| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T25315 | ||||
| Target Name | C-X-C chemokine receptor type 3 (CXCR3) | ||||
| Type of Target |
Preclinical |
||||
| Drug Potency against Target | T487 | Drug Info | IC50 = 13.27 nM | ||
| T487 | Drug Info | IC50 = 240 nM | [1] | ||
| Action against Disease Model | T487 | Drug Info | Treatment of osteosarcoma cells in vitro with AMG487, ananomolar CXCR3 antagonist, led to decreased migration, decreased matrix metalloproteinase activity, decreased proliferation/survival and increased caspase-independent death. | [2] | |
| References | |||||
| REF 1 | Optimization of a series of quinazolinone-derived antagonists of CXCR3. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5114-8. | ||||
| REF 2 | Synthesis and structure-activity relationships of 3H-quinazolin-4-ones and 3H-pyrido[2,3-d]pyrimidin-4-ones as CXCR3 receptor antagonists. Arch Pharm (Weinheim). 2007 Jun;340(6):281-91. | ||||
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