Reaction Details |
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Target | Nuclear receptor ROR-gamma |
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Ligand | BDBM504259 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Transcreener-Fluorecescence Polarization Assay |
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Ki | 2.60±n/a nM |
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Citation | Bryan, MC; Do, S; Drobnick, J; Gobbi, A; Katsumoto, T; Kiefer, Jr., JR; Liang, J; Rajapaksa, NS; Chen, Y; Fu, L; Lai, KW; Liu, Z; Wai, J; Wang, F Pyrazolo[ 1,5a]pyrimidine derivatives as IRAK4 modulators US Patent US11034698 Publication Date 6/15/2021 |
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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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BDBM504259 |
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n/a |
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Name | BDBM504259 |
Synonyms: | (R)-N-(2-(2-Fluoro-3-hydroxy- 3-methylbutyl)-1-oxo-6-(4- (2,2,2-trifluoroethyl)piperazin-1- yl)isoindolin-5-yl)pyrazolo[1,5 a]pyrimidine-3-carboxamide | US11034698, Example 109 |
Type | Small organic molecule |
Emp. Form. | C27H32F3N7O3 |
Mol. Mass. | 559.5833 |
SMILES | CC(F)(F)CN1CCN(CC1)c1cc2C(=O)N(C[C@@H](F)C(C)(C)O)Cc2cc1NC(=O)c1cnn2cccnc12 |r| |
Structure |
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