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Target
Nuclear receptor ROR-gamma
Ligand
BDBM310126
Substrate
n/a
Meas. Tech.
TR-FRET Assay Protocol II
EC50
18.0±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:
BDBM310126
Synonyms:
(R)-N-(7-amino-5-(m-tolylsulfonyl)-5,6,7,8-tetrahydro-1,5-naphthyridin-3-yl)-2,6-dichlorobenzamide trifluoroacetic acid salt | US10377768, Compound 40 | US9657033, Compound 40
Type:
Small organic molecule
Emp. Form.:
C22H20Cl2N4O3S
Mol. Mass.:
491.39
SMILES:
Cc1cccc(c1)S(=O)(=O)N1C[C@H](N)Cc2ncc(NC(=O)c3c(Cl)cccc3Cl)cc12 |r|
Structure:
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