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Assay Detail

CHEMBL5215369

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

Binding
Inhibition of bovine brain PP2A assessed as dephosphorylation of substrate using P32 labelled peptide DLDVPIPGRFDRRVSVAAE as substrate by radiometric analysis
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Antitumor potential of the protein phosphatase inhibitor, cantharidin, and selected derivatives.
Ren Y, Kinghorn AD.
Bioorg Med Chem (2021) 32 : 116012 -116012
PubMed 33454654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.34 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48449 CANTHARIDIN 4.0 1 7.40
CHEMBL1234720 1 7.30
CHEMBL5219035 1 6.92
CHEMBL8327 DEMETHYL-CANTHARIDIN 1 6.43
CHEMBL428650 ENDOTHALL 1 6.01
CHEMBL5218547 1 4.00
CHEMBL5218860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48449 CANTHARIDIN IC50 = 40.0 nM 7.40
CHEMBL1234720 IC50 = 50.0 nM 7.30
CHEMBL5219035 IC50 = 120.0 nM 6.92
CHEMBL8327 DEMETHYL-CANTHARIDIN IC50 = 370.0 nM 6.43
CHEMBL428650 ENDOTHALL IC50 = 970.0 nM 6.01
CHEMBL5218547 IC50 = 99900.0 nM 4.00
CHEMBL5218860 IC50 > 200000.0 nM -