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Target
Nuclear receptor ROR-gamma
Ligand
BDBM383417
Substrate
n/a
Meas. Tech.
In Vitro RORc Ligand Binding Assay
IC50
2.60±n/a nM
Citation
 Fauber, B; Crawford, JJ; Bronner, SM; van Niel, MB; Cridland, A; Gancia, E; Hurley, C; Killen, J; Ward, S Pyridazine derivatives as RORc modulators US Patent  US10280144 Publication Date 5/7/2019 
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:
BDBM383417
Synonyms:
1-(2,4-difluorophenyl)-N- (((5R,8S)-3-(2,6-difluorophenyl)- 9,9-dimethyl-5,6,7,8-tetrahydro- 5,8-methanocinnolin-8- yl)methyl)-N- ethylmethanesulfonamide | US10280144, Compound 133
Type:
Small organic molecule
Emp. Form.:
C27H27F4N3O2S
Mol. Mass.:
533.581
SMILES:
CCN(C[C@@]12CC[C@@H](c3cc(nnc13)-c1c(F)cccc1F)C2(C)C)S(=O)(=O)Cc1ccc(F)cc1F |r|
Structure:
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