Reaction Details Report a problem with these data
Target
Nuclear receptor ROR-gamma [238-497]
Ligand
BDBM175864
Substrate
n/a
Meas. Tech.
TR-FRET Assay
pH
6.8±n/a
IC50
500±n/a nM
Comments
extracted
Citation
 Finsinger, D; Wucherer-Plietker, M; Blume, B Substituted tetrazolo[1,5-a]pyrazines as ROR-gamma inhibitors US Patent  US9688684 Publication Date 6/27/2017 
Target
Name:
Nuclear receptor ROR-gamma [238-497]
Synonyms:
NR1F3 | RORC | RORG | RORG_HUMAN | RZRG | Retinoid-related orphan receptor gamma (RORgamma-LBD)
Type:
Protein
Mol. Mass.:
29835.99
Organism:
Homo sapiens (Human)
Description:
Human RORgamma ligand-binding domain.
Residue:
260
Sequence:
HPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAA
  
Inhibitor
Name:
BDBM175864
Synonyms:
US9688684, Compound 61: 8-(3-Isopropyl-1-phenyl-1H-pyrazol-4-yl)-7-thiophen-2-ylmethyl-5,6,7,8-tetrahydro-tetrazolo[1,5-a]pyrazine
Type:
Small organic molecule
Emp. Form.:
C21H23N7S
Mol. Mass.:
405.519
SMILES:
CC(C)c1nn(cc1C1N(Cc2cccs2)CCn2nnnc12)-c1ccccc1
Structure:
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