Target
Nuclear receptor ROR-gamma
Ligand
BDBM293062
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:
BDBM293062
Synonyms:
US10106501, Example AI1 | cis-4-(2,4-dichloro-3-((1,4-dimethyl-6-(trifluoromethyl)-1H-indol-2-yl)methyl)phenoxy)cyclohexanecarboxylic acid
Type:
Small organic molecule
Emp. Form.:
C23H20Cl2F3NO3
Mol. Mass.:
486.311
SMILES:
Cc1cc(cc2n(C)c(Cc3c(Cl)ccc(O[C@H]4C[C@H](C4)C(O)=O)c3Cl)cc12)C(F)(F)F |r,wU:17.16,19.21,(3.14,-8.45,;2.37,-7.11,;3.14,-5.78,;2.37,-4.45,;.83,-4.45,;.06,-5.78,;-1.45,-6.1,;-2.59,-5.07,;-1.61,-7.63,;-2.94,-8.4,;-2.94,-9.94,;-4.28,-10.71,;-5.61,-9.94,;-4.28,-12.25,;-2.94,-13.02,;-1.61,-12.25,;-.28,-13.02,;1.06,-12.25,;1.46,-10.76,;2.94,-11.16,;2.55,-12.65,;4.28,-10.39,;5.61,-11.16,;4.28,-8.85,;-1.61,-10.71,;-.28,-9.94,;-.2,-8.26,;.83,-7.11,;3.14,-3.11,;2.37,-1.78,;4.68,-3.11,;3.91,-1.78,)|
Structure:
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