Synonyms: AMG 487 | AMG-487 | compound 47 [PMID: 17448658]
Compound class:
Synthetic organic
Comment: AMG487 is a small molecule CXCR3 antagonist [2-3]. It was investigated for activity as a tumour metastasis inhibitor, based on evidence that CXCR3 expressed on tumour cells directly promotes metastasis [4].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Bakheet SA, Ansari MA, Nadeem A, Attia SM, Alhoshani AR, Gul G, Al-Qahtani QH, Albekairi NA, Ibrahim KE, Ahmad SF. (2019)
CXCR3 antagonist AMG487 suppresses rheumatoid arthritis pathogenesis and progression by shifting the Th17/Treg cell balance. Cell Signal, 64: 109395. [PMID:31449849] |
2. Jiao H, Pang B, Chiang YC, Chen Q, Pan Q, Ren R, Hu H. (2023)
Structure basis for the modulation of CXC chemokine receptor 3 by antagonist AMG487. Cell Discov, 9 (1): 119. [PMID:38012179] |
3. Johnson M, Li AR, Liu J, Fu Z, Zhu L, Miao S, Wang X, Xu Q, Huang A, Marcus A et al.. (2007)
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett, 17 (12): 3339-43. [PMID:17448658] |
4. Walser TC, Rifat S, Ma X, Kundu N, Ward C, Goloubeva O, Johnson MG, Medina JC, Collins TL, Fulton AM. (2006)
Antagonism of CXCR3 inhibits lung metastasis in a murine model of metastatic breast cancer. Cancer Res, 66 (15): 7701-7. [PMID:16885372] |