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Assay Detail

CHEMBL976899

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Binding
Inhibition of EGFR
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

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

Publication

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
McDermott U, Sharma SV, Dowell L, Greninger P, Montagut C, Lamb J, Archibald H, Raudales R, Tam A, Lee D, Rothenberg SM, Supko JG, Sordella R, Ulkus LE, Iafrate AJ, Maheswaran S, Njauw CN, Tsao H, Drew L, Hanke JH, Ma XJ, Erlander MG, Gray NS, Haber DA, Settleman J.
Proc Natl Acad Sci U S A (2007) 104 : 19936 -19941
PubMed 18077425 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.86 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 9.40
CHEMBL180022 NERATINIB 4.0 1 7.04
CHEMBL217092 SARACATINIB 3.0 1 5.59
CHEMBL450786 PHA-665752 1 5.42
CHEMBL189584 PD-173074 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB IC50 = 0.4 nM 9.40
CHEMBL180022 NERATINIB IC50 = 92.0 nM 7.04
CHEMBL217092 SARACATINIB IC50 = 2590.0 nM 5.59
CHEMBL450786 PHA-665752 IC50 = 3800.0 nM 5.42
CHEMBL189584 PD-173074 IC50 > 50000.0 nM -