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Assay Detail

CHEMBL677384

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

Binding
Inhibition of epidermal growth factor receptor kinase autophosphorylation
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Epidermal growth factor receptor (CHEMBL203)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.
Wissner A, Hamann PR, Nilakantan R, Greenberger LM, Ye F, Rapuano TA, Loganzo F.
Bioorg Med Chem Lett (2004) 14 : 1411 -1416
PubMed 15006373 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.45 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31276 1 8.07
CHEMBL281300 1 7.06
CHEMBL607707 PELITINIB 2.0 1 7.01
CHEMBL30973 1 6.91
CHEMBL281467 1 6.01
CHEMBL31876 1 5.99
CHEMBL441518 1 5.38
CHEMBL287022 1 5.17
CHEMBL31745 1 -
CHEMBL283682 1 -
CHEMBL31437 1 -
CHEMBL31118 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31276 IC50 = 8.6 nM 8.07
CHEMBL281300 IC50 = 86.9 nM 7.06
CHEMBL607707 PELITINIB IC50 = 97.6 nM 7.01
CHEMBL30973 IC50 = 122.9 nM 6.91
CHEMBL281467 IC50 = 975.7 nM 6.01
CHEMBL31876 IC50 = 1027.8 nM 5.99
CHEMBL441518 IC50 = 4128.6 nM 5.38
CHEMBL287022 IC50 = 6794.8 nM 5.17
CHEMBL31745 IC50 > 10000.0 nM -
CHEMBL283682 IC50 > 1000.0 nM -
CHEMBL31437 IC50 > 10000.0 nM -
CHEMBL31118 IC50 > 10000.0 nM -