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Assay Detail

CHEMBL5684064

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

Binding
ATP competitive inhibition of recombinant human N-terminal GST-fused CDK4 (S4 to E303 residues)/cyclin D1 expressed in Sf9 insect cells using C-terminal Rb fragment as substrate measured after 50 mins in presence of varying levels of [33P]gamma-ATP by Michaelis-Menten equation based kinetic analysis
1
Total Activities
1
Compounds Tested
1
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine.
Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A.
Invest New Drugs (2014) 32 : 825 -837
PubMed 24919854 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.22 9.22

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_TERM EFO_TERM - cancer

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3301610 ABEMACICLIB 4.0 1 9.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3301610 ABEMACICLIB Ki = 0.6 nM 9.22