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Assay Detail

CHEMBL3708010

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Kinase Inhibition Assay: The compound of Example 39, 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one, was subjected to a kinase inhibition assay for the kinases. Compounds were tested in 5 dose IC50 mode with 10-fold serial dilution starting at 10 μM. Staurosporine, a known protein kinase inhibitor, was tested in 5-dose IC50 mode with 3-fold serial dilution starting at 20 μM. Reactions were carried out in 10 μM ATP. The results are shown in Table 5. The results show that the compound of Example 39 is a kinase inhibitor highly selective for the kinase Plk2.
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted pyrido[2,3-d]pyrimidin-7(8H)-ones and therapeutic uses thereof
(2014)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.62 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3683258 2 9.49
CHEMBL3702566 2 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3683258 IC50 = 0.32 nM 9.49
CHEMBL3683258 IC50 = 4.66 nM 8.33
CHEMBL3702566 IC50 = 8847.0 nM 5.05
CHEMBL3702566 IC50 > 10000.0 nM -