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Literature summary extracted from

  • Bardelle, C.; Cross, D.; Davenport, S.; Kettle, J.G.; Ko, E.J.; Leach, A.G.; Mortlock, A.; Read, J.; Roberts, N.J.; Robins, P.; Williams, E.J.
    Inhibitors of the tyrosine kinase EphB4. Part 1: Structure-based design and optimization of a series of 2,4-bis-anilinopyrimidines (2008), Bioorg. Med. Chem. Lett., 18, 2776-2780.
    View publication on PubMed

Application

EC Number Application Comment Organism
2.7.10.2 medicine over-expression of Eph receptors on cancer cells is able to confer tumourigenic phenotypes such as proliferation and invasion, EphB4 could be a target for therapeutic intervention Mammalia

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.10.2 2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
 Mammalia
2.7.10.2 2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
 Mammalia
2.7.10.2 3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
 Mammalia
2.7.10.2 3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
 Mammalia
2.7.10.2 4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
-
 Mammalia
2.7.10.2 4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
-
 Mammalia
2.7.10.2 N-(5-chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine
-
 Mammalia
2.7.10.2 N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)-1,3,5-triazine-2,4-diamine
-
 Mammalia
2.7.10.2 N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)pyrimidine-4,6-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-chlorophenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-fluorophenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methoxyphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methylphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-chlorophenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-fluorophenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methoxyphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methylphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-chlorophenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-fluorophenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methoxyphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methylphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-phenylpyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[2-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[3-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
 Mammalia
2.7.10.2 N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[4-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
-
 Mammalia

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 Mammalia
-
 ADP + [protein]-L-tyrosine phosphate
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.7.10.2 Mammalia
-
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.7.10.2 EphB4
-
 Mammalia

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.10.2 0.00004
-
-
 Mammalia 3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
2.7.10.2 0.00009
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[3-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
2.7.10.2 0.00024
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.0003
-
-
 Mammalia 4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
2.7.10.2 0.00035
-
-
 Mammalia N-(5-chloro-1,3-benzodioxol-4-yl)-6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-amine
2.7.10.2 0.00046
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methylphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00055
-
-
 Mammalia 3-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
2.7.10.2 0.00058
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00063
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[4-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine
2.7.10.2 0.00064
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-methoxyphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.001
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00115
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-fluorophenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00125
-
-
 Mammalia 4-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
2.7.10.2 0.00133
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(3-chlorophenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00155
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-phenylpyrimidine-2,4-diamine
2.7.10.2 0.0016
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methylphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00194
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-methoxyphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.0023
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-fluorophenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00254
-
-
 Mammalia N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)pyrimidine-4,6-diamine
2.7.10.2 0.00296
-
-
 Mammalia N-(5-chloro-1,3-benzodioxol-4-yl)-N'-(3,4,5-trimethoxyphenyl)-1,3,5-triazine-2,4-diamine
2.7.10.2 0.00388
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methoxyphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.005
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-fluorophenyl)pyrimidine-2,4-diamine
2.7.10.2 0.006
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(4-chlorophenyl)pyrimidine-2,4-diamine
2.7.10.2 0.00785
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-morpholin-4-ylphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.01132
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-chlorophenyl)pyrimidine-2,4-diamine
2.7.10.2 0.01396
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-(2-methylphenyl)pyrimidine-2,4-diamine
2.7.10.2 0.02049
-
-
 Mammalia 2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzonitrile
2.7.10.2 0.0355
-
-
 Mammalia 2-([4-[(5-chloro-1,3-benzodioxol-4-yl)amino]pyrimidin-2-yl]amino)benzenesulfonamide
2.7.10.2 0.041
-
-
 Mammalia N4-(5-chloro-1,3-benzodioxol-4-yl)-N2-[2-(methylsulfonyl)phenyl]pyrimidine-2,4-diamine