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Literature summary for 2.7.10.2 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
Search for more literature for 2.7.10.2

Application

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Homo sapiens P12931
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
Abl tyrosine kinase
-
 Homo sapiens
Src tyrosine kinase
-
 Homo sapiens

IC50 Value

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