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Assay Detail

CHEMBL834809

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

Functional
Inhibitory concentration was measured by the incorporation of [14C]thymidine in (human breast carcinoma) MDA-MB-435
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-435
Confidence 1 — Organism
Curated By Intermediate

Target

MDA-MB-435 (CHEMBL614697)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6.
Toogood PL, Harvey PJ, Repine JT, Sheehan DJ, VanderWel SN, Zhou H, Keller PR, McNamara DJ, Sherry D, Zhu T, Brodfuehrer J, Choi C, Barvian MR, Fry DW.
J Med Chem (2005) 48 : 2388 -2406
PubMed 15801831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.09 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370295 1 6.66
CHEMBL372712 1 6.38
CHEMBL189978 1 6.24
CHEMBL192749 1 6.24
CHEMBL191138 1 5.85
CHEMBL193167 1 5.71
CHEMBL189215 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370295 IC50 = 220.0 nM 6.66
CHEMBL372712 IC50 = 420.0 nM 6.38
CHEMBL189978 IC50 = 570.0 nM 6.24
CHEMBL192749 IC50 = 570.0 nM 6.24
CHEMBL191138 IC50 = 1400.0 nM 5.85
CHEMBL193167 IC50 = 1930.0 nM 5.71
CHEMBL189215 IC50 = 2770.0 nM 5.56