Target
Nuclear receptor ROR-gamma
Ligand
BDBM292884
Substrate
n/a
Meas. Tech.
transient transactivation assay
IC50
<100±n/a nM
Citation
 Argiriadi, MABreinlinger, ECCusack, KPHobson, ADPotin, DBarth, MAmaudrut, JPoupardin, OMounier, LKort, ME Nuclear receptor modulators US Patent  US10106501 Publication Date 10/23/2018 
Target
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:
MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQRCNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQKQLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKASGSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
  
Inhibitor
Name:
BDBM292884
Synonyms:
US10106501, Example S
Type:
Small organic molecule
Emp. Form.:
C28H28Cl2F3N3O3
Mol. Mass.:
582.441
SMILES:
Cc1cc(cc2n(C)c(Cc3c(Cl)ccc(C(=O)N4CCN(CC4)C4CC(C4)C(O)=O)c3Cl)cc12)C(F)(F)F |(1.14,-.28,;.37,1.06,;1.14,2.39,;.37,3.72,;-1.17,3.72,;-1.94,2.39,;-3.45,2.07,;-4.54,3.16,;-3.61,.54,;-4.94,-.23,;-4.94,-1.77,;-6.28,-2.54,;-7.61,-1.77,;-6.28,-4.08,;-4.94,-4.85,;-3.61,-4.08,;-2.28,-4.85,;-2.28,-6.39,;-.94,-4.08,;.39,-4.85,;1.72,-4.08,;1.72,-2.54,;.39,-1.77,;-.94,-2.54,;3.06,-1.77,;4.55,-2.17,;4.94,-.68,;3.46,-.28,;6.28,.09,;7.61,-.68,;6.28,1.63,;-3.61,-2.54,;-2.28,-1.77,;-2.2,-.09,;-1.17,1.06,;1.14,5.06,;1.91,6.39,;2.47,4.29,;-.2,5.83,)|
Structure:
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