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Literature summary for 2.7.1.153 extracted from

  • Chen, Z.; Venkatesan, A.M.; Dehnhardt, C.M.; Ayral-Kaloustian, S.; Brooijmans, N.; Mallon, R.; Feldberg, L.; Hollander, I.; Lucas, J.; Yu, K.; Kong, F.; Mansour, T.S.
    Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors (2010), J. Med. Chem., 53, 3169-3182.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
1-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]-3-[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]urea dual catalytic subunit alpha isoform/mTOR kinase inhibitor, demonstrates inhibition of tumor cell growth in vitro and in vivo and causes suppression of the pathway specific biomarkers in the human MDA-361 cell line Homo sapiens
N-[2-(dimethylamino)ethyl]-N-methyl-4-[([4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]carbamoyl)amino]benzamide dual catalytic subunit alpha isoform/mTOR kinase inhibitor, demonstrates inhibition of tumor cell growth in vitro and in vivo and causes suppression of the pathway specific biomarkers in the human MDA-361 cell line. Good in vivo efficacy in the MDA361 human breast tumor xenograft model Homo sapiens
[3-[4-morpholin-4-yl-7-(pyrrolidin-1-ylmethyl)-5H-pyrrolo-[3,2-d ]pyrimidin-2-yl]phenyl]methanol selective for catalytic subunit alpha isoform Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P42336 catalytic subunit alpha isoform
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IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000009
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[2-(dimethylamino)ethyl]-N-methyl-4-[([4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]carbamoyl)amino]benzamide
0.0000024
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 1-[4-[(4-methylpiperazin-1-yl)carbonyl]phenyl]-3-[4-[4-morpholin-4-yl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d ]pyrimidin-2-yl]phenyl]urea
0.000021
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens [3-[4-morpholin-4-yl-7-(pyrrolidin-1-ylmethyl)-5H-pyrrolo-[3,2-d ]pyrimidin-2-yl]phenyl]methanol