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Target
Nuclear receptor ROR-gamma
Ligand
BDBM292761
Substrate
n/a
Meas. Tech.
transient transactivation assay
IC50
<100±n/a nM
Citation
 Argiriadi, MA; Breinlinger, EC; Cusack, KP; Hobson, AD; Potin, D; Barth, M; Amaudrut, J; Poupardin, O; Mounier, L; Kort, ME Nuclear receptor modulators US Patent  US10106501 Publication Date 10/23/2018 
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:
BDBM292761
Synonyms:
(2,4-dichloro-3-((3,7-dimethyl-5-(trifluoromethyl)-1H-indazol-1-yl)methyl)phenyl)(4-(oxetan-3-yl)piperidin-1-yl)methanone | US10106501, Example DD-1
Type:
Small organic molecule
Emp. Form.:
C26H26Cl2F3N3O2
Mol. Mass.:
540.405
SMILES:
Cc1nn(Cc2c(Cl)ccc(C(=O)N3CCC(CC3)C3COC3)c2Cl)c2c(C)cc(cc12)C(F)(F)F
Structure:
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