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Assay Detail

CHEMBL964936

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Binding
Inhibition of ErbB2 by SPA assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors.
Waterson AG, Petrov KG, Hornberger KR, Hubbard RD, Sammond DM, Smith SC, Dickson HD, Caferro TR, Hinkle KW, Stevens KL, Dickerson SH, Rusnak DW, Spehar GM, Wood ER, Griffin RJ, Uehling DE.
Bioorg Med Chem Lett (2009) 19 : 1332 -1336
PubMed 19208477 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.81 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL504117 1 7.52
CHEMBL453398 1 7.22
CHEMBL452768 1 6.92
CHEMBL447720 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL504117 IC50 = 30.0 nM 7.52
CHEMBL453398 IC50 = 60.0 nM 7.22
CHEMBL452768 IC50 = 120.0 nM 6.92
CHEMBL447720 IC50 = 2660.0 nM 5.58