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Literature summary for 2.7.10.2 extracted from

  • Farmer, L.J.; Bemis, G.; Britt, S.D.; Cochran, J.; Connors, M.; Harrington, E.M.; Hoock, T.; Markland, W.; Nanthakumar, S.; Taslimi, P.; Haar, E.T.; Wang, J.; Zhaveri, D.; Salituro, F.G.
    Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK) (2008), Bioorg. Med. Chem. Lett., 18, 6231-6235.
    View publication on PubMed

Application

Application Comment Organism
medicine SYK is a good target for therapeutic intervention in allergic diseases such as asthma, roles in the development of cancer are reported Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
Homo sapiens
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
Homo sapiens
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
Homo sapiens
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
Homo sapiens
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
Homo sapiens
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
Homo sapiens
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
Homo sapiens
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
Homo sapiens
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
Homo sapiens
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
Homo sapiens
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
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
-
-
-

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
Spleen tyrosine kinase
-
Homo sapiens
Syk
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000004
-
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-5-yl)methanol
-
Homo sapiens
0.000008
-
N-(3,5-dimethylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.000009
-
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1S)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
Homo sapiens
0.00001
-
(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-1,3-thiazol-4-yl)methanol
-
Homo sapiens
0.00001
-
[2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
Homo sapiens
0.000014
-
N-(3,5-dimethoxyphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.000022
-
2-[4-methyl-2-(2-[[3-methyl-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-5-yl]ethanol
-
Homo sapiens
0.000023
-
N-(3,5-dimethylphenyl)-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.000023
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(5-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.000026
-
3-[3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenoxy]propan-1-ol
-
Homo sapiens
0.000028
-
N-[3-methoxy-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.000032
-
2-(2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-4-methyl-1,3-thiazol-5-yl)ethanol
-
Homo sapiens
0.000033
-
[2-(2-[[3-methoxy-5-(trifluoromethyl)phenyl]amino]pyrimidin-4-yl)-1,3-thiazol-4-yl]methanol
-
Homo sapiens
0.000044
-
3-[[4-(1,3-thiazol-2-yl)pyrimidin-2-yl]amino]-5-(trifluoromethyl)phenol
-
Homo sapiens
0.00005
-
3-([4-[4-(hydroxymethyl)-1,3-thiazol-2-yl]pyrimidin-2-yl]amino)-5-(trifluoromethyl)phenol
-
Homo sapiens
0.000056
-
N-(3,5-dimethylphenyl)-4-(4-methyl-1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.000082
-
N-(3-methylphenyl)-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.00011
-
N-[3-methyl-5-(trifluoromethyl)phenyl]-4-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.00021
-
2-[2-[(3,5-dimethylphenyl)amino]pyrimidin-4-yl]-N-[(1R)-2-hydroxy-1-methylethyl]-4-methyl-1,3-thiazole-5-carboxamide
-
Homo sapiens
0.00063
-
N-(3-phenoxyphenyl)-4-(thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens
0.001817
-
4-methyl-N-(3-methylphenyl)-6-(1,3-thiazol-2-yl)pyrimidin-2-amine
-
Homo sapiens