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Assay Detail

CHEMBL5546060

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

Functional
Antiproliferative activity against human BT-474 cells by CellTiter-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type BT-474
Confidence 1 — Organism
Curated By Autocuration

Target

BT-474 (CHEMBL614529)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of Novel 5,6-Dihydro-4<i>H</i>-pyrido[2,3,4-<i>de</i>]quinazoline Irreversible Inhibitors Targeting Both Wild-Type and A775_G776insYVMA Mutated HER2 Kinases.
Yang L, Li Y, Du Y, Guo Y, Guo Z, Liu B, Liu J, Liu Y, Niu H, Sun Y, Yan H, Yang Y, Yu S, Zhang Y, Zhang Y, Zheng K, Zheng N, Zhang X, Zhang Q, Hu L.
J Med Chem (2024) 67 : 5662 -5682
PubMed 38518121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.79 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180022 NERATINIB 4.0 1 8.00
CHEMBL5563672 1 7.82
CHEMBL5572660 1 7.76
CHEMBL5572514 1 7.75
CHEMBL5570443 1 7.73
CHEMBL5569244 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180022 NERATINIB IC50 = 10.0 nM 8.00
CHEMBL5563672 IC50 = 15.17 nM 7.82
CHEMBL5572660 IC50 = 17.38 nM 7.76
CHEMBL5572514 IC50 = 17.93 nM 7.75
CHEMBL5570443 IC50 = 18.55 nM 7.73
CHEMBL5569244 IC50 = 20.18 nM 7.70