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TargetNuclear receptor ROR-gamma
LigandBDBM392006
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1989650 (CHEMBL4623385)
IC50 2.6±n/a nM
Citation Steeneck, CGege, CKinzel, OAlbers, MKleymann, GSchlüter, TSchulz, AXue, XCummings, MDFourie, AMLeonard, KAScott, BEdwards, JPHoffmann, TGoldberg, SD Discovery and optimization of new oxadiazole substituted thiazole ROR?t inverse agonists through a bioisosteric amide replacement approach. Bioorg Med Chem Lett30:0 (2020) [PubMed]  Article
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:
BDBM392006
n/a
NameBDBM392006
Synonyms:US10301272, Example 6/4
TypeSmall organic molecule
Emp. Form.C29H39N3O4S2
Mol. Mass.557.768
SMILESCC(C)(C)NS(=O)(=O)c1ccc(-c2sc(nc2CC2CCCCC2)C(=O)NCC(C)(C)O)c2ccccc12
Structure
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