Target Validation Information
TTD ID T48069
Target Name Insulin-like growth factor I receptor (IGF1R)
Type of Target
Drug Potency against Target AEW-541 Drug Info IC50 = 86 nM [5]
4-((1H-indazol-6-ylamino)methyl)benzene-1,2-diol Drug Info IC50 = 1500 nM [1]
4-((naphthalen-2-ylamino)methyl)benzene-1,2-diol Drug Info IC50 = 4500 nM [1]
BMS-536924 Drug Info IC50 = 100 nM [3]
BMS-695735 Drug Info IC50 = 34 nM [2]
OSI-906 Drug Info IC50 = 18 nM [4]
REF 1 ATP non-competitive IGF-1 receptor kinase inhibitors as lead anti-neoplastic and anti-papilloma agents. Eur J Pharmacol. 2007 May 7;562(1-2):1-11.
REF 2 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)py... J Med Chem. 2008 Oct 9;51(19):5897-900.
REF 3 SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1744-8.
REF 4 Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family... Bioorg Med Chem Lett. 2010 Apr 15;20(8):2452-5.
REF 5 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.

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