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Assay Detail

CHEMBL4721179

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

Functional
Antiproliferative activity against human A431 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo luminescent cell viability assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-431
Confidence 1 — Organism
Curated By Autocuration

Target

A-431 (CHEMBL614069)
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 17 6.50 7.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4752951 1 7.18
CHEMBL4759414 1 6.97
CHEMBL4755832 1 6.87
CHEMBL4790655 1 6.84
CHEMBL4776057 1 6.72
CHEMBL4741678 1 6.66
CHEMBL4743566 1 6.58
CHEMBL4751768 1 6.48
CHEMBL4760606 1 6.40
CHEMBL939 GEFITINIB 4.0 1 6.12
CHEMBL4750608 1 6.05
CHEMBL4754811 1 5.96
CHEMBL4750196 1 5.63
CHEMBL4789811 1 -
CHEMBL4760864 1 -
CHEMBL4782025 1 -
CHEMBL4762998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4752951 IC50 = 66.0 nM 7.18
CHEMBL4759414 IC50 = 107.0 nM 6.97
CHEMBL4755832 IC50 = 134.0 nM 6.87
CHEMBL4790655 IC50 = 146.0 nM 6.84
CHEMBL4776057 IC50 = 189.0 nM 6.72
CHEMBL4741678 IC50 = 220.0 nM 6.66
CHEMBL4743566 IC50 = 265.0 nM 6.58
CHEMBL4751768 IC50 = 331.0 nM 6.48
CHEMBL4760606 IC50 = 396.0 nM 6.40
CHEMBL939 GEFITINIB IC50 = 768.0 nM 6.12
CHEMBL4750608 IC50 = 887.0 nM 6.05
CHEMBL4754811 IC50 = 1100.0 nM 5.96
CHEMBL4750196 IC50 = 2352.0 nM 5.63
CHEMBL4789811 IC50 > 50000.0 nM -
CHEMBL4760864 IC50 > 10000.0 nM -
CHEMBL4782025 IC50 > 50000.0 nM -
CHEMBL4762998 IC50 > 10000.0 nM -