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Assay Detail

CHEMBL5143813

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

Binding
Inhibition of N-terminal GST fused HER2 (679 to 1255 residues) (unknown origin) using poly (Glu-Tyr) E4Y1 peptide as substrate measured after 4 hrs by ADP-Glo reagent method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Small Molecule Kinase Inhibitor Drugs (1995-2021): Medical Indication, Pharmacology, and Synthesis.
Ayala-Aguilera CC, Valero T, Lorente-Macías Á, Baillache DJ, Croke S, Unciti-Broceta A.
J Med Chem (2022) 65 : 1047 -1131
PubMed 34624192 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 8.16 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3989868 TUCATINIB 4.0 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3989868 TUCATINIB IC50 = 6.9 nM 8.16