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Assay Detail

CHEMBL767152

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Binding
Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by soluble assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytosolic phospholipase A2 beta (CHEMBL4136)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of a novel and potent series of inhibitors of cytosolic phospholipase A(2) based on a 1,3-disubstituted propan-2-one skeleton.
Connolly S, Bennion C, Botterell S, Croshaw PJ, Hallam C, Hardy K, Hartopp P, Jackson CG, King SJ, Lawrence L, Mete A, Murray D, Robinson DH, Smith GM, Stein L, Walters I, Wells E, Withnall WJ.
J Med Chem (2002) 45 : 1348 -1362
PubMed 11882004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.79 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418207 1 7.58
CHEMBL30108 1 7.52
CHEMBL29838 1 7.10
CHEMBL286067 1 6.92
CHEMBL286068 1 6.82
CHEMBL26200 1 6.82
CHEMBL29246 1 6.70
CHEMBL282164 1 6.39
CHEMBL30130 1 6.34
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE 1 6.10
CHEMBL27531 1 5.70
CHEMBL25853 1 5.66
CHEMBL281320 1 5.48
CHEMBL413539 1 5.34
CHEMBL29987 1 5.28
CHEMBL442099 1 5.19
CHEMBL25900 1 5.13
CHEMBL30198 1 4.80
CHEMBL416760 1 4.70
CHEMBL27543 1 4.58
CHEMBL29707 1 4.55
CHEMBL416027 1 4.28
CHEMBL29497 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418207 IC50 = 26.0 nM 7.58
CHEMBL30108 IC50 = 30.0 nM 7.52
CHEMBL29838 IC50 = 80.0 nM 7.10
CHEMBL286067 IC50 = 120.0 nM 6.92
CHEMBL286068 IC50 = 150.0 nM 6.82
CHEMBL26200 IC50 = 150.0 nM 6.82
CHEMBL29246 IC50 = 200.0 nM 6.70
CHEMBL282164 IC50 = 410.0 nM 6.39
CHEMBL30130 IC50 = 460.0 nM 6.34
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE IC50 = 800.0 nM 6.10
CHEMBL27531 IC50 = 2000.0 nM 5.70
CHEMBL25853 IC50 = 2200.0 nM 5.66
CHEMBL281320 IC50 = 3300.0 nM 5.48
CHEMBL413539 IC50 = 4600.0 nM 5.34
CHEMBL29987 IC50 = 5300.0 nM 5.28
CHEMBL442099 IC50 = 6500.0 nM 5.19
CHEMBL25900 IC50 = 7400.0 nM 5.13
CHEMBL30198 IC50 = 16000.0 nM 4.80
CHEMBL416760 IC50 = 20000.0 nM 4.70
CHEMBL27543 IC50 = 26000.0 nM 4.58
CHEMBL29707 IC50 = 28000.0 nM 4.55
CHEMBL416027 IC50 = 53000.0 nM 4.28
CHEMBL29497 IC50 = 67000.0 nM 4.17