Drug General Information
Drug ID
D04QAE
Former ID
DIB012132
Drug Name
CXCR3 antagonists
Synonyms
CXCR3 antagonists (autoimmune disease); CXCR3 antagonists (autoimmune disease), Amgen
Indication Autoimmune diabetes [ICD10:E08-E13] Investigative [552115]
Company
Amgen Inc
Structure
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2D MOL

3D MOL

Canonical SMILES
O=S1(=O)CCC(CN([C@@H](c2nc3ncccc3c(=O)n2c2ccc(cc2)Cl)C)<br />C(=O)Cc2ccc(C(F)(F)F)c(c2)F)CC1
Target and Pathway
Target(s) C-X-C chemokine receptor type 3 Target Info Antagonist [543922]
KEGG Pathway Cytokine-cytokine receptor interaction
Chemokine signaling pathway
NetPath Pathway IL2 Signaling Pathway
PANTHER Pathway Inflammation mediated by chemokine and cytokine signaling pathway
Pathway Interaction Database CXCR3-mediated signaling events
Reactome Chemokine receptors bind chemokines
G alpha (i) signalling events
WikiPathways GPCRs, Class A Rhodopsin-like
Peptide GPCRs
GPCR ligand binding
GPCR downstream signaling
GPCRs, Other
References
Ref 552115Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme. Drug Metab Dispos. 2012 Jul;40(7):1429-40
Ref 543922(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 70).

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