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Assay Detail

CHEMBL767317

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Binding
Inhibitory concentration against protein phosphatase 1 (PP1) using pNPP assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein phosphatase 1B (CHEMBL2845)
Type SINGLE PROTEIN
Organism Homo sapiens

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 17 6.56 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421377 1 8.52
CHEMBL318253 1 4.60
CHEMBL318666 1 -
CHEMBL318434 1 -
CHEMBL100880 1 -
CHEMBL100033 1 -
CHEMBL98661 1 -
CHEMBL99826 1 -
CHEMBL97984 1 -
CHEMBL99251 1 -
CHEMBL101402 1 -
CHEMBL316507 1 -
CHEMBL318677 1 -
CHEMBL99014 1 -
CHEMBL97878 1 -
CHEMBL98309 1 -
CHEMBL317292 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421377 IC50 = 3.0 nM 8.52
CHEMBL318253 IC50 = 25000.0 nM 4.60
CHEMBL318666 IC50 > 50000.0 nM -
CHEMBL318434 IC50 > 50000.0 nM -
CHEMBL100880 IC50 > 100000.0 nM -
CHEMBL100033 IC50 > 100000.0 nM -
CHEMBL98661 IC50 > 100000.0 nM -
CHEMBL99826 IC50 > 100000.0 nM -
CHEMBL97984 IC50 > 100000.0 nM -
CHEMBL99251 IC50 > 100000.0 nM -
CHEMBL101402 IC50 > 100000.0 nM -
CHEMBL316507 IC50 > 55000.0 nM -
CHEMBL318677 IC50 > 100000.0 nM -
CHEMBL99014 IC50 > 100000.0 nM -
CHEMBL97878 IC50 > 100000.0 nM -
CHEMBL98309 IC50 > 100000.0 nM -
CHEMBL317292 IC50 > 100000.0 nM -