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Assay Detail

CHEMBL666141

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

Binding
Inhibition of Cyclin-dependent kinase 1 (CDK1) at 12.5 uM ATP
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cyclin-dependent kinase 1 (CHEMBL308)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of 2-arylamino-4-cyclohexylmethyl-5-nitroso-6-aminopyrimidine inhibitors of cyclin-dependent kinases 1 and 2.
Sayle KL, Bentley J, Boyle FT, Calvert AH, Cheng Y, Curtin NJ, Endicott JA, Golding BT, Hardcastle IR, Jewsbury P, Mesguiche V, Newell DR, Noble ME, Parsons RJ, Pratt DJ, Wang LZ, Griffin RJ.
Bioorg Med Chem Lett (2003) 13 : 3079 -3082
PubMed 12941338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.31 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318999 1 8.30
CHEMBL319467 1 8.02
CHEMBL101801 1 7.16
CHEMBL322568 1 6.66
CHEMBL102636 1 6.64
CHEMBL107530 1 6.10
CHEMBL303958 1 5.54
CHEMBL104467 1 5.28
CHEMBL269881 1 5.16
CHEMBL319709 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318999 IC50 = 5.0 nM 8.30
CHEMBL319467 IC50 = 9.5 nM 8.02
CHEMBL101801 IC50 = 70.0 nM 7.16
CHEMBL322568 IC50 = 220.0 nM 6.66
CHEMBL102636 IC50 = 230.0 nM 6.64
CHEMBL107530 IC50 = 800.0 nM 6.10
CHEMBL303958 IC50 = 2900.0 nM 5.54
CHEMBL104467 IC50 = 5300.0 nM 5.28
CHEMBL269881 IC50 = 7000.0 nM 5.16
CHEMBL319709 IC50 = 63000.0 nM 4.20