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Assay Detail

CHEMBL768162

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Binding
Inhibitory concentration against protein phosphatase 2A (PP2A) using phosphorylase-a assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Oryctolagus cuniculus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Microcystin analogues comprised only of Adda and a single additional amino acid retain moderate activity as PP1/PP2A inhibitors.
Gulledge BM, Aggen JB, Eng H, Sweimeh K, Chamberlin AR.
Bioorg Med Chem Lett (2003) 13 : 2907 -2911
PubMed 14611855 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.93 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421377 1 9.52
CHEMBL318253 1 6.80
CHEMBL101932 1 6.30
CHEMBL97992 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421377 IC50 = 0.3 nM 9.52
CHEMBL318253 IC50 = 160.0 nM 6.80
CHEMBL101932 IC50 = 500.0 nM 6.30
CHEMBL97992 IC50 = 7800.0 nM 5.11