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Assay Detail

CHEMBL5031648

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

Binding
Inhibition of ALDH1A1 in human drug-tolerant MDA-MB-231/lapatinib cells assessed as after 24 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aldehyde dehydrogenase 1A1 (CHEMBL3577)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conjugates Derived from Lapatinib Derivatives with Cancer Cell Stemness Inhibitors Effectively Reversed Drug Resistance in Triple-Negative Breast Cancer.
Wang Y, Lv Z, Chen F, Wang X, Gou S.
J Med Chem (2021) 64 : 12877 -12892
PubMed 34435487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.65 7.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5094282 1 7.06
CHEMBL5079998 1 6.87
CHEMBL64130 NAPABUCASIN 3.0 1 6.37
CHEMBL567 PERPHENAZINE 4.0 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5094282 IC50 = 86.42 nM 7.06
CHEMBL5079998 IC50 = 134.58 nM 6.87
CHEMBL64130 NAPABUCASIN IC50 = 425.32 nM 6.37
CHEMBL567 PERPHENAZINE IC50 = 524.21 nM 6.28