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Target
Nuclear receptor ROR-gamma
Ligand
BDBM310087
Substrate
n/a
Meas. Tech.
TR-FRET Assay Protocol II
EC50
25.0±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:
BDBM310087
Synonyms:
2-chloro-6-fluoro-N-[1-(3-trifluoromethylbenzenesulfonyl)-1H-pyrazolo[4,3-b]pyridin-6-yl]benzamide | US10377768, Compound 1 | US9657033, Compound 1
Type:
Small organic molecule
Emp. Form.:
C20H11ClF4N4O3S
Mol. Mass.:
498.838
SMILES:
Fc1cccc(Cl)c1C(=O)Nc1cnc2cnn(c2c1)S(=O)(=O)c1cccc(c1)C(F)(F)F
Structure:
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