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Assay Detail

CHEMBL767489

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Binding
Inhibitory activity against partially purified (chicken skeletal muscle) Protein phosphatase 2A
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Muscle tissue
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Anhydride modified cantharidin analogues: synthesis, inhibition of protein phosphatases 1 and 2A and anticancer activity.
McCluskey A, Bowyer MC, Collins E, Sim ATR, Sakoff JA, Baldwin ML.
Bioorg Med Chem Lett (2000) 10 : 1687 -1690
PubMed 10937725 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.06 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48449 CANTHARIDIN 4.0 1 6.58
CHEMBL8327 DEMETHYL-CANTHARIDIN 1 6.43
CHEMBL47665 1 6.39
CHEMBL48076 1 6.35
CHEMBL48010 1 6.33
CHEMBL47461 1 4.26
CHEMBL45742 1 -
CHEMBL298459 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48449 CANTHARIDIN IC50 = 260.0 nM 6.58
CHEMBL8327 DEMETHYL-CANTHARIDIN IC50 = 370.0 nM 6.43
CHEMBL47665 IC50 = 410.0 nM 6.39
CHEMBL48076 IC50 = 450.0 nM 6.35
CHEMBL48010 IC50 = 470.0 nM 6.33
CHEMBL47461 IC50 = 55000.0 nM 4.26
CHEMBL45742 IC50 > 1000000.0 nM -
CHEMBL298459 IC50 > 1000000.0 nM -