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Assay Detail

CHEMBL3815447

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Functional
Antiproliferative activity against gefitinib-sensitive human PC9 cells assessed as cell viability after 72 hrs by cell titer-glo luminescence assay
6
Total Activities
6
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

Publication

Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.
Mowafy S, Galanis A, Doctor ZM, Paranal RM, Lasheen DS, Farag NA, Jänne PA, Abouzid KA.
Bioorg Med Chem (2016) 24 : 3501 -3512
PubMed 27288180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.25 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL939 GEFITINIB 4.0 1 7.20
CHEMBL3814257 1 6.65
CHEMBL3814846 1 6.18
CHEMBL3814211 1 6.02
CHEMBL3814021 1 5.80
CHEMBL3814940 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL939 GEFITINIB IC50 = 63.0 nM 7.20
CHEMBL3814257 IC50 = 224.7 nM 6.65
CHEMBL3814846 IC50 = 661.6 nM 6.18
CHEMBL3814211 IC50 = 961.1 nM 6.02
CHEMBL3814021 IC50 = 1583.0 nM 5.80
CHEMBL3814940 IC50 = 2156.0 nM 5.67