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Assay Detail

CHEMBL5162352

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Functional
Antiproliferative activity against mouse BaF3 cells harbouring HER2 A775_G77insYVMA mutant assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type BaF3
Confidence 1 — Organism
Curated By Autocuration

Target

BaF3 (CHEMBL614524)
Type CELL-LINE
Organism Mus musculus

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 2 8.01 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5178703 1 8.20
CHEMBL3647420 PYROTINIB 3.0 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5178703 IC50 = 6.3 nM 8.20
CHEMBL3647420 PYROTINIB IC50 = 15.0 nM 7.82