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Assay Detail

CHEMBL3299997

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

Functional
Cytotoxicity against human MDA-MB-435 cells
5
Total Activities
5
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 Autocuration

Target

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

Publication

The design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
Zhang X, Raghavan S, Ihnat M, Thorpe JE, Disch BC, Bastian A, Bailey-Downs LC, Dybdal-Hargreaves NF, Rohena CC, Hamel E, Mooberry SL, Gangjee A.
Bioorg Med Chem (2014) 22 : 3753 -3772
PubMed 24890652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.52 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3545252 DOCETAXEL 4.0 1 8.57
CHEMBL535 SUNITINIB 4.0 1 8.01
CHEMBL554 LAPATINIB 4.0 1 7.53
CHEMBL3298000 1 7.28
CHEMBL553 ERLOTINIB 4.0 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3545252 DOCETAXEL IC50 = 2.7 nM 8.57
CHEMBL535 SUNITINIB IC50 = 9.7 nM 8.01
CHEMBL554 LAPATINIB IC50 = 29.7 nM 7.53
CHEMBL3298000 IC50 = 53.0 nM 7.28
CHEMBL553 ERLOTINIB IC50 = 622.1 nM 6.21