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Assay Detail

CHEMBL666101

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Binding
In vitro inhibition of Cyclin-dependent kinase 4 was determined.
17
Total Activities
17
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 4 (CHEMBL331)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.
Beattie JF, Breault GA, Ellston RP, Green S, Jewsbury PJ, Midgley CJ, Naven RT, Minshull CA, Pauptit RA, Tucker JA, Pease JE.
Bioorg Med Chem Lett (2003) 13 : 2955 -2960
PubMed 12941311 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.46 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101119 1 7.30
CHEMBL421583 1 7.00
CHEMBL317378 1 6.30
CHEMBL100945 1 6.10
CHEMBL322640 1 6.00
CHEMBL316887 1 5.70
CHEMBL100811 1 5.40
CHEMBL316809 1 5.30
CHEMBL101557 1 5.22
CHEMBL418793 1 5.10
CHEMBL99647 1 5.10
CHEMBL101558 1 5.05
CHEMBL317281 1 4.82
CHEMBL99699 1 4.75
CHEMBL101868 1 4.64
CHEMBL318485 1 4.57
CHEMBL318188 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101119 IC50 = 50.0 nM 7.30
CHEMBL421583 IC50 = 100.0 nM 7.00
CHEMBL317378 IC50 = 500.0 nM 6.30
CHEMBL100945 IC50 = 800.0 nM 6.10
CHEMBL322640 IC50 = 1000.0 nM 6.00
CHEMBL316887 IC50 = 2000.0 nM 5.70
CHEMBL100811 IC50 = 4000.0 nM 5.40
CHEMBL316809 IC50 = 5000.0 nM 5.30
CHEMBL101557 IC50 = 6000.0 nM 5.22
CHEMBL418793 IC50 = 8000.0 nM 5.10
CHEMBL99647 IC50 = 8000.0 nM 5.10
CHEMBL101558 IC50 = 9000.0 nM 5.05
CHEMBL317281 IC50 = 15000.0 nM 4.82
CHEMBL99699 IC50 = 18000.0 nM 4.75
CHEMBL101868 IC50 = 23000.0 nM 4.64
CHEMBL318485 IC50 = 27000.0 nM 4.57
CHEMBL318188 IC50 = 33000.0 nM 4.48