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Assay Detail

CHEMBL764349

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

Functional
Inhibitory activity against cPLA2 (cytosolic Phospholipase A2) by measuring the calcium ionophore A-23,187-induced arachidonic acid release from bovine platelets
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cytosolic phospholipase A2 (CHEMBL2304401)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Synthesis, biological evaluation, and structure-activity relationships of 3-acylindole-2-carboxylic acids as inhibitors of the cytosolic phospholipase A2.
Lehr M.
J Med Chem (1997) 40 : 2694 -2705
PubMed 9276015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.25 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL87987 1 6.30
CHEMBL91419 1 5.85
CHEMBL90083 1 5.85
CHEMBL313460 1 5.80
CHEMBL312824 1 5.80
CHEMBL91323 1 5.80
CHEMBL91502 1 5.80
CHEMBL90297 1 5.72
CHEMBL89888 1 5.52
CHEMBL91612 1 5.40
CHEMBL88762 1 5.39
CHEMBL90527 1 5.37
CHEMBL91625 1 5.28
CHEMBL313643 1 5.16
CHEMBL90205 1 5.16
CHEMBL328567 1 5.16
CHEMBL422774 1 5.16
CHEMBL327256 1 5.10
CHEMBL314654 1 5.10
CHEMBL90537 1 5.10
CHEMBL92423 1 5.10
CHEMBL90033 1 5.10
CHEMBL88258 1 5.10
CHEMBL330088 1 5.05
CHEMBL90122 1 5.05
CHEMBL90412 1 5.05
CHEMBL93788 1 5.00
CHEMBL316279 1 5.00
CHEMBL90404 1 5.00
CHEMBL91312 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL87987 IC50 = 500.0 nM 6.30
CHEMBL91419 IC50 = 1400.0 nM 5.85
CHEMBL90083 IC50 = 1400.0 nM 5.85
CHEMBL313460 IC50 = 1600.0 nM 5.80
CHEMBL312824 IC50 = 1600.0 nM 5.80
CHEMBL91323 IC50 = 1600.0 nM 5.80
CHEMBL91502 IC50 = 1600.0 nM 5.80
CHEMBL90297 IC50 = 1900.0 nM 5.72
CHEMBL89888 IC50 = 3000.0 nM 5.52
CHEMBL91612 IC50 = 4000.0 nM 5.40
CHEMBL88762 IC50 = 4100.0 nM 5.39
CHEMBL90527 IC50 = 4300.0 nM 5.37
CHEMBL91625 IC50 = 5300.0 nM 5.28
CHEMBL422774 IC50 = 7000.0 nM 5.16
CHEMBL328567 IC50 = 7000.0 nM 5.16
CHEMBL313643 IC50 = 7000.0 nM 5.16
CHEMBL90205 IC50 = 7000.0 nM 5.16
CHEMBL88258 IC50 = 8000.0 nM 5.10
CHEMBL90033 IC50 = 8000.0 nM 5.10
CHEMBL92423 IC50 = 8000.0 nM 5.10
CHEMBL314654 IC50 = 8000.0 nM 5.10
CHEMBL327256 IC50 = 8000.0 nM 5.10
CHEMBL90537 IC50 = 8000.0 nM 5.10
CHEMBL330088 IC50 = 9000.0 nM 5.05
CHEMBL90122 IC50 = 9000.0 nM 5.05
CHEMBL90412 IC50 = 9000.0 nM 5.05
CHEMBL93788 IC50 = 10000.0 nM 5.00
CHEMBL316279 IC50 = 10000.0 nM 5.00
CHEMBL90404 IC50 = 10000.0 nM 5.00
CHEMBL91312 IC50 = 10000.0 nM 5.00
CHEMBL88829 IC50 = 11000.0 nM 4.96
CHEMBL329898 IC50 = 11000.0 nM 4.96
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE IC50 = 11000.0 nM 4.96
CHEMBL330711 IC50 = 11000.0 nM 4.96
CHEMBL90088 IC50 = 13000.0 nM 4.89
CHEMBL329600 IC50 = 18000.0 nM 4.75
CHEMBL313642 IC50 = 34000.0 nM 4.47
CHEMBL90890 IC50 > 10000.0 nM -
CHEMBL88352 IC50 > 33000.0 nM -
CHEMBL329539 IC50 > 33000.0 nM -
CHEMBL279640 IC50 > 33000.0 nM -