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Literature summary extracted from

  • Wang, Y.; Shakespeare, W.C.; Huang, W.S.; Sundaramoorthi, R.; Lentini, S.; Das, S.; Liu, S.; Banda, G.; Wen, D.; Zhu, X.; Xu, Q.; Keats, J.; Wang, F.; Wardwell, S.; Ning, Y.; Snodgrass, J.T.; Broudy, M.I.; Russian, K.; Dalgarno, D.; Clackson, T.; Sawyer, T.K.
    Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors (2008), Bioorg. Med. Chem. Lett., 18, 4907-4912.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.10.2 medicine aberrant Src kinase activity is associated with the invasive phenotype in both early and advanced solid tumors Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.2 2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 AP23464
-
 Homo sapiens
2.7.10.2 AZD0530
-
 Homo sapiens
2.7.10.2 bosutinib
-
 Homo sapiens
2.7.10.2 dasatinib
-
 Homo sapiens
2.7.10.2 N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
-
 Homo sapiens
2.7.10.2 PD166326
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.7.10.2 ATP + [protein]-L-tyrosine Homo sapiens
-
 ADP + [protein]-L-tyrosine phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.2 Homo sapiens
-
-
-
2.7.10.2 Homo sapiens P12931
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.7.10.2 ATP + [protein]-L-tyrosine
-
 Homo sapiens ADP + [protein]-L-tyrosine phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
2.7.10.2 Abl tyrosine kinase
-
 Homo sapiens
2.7.10.2 Src tyrosine kinase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.10.2 0.00000023
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
2.7.10.2 0.00000023
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens 3-(9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-6-[[4-(dimethylphosphoryl)phenyl]amino]-9H-purin-2-yl)propanenitrile
2.7.10.2 0.00000046
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylpiperidin-4-yl)-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
2.7.10.2 0.00000046
-
-
 Homo sapiens N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(5-methyl-1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
2.7.10.2 0.0000005
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(pyrrolidin-3-yloxy)-9H-purin-6-amine
2.7.10.2 0.00000089
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
2.7.10.2 0.000001
-
-
 Homo sapiens AP23464
2.7.10.2 0.00000129
-
-
 Homo sapiens 2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.00000143
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
2.7.10.2 0.00000157
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(2-methoxyethoxy)-9H-purin-6-amine
2.7.10.2 0.00000163
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1H-imidazol-1-yl)-9H-purin-6-amine
2.7.10.2 0.00000178
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
2.7.10.2 0.0000018
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-methoxy-9H-purin-6-amine
2.7.10.2 0.00000236
-
-
 Homo sapiens N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
2.7.10.2 0.00000277
-
-
 Homo sapiens 9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.00000302
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-morpholin-4-yl-9H-purin-6-amine
2.7.10.2 0.00000358
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.00000374
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
2.7.10.2 0.000004
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.00000556
-
-
 Homo sapiens 9-[(E)-2-(2-chloro-6-methylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.00000593
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
2.7.10.2 0.00000658
-
-
 Homo sapiens 9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
2.7.10.2 0.0000068
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(4-methylpiperazin-1-yl)-9H-purin-6-amine
2.7.10.2 0.00000732
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethoxy)-9H-purin-6-amine
2.7.10.2 0.00000831
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.0000158
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
2.7.10.2 0.0000167
-
-
 Homo sapiens N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
2.7.10.2 0.000017
-
-
 Homo sapiens N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indazol-4-yl)ethenyl]-9H-purin-6-amine
2.7.10.2 0.0000173
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.0000176
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N6-[4-(dimethylphosphoryl)phenyl]-N2,N2-dimethyl-9H-purine-2,6-diamine
2.7.10.2 0.0000195
-
-
 Homo sapiens 9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-2-pyrrolidin-1-yl-9H-purin-6-amine
2.7.10.2 0.0000318
-
-
 Homo sapiens N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
2.7.10.2 0.0000323
-
-
 Homo sapiens 2-cyclopentyl-9-[(E)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.0000543
-
-
 Homo sapiens 9-[(Z)-2-(2,6-dimethylphenyl)ethenyl]-N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9H-purin-6-amine
2.7.10.2 0.0000694
-
-
 Homo sapiens 9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.0000733
-
-
 Homo sapiens N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(E)-2-phenylethenyl]-9H-purin-6-amine
2.7.10.2 0.000126
-
-
 Homo sapiens 9-[(E)-2-(2-chlorophenyl)ethenyl]-N-[4-(dimethylphosphoryl)phenyl]-9H-purin-6-amine
2.7.10.2 0.000198
-
-
 Homo sapiens N-[4-(dimethylphosphoryl)phenyl]-9-[(E)-2-(1H-indol-4-yl)ethenyl]-9H-purin-6-amine
2.7.10.2 0.000376
-
-
 Homo sapiens N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine
2.7.10.2 0.000626
-
-
 Homo sapiens N-[4-(dipropylphosphoryl)phenyl]-2-(1-methylethyl)-9-[(Z)-2-phenylethenyl]-9H-purin-6-amine