Target
Nuclear receptor ROR-gamma
Ligand
BDBM385538
Substrate
n/a
Meas. Tech.
Biological Assay for RORgammaT Activity
IC50
20.0±n/a nM
Citation
 Lapointe, BTFuller, PHGunaydin, HLiu, KScott, METrotter, BWZhang, H Substituted indazole compounds as RORgammaT inhibitors and uses thereof US Patent  US10287272 Publication Date 5/14/2019 
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:
BDBM385538
Synonyms:
US10287272, Example 19A
Type:
Small organic molecule
Emp. Form.:
C33H40ClF3N4O5
Mol. Mass.:
665.143
SMILES:
COC1CN(C1)C(=O)C1CCc2c(nn(C(=O)c3c(Cl)cccc3C3(CC3)C(F)(F)F)c2C1)N1CCC(CC1)C(=O)OC(C)(C)C
Structure:
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