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Assay Detail

CHEMBL833509

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 cell line
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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 15 6.53 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL190281 1 7.70
CHEMBL193177 1 7.16
CHEMBL192308 1 7.05
CHEMBL189963 PALBOCICLIB 4.0 1 6.80
CHEMBL366211 1 6.72
CHEMBL415773 1 6.70
CHEMBL189099 1 6.54
CHEMBL190627 1 6.49
CHEMBL189011 1 6.48
CHEMBL193184 1 6.47
CHEMBL192827 1 6.25
CHEMBL371198 1 6.00
CHEMBL190061 1 5.97
CHEMBL363589 1 5.96
CHEMBL189543 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL190281 IC50 = 20.0 nM 7.70
CHEMBL193177 IC50 = 70.0 nM 7.16
CHEMBL192308 IC50 = 90.0 nM 7.05
CHEMBL189963 PALBOCICLIB IC50 = 160.0 nM 6.80
CHEMBL366211 IC50 = 190.0 nM 6.72
CHEMBL415773 IC50 = 200.0 nM 6.70
CHEMBL189099 IC50 = 290.0 nM 6.54
CHEMBL190627 IC50 = 325.0 nM 6.49
CHEMBL189011 IC50 = 330.0 nM 6.48
CHEMBL193184 IC50 = 340.0 nM 6.47
CHEMBL192827 IC50 = 560.0 nM 6.25
CHEMBL371198 IC50 = 1000.0 nM 6.00
CHEMBL190061 IC50 = 1080.0 nM 5.97
CHEMBL363589 IC50 = 1100.0 nM 5.96
CHEMBL189543 IC50 = 2150.0 nM 5.67