| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T48069 | ||||
| Target Name | Insulin-like growth factor I receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | AEW-541 | Drug Info | IC50 = 86 nM | [552423] | |
| BMS-695735 | Drug Info | IC50 = 34 nM | [529668] | ||
| BMS-536924 | Drug Info | IC50 = 100 nM | [530722] | ||
| 4-((naphthalen-2-ylamino)methyl)benzene-1,2-diol | Drug Info | IC50 = 4500 nM | [528746] | ||
| 4-((1H-indazol-6-ylamino)methyl)benzene-1,2-diol | Drug Info | IC50 = 1500 nM | [528746] | ||
| OSI-906 | Drug Info | IC50 = 18 nM | [530811] | ||
| References | |||||
| Ref 552423 | In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer Cell. 2004 Mar;5(3):231-9. | ||||
| Ref 529668 | J Med Chem. 2008 Oct 9;51(19):5897-900. Epub 2008 Sep 3.Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity. | ||||
| Ref 530722 | Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8. Epub 2010 Jan 21.SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. | ||||
| Ref 528746 | Eur J Pharmacol. 2007 May 7;562(1-2):1-11. Epub 2007 Feb 3.ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents. | ||||
| Ref 528746 | Eur J Pharmacol. 2007 May 7;562(1-2):1-11. Epub 2007 Feb 3.ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents. | ||||
| Ref 530811 | Bioorg Med Chem Lett. 2010 Apr 15;20(8):2452-5. Epub 2010 Mar 7.Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.