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Assay Detail

CHEMBL5162370

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

Binding
Inhibition of EGFR (unknown origin)
3
Total Activities
3
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

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment.
Li D, Tu Y, Jin K, Duan L, Hong Y, Xu J, Chen N, Zhang Z, Zuo H, Gong W, Zhang J, Wang Q, Qian H, Wang X, Ke Y, Xia G.
J Med Chem (2022) 65 : 5334 -5354
PubMed 35319895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.36 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180022 NERATINIB 4.0 1 9.41
CHEMBL3647420 PYROTINIB 3.0 1 9.32
CHEMBL3989868 TUCATINIB 4.0 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180022 NERATINIB IC50 = 0.39 nM 9.41
CHEMBL3647420 PYROTINIB IC50 = 0.48 nM 9.32
CHEMBL3989868 TUCATINIB IC50 = 449.0 nM 6.35