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Assay Detail

CHEMBL4388528

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

Binding
Inhibition of probe binding to HER2 (unknown origin) using rabbit reticulate lysate system after 1 hr by luminescence assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
Mansour TS, Potluri V, Pallepati RR, Basetti V, Keesara M, Moghudula AG, Maiti P.
Bioorg Med Chem Lett (2019) 29 : 1435 -1439
PubMed 31023512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.52 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4519470 1 7.03
CHEMBL4457447 1 6.80
CHEMBL4517633 1 6.78
CHEMBL4593016 1 6.23
CHEMBL4456266 1 6.14
CHEMBL4446124 1 6.14
CHEMBL4560998 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4519470 IC50 = 93.0 nM 7.03
CHEMBL4457447 IC50 = 160.0 nM 6.80
CHEMBL4517633 IC50 = 167.0 nM 6.78
CHEMBL4593016 IC50 = 590.0 nM 6.23
CHEMBL4456266 IC50 = 730.0 nM 6.14
CHEMBL4446124 IC50 = 730.0 nM 6.14
CHEMBL4560998 IC50 > 10000.0 nM -