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Assay Detail

CHEMBL964196

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

Binding
Inhibition of ErbB2 by HTRF assay
18
Total Activities
18
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 18 6.91 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510845 1 7.52
CHEMBL500072 1 7.46
CHEMBL507821 1 7.30
CHEMBL508760 1 7.22
CHEMBL500217 1 7.22
CHEMBL455434 1 7.22
CHEMBL507329 GW869810X 1 7.10
CHEMBL451074 1 7.07
CHEMBL455433 1 7.06
CHEMBL503253 1 6.89
CHEMBL451347 1 6.75
CHEMBL505463 1 6.75
CHEMBL452980 1 6.68
CHEMBL457250 1 6.66
CHEMBL452716 1 6.58
CHEMBL461811 1 6.43
CHEMBL449949 1 6.35
CHEMBL501050 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510845 IC50 = 30.0 nM 7.52
CHEMBL500072 IC50 = 35.0 nM 7.46
CHEMBL507821 IC50 = 50.0 nM 7.30
CHEMBL508760 IC50 = 60.0 nM 7.22
CHEMBL500217 IC50 = 60.0 nM 7.22
CHEMBL455434 IC50 = 60.0 nM 7.22
CHEMBL507329 GW869810X IC50 = 80.0 nM 7.10
CHEMBL451074 IC50 = 85.0 nM 7.07
CHEMBL455433 IC50 = 87.0 nM 7.06
CHEMBL503253 IC50 = 130.0 nM 6.89
CHEMBL451347 IC50 = 180.0 nM 6.75
CHEMBL505463 IC50 = 180.0 nM 6.75
CHEMBL452980 IC50 = 210.0 nM 6.68
CHEMBL457250 IC50 = 220.0 nM 6.66
CHEMBL452716 IC50 = 260.0 nM 6.58
CHEMBL461811 IC50 = 370.0 nM 6.43
CHEMBL449949 IC50 = 450.0 nM 6.35
CHEMBL501050 IC50 = 800.0 nM 6.10