Reaction Details Report a problem with these data
Target
Nuclear receptor ROR-gamma
Ligand
BDBM419138
Substrate
n/a
Meas. Tech.
GAL4-RORgamma Transactivation
IC50
>1000±n/a nM
Citation
 Musicki, B; Bouix-Peter, C; Ouvry, G; Thoreau, 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 | 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:
BDBM419138
Synonyms:
4-(tetrahydropyran-4- ylmethyl)-3,4-dihydro-2H- benzo[1,4]thiazine-6- sulfonic acid (4- ethylphenyl)isobutylamide | US10457637, Compound 6
Type:
Small organic molecule
Emp. Form.:
C26H36N2O3S2
Mol. Mass.:
488.706
SMILES:
CCc1ccc(cc1)N(CC(C)C)S(=O)(=O)c1ccc2SCCN(CC3CCOCC3)c2c1
Structure:
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