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Assay Detail

CHEMBL1959299

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

Functional
Cytotoxicity against human A431 cells overexpressing EGFR
11
Total Activities
11
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

N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.
Gangjee A, Zaware N, Raghavan S, Yang J, Thorpe JE, Ihnat MA.
Bioorg Med Chem (2012) 20 : 2444 -2454
PubMed 22370340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.81 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1095464 1 5.92
CHEMBL1095761 1 5.55
CHEMBL1956887 1 4.63
CHEMBL1956885 1 4.54
CHEMBL499344 1 4.50
CHEMBL502015 1 4.48
CHEMBL1956886 1 4.47
CHEMBL514014 1 4.38
CHEMBL499345 1 -
CHEMBL1095465 1 -
CHEMBL474538 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1095464 IC50 = 1210.0 nM 5.92
CHEMBL1095761 IC50 = 2800.0 nM 5.55
CHEMBL1956887 IC50 = 23500.0 nM 4.63
CHEMBL1956885 IC50 = 28600.0 nM 4.54
CHEMBL499344 IC50 = 31800.0 nM 4.50
CHEMBL502015 IC50 = 33200.0 nM 4.48
CHEMBL1956886 IC50 = 33500.0 nM 4.47
CHEMBL514014 IC50 = 42100.0 nM 4.38
CHEMBL499345 IC50 > 50000.0 nM -
CHEMBL1095465 IC50 > 50000.0 nM -
CHEMBL474538 IC50 > 50000.0 nM -