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Assay Detail

CHEMBL5721480

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

Binding
Inhibition of human CDK6/cyclin D1 preincubated with compound for 20 mins followed by [33P]ATP addition and measured after 2 hrs by filter binding method
2
Total Activities
2
Compounds Tested
1
Activity Types
4
Assay Parameters

Assay Information

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

Target

CDK6/cyclin D1 (CHEMBL2111455)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Competitive Kinase Enrichment Proteomics Reveals that Abemaciclib Inhibits GSK3β and Activates WNT Signaling.
Cousins EM, Goldfarb D, Yan F, Roques J, Darr D, Johnson GL, Major MB.
Mol Cancer Res (2018) 16 : 333 -344
PubMed 29133594 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.37 9.37

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0004992
EFO_ID EFO_ID - EFO:0005140
EFO_TERM EFO_TERM - cancer
EFO_TERM EFO_TERM - autoimmune disease

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3301610 ABEMACICLIB 4.0 1 9.37
CHEMBL189963 PALBOCICLIB 4.0 1 9.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3301610 ABEMACICLIB IC50 = 0.43 nM 9.37
CHEMBL189963 PALBOCICLIB IC50 = 0.43 nM 9.37