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TargetNuclear receptor ROR-gamma
LigandBDBM190341
Substrate/Competitorn/a
Meas. Tech.Assay of Co-Activator Recruitment by TR-FRET
IC50 16.5±n/a nM
Citation Schnute, MEFlick, ACJones, PKaila, NMente, SRTrzupek, JDVazquez, MLWennerstal, GMXing, LZamaratski, EZhang, LUnwalla, RJ Methyl- and trifluoromethyl-substituted pyrrolopyridine modulators of RORC2 and methods of use therof US Patent US10227346 Publication Date 3/12/2019
More Info.:Get all data from this article,  Assay Method
 
Nuclear receptor ROR-gamma
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM190341
n/a
NameBDBM190341
Synonyms:US10227346, Example 92 | US10426135, Example 92 | US9670201, 92 3-cyano-N-(1,4-dimethyl-3-((2S,4R)-2-methyl-1-((R)-3,3,3-trifluoro-2-methylpropanoyl)piperidin-4-yl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide | US9920054, Example 92
TypeSmall organic molecule
Emp. Form.C27H28F3N5O2
Mol. Mass.511.5387
SMILESC[C@H](C(=O)N1CC[C@H](C[C@@H]1C)c1cn(C)c2ncc(NC(=O)c3cccc(c3)C#N)c(C)c12)C(F)(F)F |r|
Structure
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