Target
Nuclear receptor ROR-gamma
Ligand
BDBM419256
Substrate
n/a
Meas. Tech.
GAL4-RORgamma Transactivation
IC50
<100±n/a nM
Citation
 Musicki, BBouix-Peter, COuvry, GThoreau, E Benzenesulfonamide derivatives as inverse agonists of retinoid-related orphan receptor gamma (RORγ(T)) US Patent  US10457637 Publication Date 10/29/2019
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 | 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:
BDBM419256
Synonyms:
N-(2,4-dimethylphenyl)-N- isobutyl-3-(S- methylsulfonimidoyl)-4- ((tetrahydro-2H-pyran-4- yl)methoxy)benzene- sulfonamide | US10457637, Compound 142
Type:
Small organic molecule
Emp. Form.:
C25H36N2O5S2
Mol. Mass.:
508.694
SMILES:
CC(C)CN(c1ccc(C)cc1C)S(=O)(=O)c1ccc(OCC2CCOCC2)c(c1)S(C)(=N)=O
Structure:
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