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Assay Detail

CHEMBL876396

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

Functional
Inhibition of human epidermoid carcinoma xenograft (A431) tumor growth
9
Total Activities
9
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 Expert

Target

A-431 (CHEMBL614069)
Type CELL-LINE
Organism Homo sapiens

Publication

6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
Tsou HR, Mamuya N, Johnson BD, Reich MF, Gruber BC, Ye F, Nilakantan R, Shen R, Discafani C, DeBlanc R, Davis R, Koehn FE, Greenberger LM, Wang YF, Wissner A.
J Med Chem (2001) 44 : 2719 -2734
PubMed 11495584 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.20 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414220 1 7.48
CHEMBL285063 1 7.02
CHEMBL94066 1 6.89
CHEMBL93049 1 6.51
CHEMBL94123 1 5.97
CHEMBL92086 1 5.88
CHEMBL91748 1 5.68
CHEMBL93464 1 5.23
CHEMBL329642 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414220 IC50 = 33.0 nM 7.48
CHEMBL285063 IC50 = 95.0 nM 7.02
CHEMBL94066 IC50 = 128.0 nM 6.89
CHEMBL93049 IC50 = 306.0 nM 6.51
CHEMBL94123 IC50 = 1079.0 nM 5.97
CHEMBL92086 IC50 = 1310.0 nM 5.88
CHEMBL91748 IC50 = 2100.0 nM 5.68
CHEMBL93464 IC50 = 5840.0 nM 5.23
CHEMBL329642 IC50 = 6610.0 nM 5.18