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Target
Nuclear receptor ROR-gamma
Ligand
BDBM220233
Substrate
n/a
Meas. Tech.
ChEMBL_1841426 (CHEMBL4341725)
IC50
3.9±n/a nM
Citation
 Tanis, VM; Venkatesan, H; Cummings, MD; Albers, M; Kent Barbay, J; Herman, K; Kummer, DA; Milligan, C; Nelen, MI; Nishimura, R; Schlueter, T; Scott, B; Spurlino, J; Wolin, R; Woods, C; Xue, X; Edwards, JP; Fourie, AM; Leonard, K 3-Substituted Quinolines as ROR?t Inverse Agonists. Bioorg Med Chem Lett 29:1463-1470 (2019) [PubMed]  Article 
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:
BDBM220233
Synonyms:
US9290476, 77A | US9290476, 77B | US9290476, 77C
Type:
Small organic molecule
Emp. Form.:
C29H25ClF3N5O2
Mol. Mass.:
567.989
SMILES:
COc1nc2ccc(cc2c(Cl)c1Cc1ccc(cc1)C(F)(F)F)C(O)(c1cnnn1C)c1ccc(C)nc1C
Structure:
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