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Assay Detail

CHEMBL1645699

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

Functional
Antiproliferative activity against EGFR-deficient human PC9 cells
39
Total Activities
39
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

Discovery of selective irreversible inhibitors for EGFR-T790M.
Zhou W, Ercan D, Jänne PA, Gray NS.
Bioorg Med Chem Lett (2011) 21 : 638 -643
PubMed 21208802 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 39 6.45 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1643989 1 8.22
CHEMBL1643976 1 7.82
CHEMBL939 GEFITINIB 4.0 1 7.77
CHEMBL1643988 1 7.70
CHEMBL1229592 1 7.44
CHEMBL1643990 1 7.40
CHEMBL1643994 1 7.10
CHEMBL1643977 1 7.10
CHEMBL1643973 1 7.00
CHEMBL1643974 1 7.00
CHEMBL1643972 1 6.70
CHEMBL1643963 1 6.52
CHEMBL1643964 1 6.30
CHEMBL1643982 1 6.30
CHEMBL1643995 1 6.16
CHEMBL1643981 1 6.10
CHEMBL1643996 1 6.10
CHEMBL1643978 1 6.10
CHEMBL1643962 1 6.05
CHEMBL1643960 1 6.00
CHEMBL1643967 1 5.22
CHEMBL1643965 1 5.22
CHEMBL1643966 1 5.22
CHEMBL1643959 1 5.16
CHEMBL1643961 1 5.00
CHEMBL1643968 1 5.00
CHEMBL1643986 1 -
CHEMBL1643993 1 -
CHEMBL1643992 1 -
CHEMBL1643991 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1643989 EC50 = 6.0 nM 8.22
CHEMBL1643976 EC50 = 15.0 nM 7.82
CHEMBL939 GEFITINIB EC50 = 17.0 nM 7.77
CHEMBL1643988 EC50 = 20.0 nM 7.70
CHEMBL1229592 EC50 = 36.0 nM 7.44
CHEMBL1643990 EC50 = 40.0 nM 7.40
CHEMBL1643994 EC50 = 80.0 nM 7.10
CHEMBL1643977 EC50 = 80.0 nM 7.10
CHEMBL1643973 EC50 = 100.0 nM 7.00
CHEMBL1643974 EC50 = 100.0 nM 7.00
CHEMBL1643972 EC50 = 200.0 nM 6.70
CHEMBL1643963 EC50 = 300.0 nM 6.52
CHEMBL1643964 EC50 = 500.0 nM 6.30
CHEMBL1643982 EC50 = 500.0 nM 6.30
CHEMBL1643995 EC50 = 700.0 nM 6.16
CHEMBL1643981 EC50 = 800.0 nM 6.10
CHEMBL1643978 EC50 = 800.0 nM 6.10
CHEMBL1643996 EC50 = 800.0 nM 6.10
CHEMBL1643962 EC50 = 900.0 nM 6.05
CHEMBL1643960 EC50 = 1000.0 nM 6.00
CHEMBL1643965 EC50 = 6000.0 nM 5.22
CHEMBL1643966 EC50 = 6000.0 nM 5.22
CHEMBL1643967 EC50 = 6000.0 nM 5.22
CHEMBL1643959 EC50 = 7000.0 nM 5.16
CHEMBL1643961 EC50 = 10000.0 nM 5.00
CHEMBL1643968 EC50 = 10000.0 nM 5.00
CHEMBL1643971 EC50 - -
CHEMBL1643970 EC50 - -
CHEMBL1643969 EC50 - -
CHEMBL1643979 EC50 > 1000.0 nM -
CHEMBL1643983 EC50 - -
CHEMBL1643984 EC50 - -
CHEMBL1643985 EC50 - -
CHEMBL1643975 EC50 - -
CHEMBL1643987 EC50 - -
CHEMBL1643991 EC50 > 1000.0 nM -
CHEMBL1643992 EC50 - -
CHEMBL1643993 EC50 - -
CHEMBL1643986 EC50 - -