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Literature summary for 2.7.11.22 extracted from

  • VanderWel, S.N.; Harvey, P.J.; McNamara, D.J.; Repine, J.T.; Keller, P.R.; Quin, J.3rd.; Booth, R.J.; Elliott, W.L.; Dobrusin, E.M.; Fry, D.W.; Toogood, P.L.
    Pyrido[2,3-d]pyrimidin-7-ones as specific inhibitors of cyclin-dependent kinase 4 (2005), J. Med. Chem., 48, 2371-2387.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(3-chloro-4-piperazin-1-yl-phenylamino)-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
2-[4-(4-acetyl-piperazin-1-yl)-phenylamino]-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido-[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carbaldehyde
-
Homo sapiens
4-[4-(8-cyclopentyl-5-methyl-7-oxo-7,8-dihydro-pyrido-[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester
-
Homo sapiens
4-[4-(8-cyclopentyl-7-oxo-5-trifluoromethyl-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino)-phenyl]-piperazine-1-carboxylic acid tert-butyl ester
-
Homo sapiens
6-acetyl-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
6-bromo-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
6-chloro-8-cyclopentyl-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-(1-ethyl-propyl)-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-(4-morpholin-4-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-(4-piperazin-1-yl-phenylamino)-5-trifluoromethyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-(4-piperazin-1-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-(4-piperidin-1-yl-phenylamino)-8Hpyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-(4-[1,4]diazepan-1-yl-phenylamino)-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-[4-(3,3-dimethyl-piperazin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-[4-(3,5-dimethyl-piperazin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-[4-(3-hydroxy-pyrrolidin-1-yl)-phenylamino]-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-2-{4-[4-(3-hydroxy-propyl)-piperidin-1-yl]-phenylamino}-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5,6-dimethyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5-ethyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5-methyl-2-(4-morpholin-4-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5-methyl-2-(4-piperidin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5-methyl-2-[4-(4-methyl-piperazin-1-yl)-phenylamino]-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid
-
Homo sapiens
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid ethyl ester
-
Homo sapiens
8-cyclopentyl-5-methyl-7-oxo-2-(4-piperazin-1-yl-phenylamino)-7,8-dihydro-pyrido[2,3-d]pyrimidine-6-carboxylic acid methyl ester
-
Homo sapiens
8-cyclopentyl-6-ethyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-6-fluoro-5-methyl-2-(4-piperazin-1-ylphenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-cyclopentyl-6-iodo-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
8-isopropyl-5-methyl-2-(4-piperazin-1-yl-phenylamino)-8H-pyrido[2,3-d]pyrimidin-7-one
-
Homo sapiens
butyrolactone-1
-
Homo sapiens
flavopiridol
-
Homo sapiens
additional information IC50 values of pyrido[2,3-d]pyrimidin-7-one inhibitors on Cdk4/cyclin D1, Cdk1/cyclin B, Cdk2/cyclinA, and Cdk2/cyclin E, overview, antiproliferating activity of pyrido[2,3-d]pyrimidin-7-one inhibitors on MDA-MB-435 cells, overview Homo sapiens
Olomoucine
-
Homo sapiens
purvalanol A
-
Homo sapiens
roscovitine
-
Homo sapiens
UCN-01
-
Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
breast carcinoma cell
-
Homo sapiens
-
MDA-MB-435 cell breast carcinoma cell line Homo sapiens
-

Synonyms

Synonyms Comment Organism
CDK2
-
Homo sapiens
CDK4
-
Homo sapiens
cyclin-dependent kinase 2
-
Homo sapiens
cyclin-dependent kinase 4
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
25
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens
cyclin A regulatory subunit of Cdk2 Homo sapiens
cyclin D1 regulatory subunit of Cdk2 Homo sapiens
cyclin E regulatory subunit of Cdk2 Homo sapiens