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Assay Detail

CHEMBL992479

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Binding
Inhibition of CDK4
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cyclin-dependent kinase 4 (CHEMBL331)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Anderson M, Andrews DM, Barker AJ, Brassington CA, Breed J, Byth KF, Culshaw JD, Finlay MR, Fisher E, McMiken HH, Green CP, Heaton DW, Nash IA, Newcombe NJ, Oakes SE, Pauptit RA, Roberts A, Stanway JJ, Thomas AP, Tucker JA, Walker M, Weir HM.
Bioorg Med Chem Lett (2008) 18 : 5487 -5492
PubMed 18815031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.24 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL457887 1 6.85
CHEMBL478409 1 6.70
CHEMBL457888 1 6.68
CHEMBL488436 AZD-5438 1.0 1 6.35
CHEMBL515854 1 6.31
CHEMBL515839 1 6.28
CHEMBL485618 1 5.89
CHEMBL457979 1 5.82
CHEMBL520187 1 5.25
CHEMBL483590 1 -
CHEMBL458547 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL457887 IC50 = 140.0 nM 6.85
CHEMBL478409 IC50 = 200.0 nM 6.70
CHEMBL457888 IC50 = 210.0 nM 6.68
CHEMBL488436 AZD-5438 IC50 = 450.0 nM 6.35
CHEMBL515854 IC50 = 490.0 nM 6.31
CHEMBL515839 IC50 = 530.0 nM 6.28
CHEMBL485618 IC50 = 1300.0 nM 5.89
CHEMBL457979 IC50 = 1500.0 nM 5.82
CHEMBL520187 IC50 = 5600.0 nM 5.25
CHEMBL483590 IC50 > 9000.0 nM -
CHEMBL458547 IC50 > 8600.0 nM -