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Assay Detail

CHEMBL4373063

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

Functional
Antiproliferative activity against human PC9 cells harboring EGFR exon-19 del mutant after 72 hrs by EZ-Cytox assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type PC-9
Confidence 1 — Organism
Curated By Autocuration

Target

PC-9 (CHEMBL614102)
Type CELL-LINE
Organism Homo sapiens

Publication

Click chemistry for improvement in selectivity of quinazoline-based kinase inhibitors for mutant epidermal growth factor receptors.
Song J, Jang S, Lee JW, Jung D, Lee S, Min KH.
Bioorg Med Chem Lett (2019) 29 : 477 -480
PubMed 30554954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.82 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1173655 AFATINIB 4.0 1 10.00
CHEMBL4521506 1 9.22
CHEMBL4460706 1 9.05
CHEMBL4454948 1 9.05
CHEMBL4515526 1 9.00
CHEMBL4436695 1 8.96
CHEMBL4578487 1 8.92
CHEMBL4468464 1 8.92
CHEMBL4563683 1 8.89
CHEMBL4476544 1 8.82
CHEMBL3787386 1 8.54
CHEMBL4584413 1 8.44
CHEMBL939 GEFITINIB 4.0 1 8.21
CHEMBL4575267 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1173655 AFATINIB IC50 = 0.1 nM 10.00
CHEMBL4521506 IC50 = 0.6 nM 9.22
CHEMBL4460706 IC50 = 0.9 nM 9.05
CHEMBL4454948 IC50 = 0.9 nM 9.05
CHEMBL4515526 IC50 = 1.0 nM 9.00
CHEMBL4436695 IC50 = 1.1 nM 8.96
CHEMBL4578487 IC50 = 1.2 nM 8.92
CHEMBL4468464 IC50 = 1.2 nM 8.92
CHEMBL4563683 IC50 = 1.3 nM 8.89
CHEMBL4476544 IC50 = 1.5 nM 8.82
CHEMBL3787386 IC50 = 2.9 nM 8.54
CHEMBL4584413 IC50 = 3.6 nM 8.44
CHEMBL939 GEFITINIB IC50 = 6.1 nM 8.21
CHEMBL4575267 IC50 = 32.0 nM 7.50