor subfamily 1 group F member 3 | RAR-related orphan receptor C (RORc) | RORC | RORG | RORG_HUMAN | RZRG | Retinoid-related orphan receptor-gamma | Retinoid-related orphan receptor-gamma (RORc) |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 58218.40 |
Organism: | Homo sapiens (Human) |
Description: | P51449 |
Residue: | 518 |
Sequence: | MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQR
CNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQK
QLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKAS
GSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPG
LGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIF
SREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEV
VLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALY
TALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHV
ERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
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BDBM190300 |
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n/a |
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Name | BDBM190300 |
Synonyms: | US10227346, Example 62 | US10426135, Example 62 | US9670201, 62 (R)-3-chloro-N-(3-(1-isobutyryl-2,2-dimethylpiperidin-4-yl)-1,4-dimethyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-5-methoxybenzamide | US9920054, Example 62 |
Type | Small organic molecule |
Emp. Form. | C28H35ClN4O3 |
Mol. Mass. | 511.055 |
SMILES | COc1cc(Cl)cc(c1)C(=O)Nc1cnc2n(C)cc([C@@H]3CCN(C(=O)C(C)C)C(C)(C)C3)c2c1C |r| |
Structure |
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