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Assay Detail

CHEMBL759989

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Binding
In vitro inhibition of porcine pancreatic phospholipase A2 evaluated by monomeric substrate assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 9 — Direct single protein target
Curated By Expert

Target

Phospholipase A2, major isoenzyme (CHEMBL4715)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Design and synthesis of some substrate analogue inhibitors of phospholipase A2 and investigations by NMR and molecular modeling into the binding interactions in the enzyme-inhibitor complex.
Bennion C, Connolly S, Gensmantel NP, Hallam C, Jackson CG, Primrose WU, Roberts GC, Robinson DH, Slaich PK.
J Med Chem (1992) 35 : 2939 -2951
PubMed 1501221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 5.89 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101972 1 7.52
CHEMBL101015 1 7.52
CHEMBL322409 1 6.64
CHEMBL102135 1 5.85
CHEMBL101890 1 5.40
CHEMBL4524081 1 5.35
CHEMBL319067 1 5.30
CHEMBL102090 1 5.22
CHEMBL99161 1 5.10
CHEMBL318193 1 5.00
CHEMBL99160 1 -
CHEMBL101925 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101972 IC50 = 30.0 nM 7.52
CHEMBL101015 IC50 = 30.0 nM 7.52
CHEMBL322409 IC50 = 230.0 nM 6.64
CHEMBL102135 IC50 = 1400.0 nM 5.85
CHEMBL101890 IC50 = 4000.0 nM 5.40
CHEMBL4524081 IC50 = 4500.0 nM 5.35
CHEMBL319067 IC50 = 5000.0 nM 5.30
CHEMBL102090 IC50 = 6000.0 nM 5.22
CHEMBL99161 IC50 = 8000.0 nM 5.10
CHEMBL318193 IC50 = 10000.0 nM 5.00
CHEMBL99160 IC50 > 1000000.0 nM -
CHEMBL101925 IC50 = 160000.0 nM -