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Assay Detail

CHEMBL795906

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

Binding
Inhibition of rat Receptor protein-tyrosine kinase erbB2
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Receptor tyrosine-protein kinase erbB-2 (CHEMBL3848)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Cockerill S, Stubberfield C, Stables J, Carter M, Guntrip S, Smith K, McKeown S, Shaw R, Topley P, Thomsen L, Affleck K, Jowett A, Hayes D, Willson M, Woollard P, Spalding D.
Bioorg Med Chem Lett (2001) 11 : 1401 -1405
PubMed 11378364 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.15 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL416031 1 9.00
CHEMBL284485 1 8.00
CHEMBL31407 1 8.00
CHEMBL30432 GW282974X 1 7.75
CHEMBL288557 1 7.58
CHEMBL281006 1 7.57
CHEMBL31653 1 7.31
CHEMBL31108 1 7.31
CHEMBL287591 1 7.05
CHEMBL31161 1 6.54
CHEMBL32464 1 6.25
CHEMBL281881 1 5.36
CHEMBL31615 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL416031 IC50 = 1.0 nM 9.00
CHEMBL284485 IC50 = 10.0 nM 8.00
CHEMBL31407 IC50 = 10.0 nM 8.00
CHEMBL30432 GW282974X IC50 = 18.0 nM 7.75
CHEMBL288557 IC50 = 26.0 nM 7.58
CHEMBL281006 IC50 = 27.0 nM 7.57
CHEMBL31653 IC50 = 49.0 nM 7.31
CHEMBL31108 IC50 = 49.0 nM 7.31
CHEMBL287591 IC50 = 90.0 nM 7.05
CHEMBL31161 IC50 = 290.0 nM 6.54
CHEMBL32464 IC50 = 560.0 nM 6.25
CHEMBL281881 IC50 = 4400.0 nM 5.36
CHEMBL31615 IC50 = 6600.0 nM 5.18