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Assay Detail

CHEMBL767151

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Binding
Inhibitory activity against cytosolic Phospholipase A2 (PLA2) by bilayer assay
ChEMBL ↗
44
Total Activities
44
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 44 6.54 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL29838 — — 1 8.40
CHEMBL30108 — — 1 8.10
CHEMBL26200 — — 1 7.77
CHEMBL286067 — — 1 7.70
CHEMBL29515 — — 1 7.52
CHEMBL286068 — — 1 7.46
CHEMBL29353 — — 1 7.40
CHEMBL282164 — — 1 7.34
CHEMBL30130 — — 1 7.32
CHEMBL30107 — — 1 7.30
CHEMBL29246 — — 1 7.22
CHEMBL29247 — — 1 7.22
CHEMBL285344 — — 1 7.16
CHEMBL25900 — — 1 7.13
CHEMBL27479 — — 1 6.82
CHEMBL27245 — — 1 6.62
CHEMBL25853 — — 1 6.57
CHEMBL413539 — — 1 6.55
CHEMBL283294 — — 1 6.40
CHEMBL29807 — — 1 6.30
CHEMBL281320 — — 1 6.18
CHEMBL27531 — — 1 6.16
CHEMBL282634 — — 1 6.16
CHEMBL27534 — — 1 6.00
CHEMBL29859 — — 1 5.92
CHEMBL442099 — — 1 5.92
CHEMBL416027 — — 1 5.89
CHEMBL284224 — — 1 5.85
CHEMBL29552 — — 1 5.85
CHEMBL27478 — — 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL29838 — IC50 = 4.0 nM 8.40
CHEMBL30108 — IC50 = 8.0 nM 8.10
CHEMBL26200 — IC50 = 17.0 nM 7.77
CHEMBL286067 — IC50 = 20.0 nM 7.70
CHEMBL29515 — IC50 = 30.0 nM 7.52
CHEMBL286068 — IC50 = 35.0 nM 7.46
CHEMBL29353 — IC50 = 40.0 nM 7.40
CHEMBL282164 — IC50 = 46.0 nM 7.34
CHEMBL30130 — IC50 = 48.0 nM 7.32
CHEMBL30107 — IC50 = 50.0 nM 7.30
CHEMBL29246 — IC50 = 60.0 nM 7.22
CHEMBL29247 — IC50 = 60.0 nM 7.22
CHEMBL285344 — IC50 = 70.0 nM 7.16
CHEMBL25900 — IC50 = 74.0 nM 7.13
CHEMBL27479 — IC50 = 150.0 nM 6.82
CHEMBL27245 — IC50 = 240.0 nM 6.62
CHEMBL25853 — IC50 = 270.0 nM 6.57
CHEMBL413539 — IC50 = 280.0 nM 6.55
CHEMBL283294 — IC50 = 400.0 nM 6.40
CHEMBL29807 — IC50 = 500.0 nM 6.30
CHEMBL281320 — IC50 = 660.0 nM 6.18
CHEMBL282634 — IC50 = 700.0 nM 6.16
CHEMBL27531 — IC50 = 690.0 nM 6.16
CHEMBL27534 — IC50 = 1000.0 nM 6.00
CHEMBL29859 — IC50 = 1200.0 nM 5.92
CHEMBL442099 — IC50 = 1200.0 nM 5.92
CHEMBL416027 — IC50 = 1300.0 nM 5.89
CHEMBL284224 — IC50 = 1400.0 nM 5.85
CHEMBL29552 — IC50 = 1400.0 nM 5.85
CHEMBL27478 — IC50 = 1900.0 nM 5.72
CHEMBL30198 — IC50 = 2200.0 nM 5.66
CHEMBL29674 — IC50 = 2300.0 nM 5.64
CHEMBL29393 — IC50 = 3600.0 nM 5.44
CHEMBL29707 — IC50 = 4300.0 nM 5.37
CHEMBL416569 — IC50 = 15000.0 nM 4.82
CHEMBL29497 — IC50 = 28000.0 nM 4.55
CHEMBL26094 — IC50 > 10000.0 nM -
CHEMBL29987 — IC50 > 1000.0 nM -
CHEMBL417665 — IC50 > 10000.0 nM -
CHEMBL27075 — IC50 > 30000.0 nM -
CHEMBL416760 — IC50 > 3000.0 nM -
CHEMBL27217 — IC50 > 1000000.0 nM -
CHEMBL27543 — IC50 > 30000.0 nM -
CHEMBL26579 — IC50 > 30000.0 nM -