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Target
Nuclear receptor ROR-gamma [238-497]
Ligand
BDBM175892
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:
Human
Description:
Human RORgamma ligand-binding domain.
Residue:
260
Sequence:
HPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAA
  
Inhibitor
Name:
BDBM175892
Synonyms:
US9688684, Compound 89: 7-Benzyl-8-(3-fluoro-phenyl)-5,6,7,8-tetrahydro-tetrazolo[1,5-a]pyrazine
Type:
Small organic molecule
Emp. Form.:
C17H16FN5
Mol. Mass.:
309.3408
SMILES:
Fc1cccc(c1)C1N(Cc2ccccc2)CCn2nnnc12
Structure:
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