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Target
Nuclear receptor ROR-gamma
Ligand
BDBM310157
Substrate
n/a
Meas. Tech.
TR-FRET Assay Protocol II
EC50
13.0±n/a nM
Citation
 Aicher, TD; Barr, KJ; Lapointe, BT; Simov, V; Stein, KA; Thomas, WD; Toogood, PL; Van Huis, CA; White, CM Tetrahydronaphthyridine and related bicyclic compounds for inhibition of RORγ activity and the treatment of disease US Patent  US9657033 Publication Date 5/23/2017 
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:
BDBM310157
Synonyms:
N-[7-amino-5-(toluene-3-sulfonyl)-5,6,7,8-tetrahydro-9-oxa-1,5-diaza-benzocyclohepten-3-yl]-2,2,2-trifluoro-acetamide | US10377768, Compound 71 | US9657033, Compound 71
Type:
Small organic molecule
Emp. Form.:
C17H17F3N4O4S
Mol. Mass.:
430.401
SMILES:
Cc1cccc(c1)S(=O)(=O)N1CC(N)COc2ncc(NC(=O)C(F)(F)F)cc12
Structure:
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