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Assay Detail

CHEMBL4679831

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

Binding
Inhibition of non-phosphorylated CDK6/Cyclin D1 (unknown origin) assessed as reduction in production of ADP using 5-FAM-RRRFRPASPLRGPPK peptide as substrate preincubated with enzyme for 12 mins and measured after 35 mins in presence of ATP by fluorescence-based microfluidic mobility shift assay
14
Total Activities
14
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

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

Publication

Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.
Abdel-Magid AF.
ACS Med Chem Lett (2021) 12 : 182 -184
PubMed 33603963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.95 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4446357 EBVACICLIB 2.0 1 10.10
CHEMBL4750658 1 9.89
CHEMBL4745424 1 9.74
CHEMBL4796501 1 9.51
CHEMBL4748471 1 9.07
CHEMBL4747638 1 9.06
CHEMBL4798327 1 9.02
CHEMBL4757341 1 8.75
CHEMBL4797526 1 8.70
CHEMBL4755392 1 8.65
CHEMBL4752291 1 8.54
CHEMBL4753883 1 8.15
CHEMBL4800105 1 8.04
CHEMBL4763871 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4446357 EBVACICLIB Ki = 0.08 nM 10.10
CHEMBL4750658 Ki = 0.13 nM 9.89
CHEMBL4745424 Ki = 0.18 nM 9.74
CHEMBL4796501 Ki = 0.31 nM 9.51
CHEMBL4748471 Ki = 0.85 nM 9.07
CHEMBL4747638 Ki = 0.88 nM 9.06
CHEMBL4798327 Ki = 0.96 nM 9.02
CHEMBL4757341 Ki = 1.77 nM 8.75
CHEMBL4797526 Ki = 1.99 nM 8.70
CHEMBL4755392 Ki = 2.23 nM 8.65
CHEMBL4752291 Ki = 2.91 nM 8.54
CHEMBL4753883 Ki = 7.0 nM 8.15
CHEMBL4800105 Ki = 9.15 nM 8.04
CHEMBL4763871 Ki = 9.59 nM 8.02