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Assay Detail

CHEMBL5229241

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Toxicity
Inhibition of human Cdk2/Cyclin A using Myelin basic protein as substrate by ATP competitive assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Toxicity
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

Engineering Selectivity for Reduced Toxicity of Bacterial Kinase Inhibitors Using Structure-Guided Medicinal Chemistry.
Wlodarchak N, Feltenberger JB, Ye Z, Beczkiewicz J, Procknow R, Yan G, King TM, Golden JE, Striker R.
ACS Med Chem Lett (2021) 12 : 228 -235
PubMed 35035774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.19 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5273566 1 6.75
CHEMBL468963 GW779439X 1 5.85
CHEMBL5316225 1 5.34
CHEMBL5283441 1 5.14
CHEMBL5284844 1 5.14
CHEMBL5266831 1 5.03
CHEMBL5277619 1 5.00
CHEMBL5280561 1 4.92
CHEMBL5277737 1 4.89
CHEMBL5285809 1 4.62
CHEMBL5266857 1 4.41
CHEMBL5277580 1 -
CHEMBL5282194 1 -
CHEMBL5280226 1 -
CHEMBL5283041 1 -
CHEMBL5282708 1 -
CHEMBL5286085 1 -
CHEMBL5283475 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5273566 IC50 = 180.0 nM 6.75
CHEMBL468963 GW779439X IC50 = 1400.0 nM 5.85
CHEMBL5316225 IC50 = 4600.0 nM 5.34
CHEMBL5283441 IC50 = 7200.0 nM 5.14
CHEMBL5284844 IC50 = 7300.0 nM 5.14
CHEMBL5266831 IC50 = 9300.0 nM 5.03
CHEMBL5277619 IC50 = 10000.0 nM 5.00
CHEMBL5280561 IC50 = 12000.0 nM 4.92
CHEMBL5277737 IC50 = 13000.0 nM 4.89
CHEMBL5285809 IC50 = 24000.0 nM 4.62
CHEMBL5266857 IC50 = 39000.0 nM 4.41
CHEMBL5277580 IC50 > 40000.0 nM -
CHEMBL5282194 IC50 > 40000.0 nM -
CHEMBL5280226 IC50 > 40000.0 nM -
CHEMBL5283041 IC50 > 40000.0 nM -
CHEMBL5282708 IC50 > 40000.0 nM -
CHEMBL5286085 IC50 > 40000.0 nM -
CHEMBL5283475 IC50 > 40000.0 nM -