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Assay Detail

CHEMBL4721177

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

Functional
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo luminescent cell viability assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H1975
Confidence 1 — Organism
Curated By Autocuration

Target

NCI-H1975 (CHEMBL614348)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
Hou W,Ren Y,Zhang Z,Sun H,Ma Y,Yan B
Bioorg Med Chem (2018) 26 : 1740 -1750
PubMed 29523467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.26 5.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4745521 1 5.97
CHEMBL4754811 1 5.61
CHEMBL4750608 1 5.57
CHEMBL4755444 1 5.42
CHEMBL4756049 1 5.41
CHEMBL4750196 1 5.27
CHEMBL4777353 1 5.26
CHEMBL4792426 1 5.16
CHEMBL939 GEFITINIB 4.0 1 5.14
CHEMBL4796407 1 5.11
CHEMBL4753193 1 4.90
CHEMBL4790583 1 4.89
CHEMBL4757724 1 4.71
CHEMBL4749765 1 -
CHEMBL4777554 1 -
CHEMBL4782025 1 -
CHEMBL4789811 1 -
CHEMBL4790485 1 -
CHEMBL4757531 1 -
CHEMBL4747893 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4745521 IC50 = 1072.0 nM 5.97
CHEMBL4754811 IC50 = 2480.0 nM 5.61
CHEMBL4750608 IC50 = 2675.0 nM 5.57
CHEMBL4755444 IC50 = 3826.0 nM 5.42
CHEMBL4756049 IC50 = 3856.0 nM 5.41
CHEMBL4750196 IC50 = 5340.0 nM 5.27
CHEMBL4777353 IC50 = 5489.0 nM 5.26
CHEMBL4792426 IC50 = 6997.0 nM 5.16
CHEMBL939 GEFITINIB IC50 = 7184.0 nM 5.14
CHEMBL4796407 IC50 = 7811.0 nM 5.11
CHEMBL4753193 IC50 = 12649.0 nM 4.90
CHEMBL4790583 IC50 = 12876.0 nM 4.89
CHEMBL4757724 IC50 = 19482.0 nM 4.71
CHEMBL4749765 IC50 > 50000.0 nM -
CHEMBL4777554 IC50 > 50000.0 nM -
CHEMBL4782025 IC50 > 50000.0 nM -
CHEMBL4789811 IC50 > 50000.0 nM -
CHEMBL4790485 IC50 > 50000.0 nM -
CHEMBL4757531 IC50 > 50000.0 nM -
CHEMBL4747893 IC50 > 50000.0 nM -