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Assay Detail

CHEMBL820845

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

Binding
Inhibition of human recombinant cyclin D2-CDK4
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

A novel approach for the development of selective Cdk4 inhibitors: library design based on locations of Cdk4 specific amino acid residues.
Honma T, Yoshizumi T, Hashimoto N, Hayashi K, Kawanishi N, Fukasawa K, Takaki T, Ikeura C, Ikuta M, Suzuki-Takahashi I, Hayama T, Nishimura S, Morishima H.
J Med Chem (2001) 44 : 4628 -4640
PubMed 11741480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.12 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL143748 1 8.80
CHEMBL336242 1 8.64
CHEMBL140216 1 7.68
CHEMBL140781 1 7.54
CHEMBL344031 1 7.25
CHEMBL140141 1 7.19
CHEMBL356535 1 6.89
CHEMBL143361 1 6.80
CHEMBL359020 1 6.68
CHEMBL143285 1 6.66
CHEMBL342336 1 6.60
CHEMBL140205 1 6.54
CHEMBL140670 1 6.33
CHEMBL143163 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL143748 IC50 = 1.6 nM 8.80
CHEMBL336242 IC50 = 2.3 nM 8.64
CHEMBL140216 IC50 = 21.0 nM 7.68
CHEMBL140781 IC50 = 29.0 nM 7.54
CHEMBL344031 IC50 = 56.0 nM 7.25
CHEMBL140141 IC50 = 65.0 nM 7.19
CHEMBL356535 IC50 = 130.0 nM 6.89
CHEMBL143361 IC50 = 160.0 nM 6.80
CHEMBL359020 IC50 = 210.0 nM 6.68
CHEMBL143285 IC50 = 220.0 nM 6.66
CHEMBL342336 IC50 = 250.0 nM 6.60
CHEMBL140205 IC50 = 290.0 nM 6.54
CHEMBL140670 IC50 = 470.0 nM 6.33
CHEMBL143163 IC50 = 720.0 nM 6.14