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Target
Isoform 2 of Nuclear receptor ROR-gamma (RORgT)
Ligand
BDBM256359
Substrate
n/a
Meas. Tech.
TR-FRET Assay
pH
7±n/a
Temperature
277.15±n/a K
IC50
6±n/a nM
Comments
extracted
Citation
 Barr, KJ; Maclean, JK; Zhang, H; Beresis, RT; Zhang, D; Andresen, BM; Anthony, NJ; Lapointe, BT; Sciammetta, N 3-cyclohexenyl and cyclohexyl substituted indole and indazole compounds as RORgammaT inhibitors and uses thereof US Patent  US9487490 Publication Date 11/8/2016 
Target
Name:
Isoform 2 of Nuclear receptor ROR-gamma (RORgT)
Synonyms:
Isoform 2 of Nuclear receptor ROR-gamma | NR1F3 | Nuclear receptor ROR-gamma (RORgT) | Nuclear receptor ROR-gammaT | RORC | RORG | RORG_HUMAN | RZRG | Retinoid-related orphan receptor-gamma (RORgT) | Retinoid-related orphan receptor-gamma (RORĪ³T)
Type:
Protein
Mol. Mass.:
55831.73
Organism:
Homo sapiens (Human)
Description:
P51449-2
Residue:
497
Sequence:
MRTQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQRCNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQKQLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKASGSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
  
Inhibitor
Name:
BDBM256359
Synonyms:
US9487490, 4G
Type:
Small organic molecule
Emp. Form.:
C28H25ClF3N3O4
Mol. Mass.:
559.964
SMILES:
C[C@H]1CCCN1C(=O)c1ccc2c(nn(C(=O)c3c(Cl)cccc3C(F)(F)F)c2c1)C1=CCC(CC1)C(O)=O |r,t:34|
Structure:
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