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Assay Detail

CHEMBL5162305

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

Functional
Antiproliferative activity against human NCI-N87 cells assessed as inhibition of cell growth incubated for 72 hrs by Celltiter-Glo assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-N87
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-N87 (CHEMBL614197)
Type CELL-LINE
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 22 8.23 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5181694 1 9.25
CHEMBL180022 NERATINIB 4.0 1 9.19
CHEMBL3647420 PYROTINIB 3.0 1 9.07
CHEMBL5170965 1 8.97
CHEMBL5178703 1 8.96
CHEMBL5184610 1 8.95
CHEMBL5176854 1 8.81
CHEMBL5190132 1 8.72
CHEMBL5179954 1 8.66
CHEMBL5193451 1 8.58
CHEMBL5201973 1 8.39
CHEMBL5192750 1 8.34
CHEMBL5183924 1 8.18
CHEMBL5209046 1 8.17
CHEMBL5175873 1 7.93
CHEMBL5180725 1 7.72
CHEMBL5202846 1 7.55
CHEMBL5180965 1 7.48
CHEMBL5176920 1 7.38
CHEMBL5175489 1 7.29
CHEMBL5203179 1 7.09
CHEMBL5200783 1 6.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5181694 IC50 = 0.56 nM 9.25
CHEMBL180022 NERATINIB IC50 = 0.64 nM 9.19
CHEMBL3647420 PYROTINIB IC50 = 0.85 nM 9.07
CHEMBL5170965 IC50 = 1.08 nM 8.97
CHEMBL5178703 IC50 = 1.09 nM 8.96
CHEMBL5184610 IC50 = 1.12 nM 8.95
CHEMBL5176854 IC50 = 1.55 nM 8.81
CHEMBL5190132 IC50 = 1.9 nM 8.72
CHEMBL5179954 IC50 = 2.17 nM 8.66
CHEMBL5193451 IC50 = 2.65 nM 8.58
CHEMBL5201973 IC50 = 4.08 nM 8.39
CHEMBL5192750 IC50 = 4.55 nM 8.34
CHEMBL5183924 IC50 = 6.56 nM 8.18
CHEMBL5209046 IC50 = 6.7 nM 8.17
CHEMBL5175873 IC50 = 11.7 nM 7.93
CHEMBL5180725 IC50 = 19.19 nM 7.72
CHEMBL5202846 IC50 = 28.28 nM 7.55
CHEMBL5180965 IC50 = 32.89 nM 7.48
CHEMBL5176920 IC50 = 41.7 nM 7.38
CHEMBL5175489 IC50 = 51.9 nM 7.29
CHEMBL5203179 IC50 = 80.74 nM 7.09
CHEMBL5200783 IC50 = 441.2 nM 6.36