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Assay Detail

CHEMBL5239891

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

Binding
Inhibition of porcine cytosolic phospholipase A2 alpha using SAPC and 2-dioleoyl-sn-glycerol as substrate incubated for 60 mins by HPLC-UV analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and pharmacokinetic properties of novel cPLA<sub>2</sub>α inhibitors with 1-(carboxyalkylpyrrolyl)-3-aryloxypropan-2-one structure.
Subeska A, Althaus J, Hake T, Hanekamp W, Bettenworth D, Mulac D, Langer K, Lehr M.
Bioorg Med Chem (2023) 77 : 117110 -117110
PubMed 36495814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.46 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5269139 1 9.00
CHEMBL5271148 1 9.00
CHEMBL30108 1 8.19
CHEMBL4097068 1 8.00
CHEMBL1085637 1 7.92
CHEMBL5288851 1 7.89
CHEMBL1800085 1 7.82
CHEMBL5269892 1 7.80
CHEMBL5289311 1 7.50
CHEMBL5269426 1 7.42
CHEMBL5277810 1 7.40
CHEMBL5276544 1 7.29
CHEMBL5266606 1 7.28
CHEMBL5288046 1 7.09
CHEMBL5281609 1 6.77
CHEMBL5277146 1 6.51
CHEMBL5282267 1 6.35
CHEMBL5287895 1 6.34
CHEMBL5267619 1 6.19
CHEMBL5273680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5269139 IC50 = 1.0 nM 9.00
CHEMBL5271148 IC50 = 1.0 nM 9.00
CHEMBL30108 IC50 = 6.5 nM 8.19
CHEMBL4097068 IC50 = 10.0 nM 8.00
CHEMBL1085637 IC50 = 12.0 nM 7.92
CHEMBL5288851 IC50 = 13.0 nM 7.89
CHEMBL1800085 IC50 = 15.0 nM 7.82
CHEMBL5269892 IC50 = 16.0 nM 7.80
CHEMBL5289311 IC50 = 32.0 nM 7.50
CHEMBL5269426 IC50 = 38.0 nM 7.42
CHEMBL5277810 IC50 = 40.0 nM 7.40
CHEMBL5276544 IC50 = 51.0 nM 7.29
CHEMBL5266606 IC50 = 53.0 nM 7.28
CHEMBL5288046 IC50 = 82.0 nM 7.09
CHEMBL5281609 IC50 = 170.0 nM 6.77
CHEMBL5277146 IC50 = 310.0 nM 6.51
CHEMBL5282267 IC50 = 450.0 nM 6.35
CHEMBL5287895 IC50 = 460.0 nM 6.34
CHEMBL5267619 IC50 = 650.0 nM 6.19
CHEMBL5273680 IC50 > 10000.0 nM -