Reaction Details Report a problem with these data
Target
Nuclear receptor ROR-gamma
Ligand
BDBM310122
Substrate
n/a
Meas. Tech.
TR-FRET Assay Protocol II
EC50
202±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
More Info.:
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:
BDBM310122
Synonyms:
2,6-difluoro-N-(5-(4-fluorobenzenesulfonyl)-5,6,7,8-tetrahydro-[1,5]naphthyridin-3-yl)benzamide | US10377768, Compound 36 | US9657033, Compound 36
Type:
Small organic molecule
Emp. Form.:
C21H16F3N3O3S
Mol. Mass.:
447.43
SMILES:
Fc1ccc(cc1)S(=O)(=O)N1CCCc2ncc(NC(=O)c3c(F)cccc3F)cc12