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Assay Detail

CHEMBL4004960

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

Binding
Inhibition of recombinant human full-length C-terminal His6-tagged Cdk7/recombinant human full-length Cyclin H expressed in baculovirus infected Sf21 insect cells
7
Total Activities
7
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 7/ cyclin H (CHEMBL2111288)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Cyclin-Dependent Kinase (CDK) Inhibitors: Structure-Activity Relationships and Insights into the CDK-2 Selectivity of 6-Substituted 2-Arylaminopurines.
Coxon CR, Anscombe E, Harnor SJ, Martin MP, Carbain B, Golding BT, Hardcastle IR, Harlow LK, Korolchuk S, Matheson CJ, Newell DR, Noble ME, Sivaprakasam M, Tudhope SJ, Turner DM, Wang LZ, Wedge SR, Wong C, Griffin RJ, Endicott JA, Cano C.
J Med Chem (2017) 60 : 1746 -1767
PubMed 28005359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.13 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4103249 1 5.55
CHEMBL4062554 1 5.39
CHEMBL319467 1 5.36
CHEMBL4105278 1 5.17
CHEMBL4092981 1 5.17
CHEMBL4085238 1 5.16
CHEMBL4073211 1 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4103249 IC50 = 2800.0 nM 5.55
CHEMBL4062554 IC50 = 4100.0 nM 5.39
CHEMBL319467 IC50 = 4400.0 nM 5.36
CHEMBL4105278 IC50 = 6800.0 nM 5.17
CHEMBL4092981 IC50 = 6800.0 nM 5.17
CHEMBL4085238 IC50 = 7000.0 nM 5.16
CHEMBL4073211 IC50 = 75000.0 nM 4.12