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Target
Nuclear receptor ROR-gamma
Ligand
BDBM310121
Substrate
n/a
Meas. Tech.
RORgamma-Ligand Binding Domain TR-FRET Assay Protocol II
EC50
7.00±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 RORgamma activity and the treatment of disease US Patent  US10377768 Publication Date 8/13/2019 
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:
BDBM310121
Synonyms:
(S)-2,6-dichloro-N-((3-cyclopropylphenyl)sulfonyl)-3-methyl-2,3-dihydro[2,3,b][1,4]oxazin-yl)benzamide | US10377768, Compound 35 | US9657033, Compound 35
Type:
Small organic molecule
Emp. Form.:
C24H21Cl2N3O4S
Mol. Mass.:
518.412
SMILES:
C[C@H]1CN(c2cc(NC(=O)c3c(Cl)cccc3Cl)cnc2O1)S(=O)(=O)c1cccc(c1)C1CC1 |r|
Structure:
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