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Target
Isoform 2 of Nuclear receptor ROR-gamma (RORgT)
Ligand
BDBM392168
Substrate
n/a
Meas. Tech.
RORgamma Gal4 Reporter Gene Assay (REN)
IC50
1.26±n/a nM
Citation
 Gege, C; Steeneck, C; Kinzel, O; Kleymann, G; Hoffmann, T Carboxamide or sulfonamide substituted thiazoles and related derivatives as modulators for the orphan nuclear receptor ROR[γ] US Patent  US10301272 Publication Date 5/28/2019 
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:
BDBM392168
Synonyms:
US10301272, Example 20 | trans-3-(4-(Cyclohexylmethyl-5-(4-(N-(4-fluoro-2-methylbutan-2-yl)sulfamoyl)naphthalen-1-yl)thiazole-2-carboxamido)cyclobutanecarboxylic acid
Type:
Small organic molecule
Emp. Form.:
C31H38FN3O5S2
Mol. Mass.:
615.779
SMILES:
CC(C)(CCF)NS(=O)(=O)c1ccc(-c2sc(nc2CC2CCCCC2)C(=O)N[C@H]2C[C@@H](C2)C(O)=O)c2ccccc12 |r,wU:29.30,wD:31.35,(7.11,-2.53,;7.51,-1.04,;8.6,-2.13,;8.6,.05,;10.08,-.35,;11.17,.74,;6.02,-.64,;4.93,-1.73,;4.53,-3.22,;6.02,-2.82,;3.44,-1.33,;3.04,.16,;1.56,.56,;.47,-.53,;-1.02,-.13,;-1.93,1.11,;-3.39,.64,;-3.39,-.9,;-1.93,-1.38,;-1.53,-2.87,;-2.62,-3.96,;-4.1,-3.56,;-5.19,-4.65,;-4.79,-6.13,;-3.31,-6.53,;-2.22,-5.44,;-4.48,1.73,;-4.08,3.21,;-5.97,1.33,;-7.06,2.42,;-8.6,2.42,;-8.6,3.96,;-7.06,3.96,;-9.68,5.04,;-11.17,4.65,;-9.29,6.53,;.87,-2.02,;-.22,-3.11,;.18,-4.6,;1.66,-4.99,;2.75,-3.91,;2.35,-2.42,)|
Structure:
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