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Literature summary for 2.7.10.1 extracted from

  • Ducray, R.; Jones, C.; Jung, F.; Simpson, I.; Curwen, J.; Pass, M.
    Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: Optimization of the aniline (2011), Bioorg. Med. Chem. Lett., 21, 4702-4704.
    View publication on PubMed
Search for more literature for 2.7.10.1

Inhibitors

Inhibitors Comment Organism Structure
2-[7-(4-[[4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-3-methoxyphenyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethanol compound shows good IGF-1R inhibitory activity in a cellular assay and a high free fraction in human plasma. However this compound shows a higher affinity for the hERG channel Homo sapiens
4-(imidazo[1,2-a]pyridin-3-yl)-N-[2-methoxyphenyl-4-(4-piperidinyl)]pyrimidin-2-amine
-
 Homo sapiens
4-(imidazo[2-methoxy-4-(9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl)phenyl])pyrimidin-2-amine
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
IGF-1R
-
 Homo sapiens
Insulin-like Growth Factor-1 receptor tyrosine kinase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-(imidazo[2-methoxy-4-(9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl)phenyl])pyrimidin-2-amine
0.000004
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-[7-(4-[[4-(imidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl]amino]-3-methoxyphenyl)-9-oxa-3,7-diazabicyclo[3.3.1]non-3-yl]ethanol
0.000005
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 4-(imidazo[1,2-a]pyridin-3-yl)-N-[2-methoxyphenyl-4-(4-piperidinyl)]pyrimidin-2-amine