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Target
Nuclear receptor ROR-gamma [258-518,Y502F]
Ligand
BDBM221259
Substrate
n/a
Meas. Tech.
RORγt Reporter Assay
IC50
280±n/a nM
Citation
 Leonard, KA; Barbay, K; Edwards, JP; Kreutter, KD; Kummer, DA; Maharoof, U; Nishimura, R; Urbanski, M; Venkatesan, H; Wang, A; Wolin, RL; Woods, CR; Fourie, A; Xue, X Heteroaryl linked quinolinyl modulators of RORγt US Patent  US9303015 Publication Date 4/5/2016 
Target
Name:
Nuclear receptor ROR-gamma [258-518,Y502F]
Synonyms:
NR1F3 | RORC | RORG | RORG_HUMAN | RZRG | Retinoic acid-related nuclear receptor gamma t (RORgammat)
Type:
Enzyme
Mol. Mass.:
30130.98
Organism:
Homo sapiens (Human)
Description:
Artificial LBD sequence mutated AF2 domain (Seq No: 9)
Residue:
261
Sequence:
STPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAAFPPLFKELFSTETESPVGLSK
  
Inhibitor
Name:
BDBM221259
Synonyms:
US9303015, 33
Type:
Small organic molecule
Emp. Form.:
C31H24ClF3N6O2
Mol. Mass.:
605.009
SMILES:
Cn1cncc1C(O)(c1ccc(nc1)C(F)(F)F)c1ccc2nc(N3CCCC3)c(Oc3ccc(cc3)C#N)c(Cl)c2c1
Structure:
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