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Assay Detail

CHEMBL660703

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

Binding
Inhibition of Cyclin-dependent kinase 2 cyclin A
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 2/cyclin A (CHEMBL2094128)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles.
Wood ER, Kuyper L, Petrov KG, Hunter RN, Harris PA, Lackey K.
Bioorg Med Chem Lett (2004) 14 : 953 -957
PubMed 15013000 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.65 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1276446 1 8.00
CHEMBL1794057 GW284408X 1 5.60
CHEMBL1794056 GW301789X 1 5.14
CHEMBL175321 1 5.10
CHEMBL1794058 GW278681X 1 5.10
CHEMBL176857 GW442130X 1 4.98
CHEMBL176544 1 -
CHEMBL1794059 GW275616X 1 -
CHEMBL369490 1 -
CHEMBL172179 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1276446 IC50 = 10.0 nM 8.00
CHEMBL1794057 GW284408X IC50 = 2500.0 nM 5.60
CHEMBL1794056 GW301789X IC50 = 7200.0 nM 5.14
CHEMBL175321 IC50 = 8000.0 nM 5.10
CHEMBL1794058 GW278681X IC50 = 8000.0 nM 5.10
CHEMBL176857 GW442130X IC50 = 10400.0 nM 4.98
CHEMBL176544 IC50 > 7000.0 nM -
CHEMBL1794059 GW275616X IC50 > 10000.0 nM -
CHEMBL369490 IC50 > 50000.0 nM -
CHEMBL172179 IC50 > 6000.0 nM -