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Assay Detail

CHEMBL875706

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

Binding
In vitro inhibition of human recombinant cytosolic phospholipase A2 (c-PLA2).
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis and evaluation of substrate-mimicking cytosolic phospholipase A2 inhibitors--reducing the lipophilicity of the arachidonyl chain isostere.
Walters I, Bennion C, Connolly S, Croshaw PJ, Hardy K, Hartopp P, Jackson CG, King SJ, Lawrence L, Mete A, Murray D, Robinson DH, Stein L, Wells E, John Withnall W.
Bioorg Med Chem Lett (2004) 14 : 3645 -3649
PubMed 15203135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.19 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30108 1 7.52
CHEMBL121193 1 7.40
CHEMBL124359 1 7.30
CHEMBL29838 1 7.10
CHEMBL121133 1 7.10
CHEMBL333523 1 7.05
CHEMBL124286 1 6.85
CHEMBL330853 1 6.75
CHEMBL122728 1 6.60
CHEMBL122828 1 6.57
CHEMBL30130 1 6.34
CHEMBL120051 1 6.25
CHEMBL332095 1 6.23
CHEMBL121684 1 6.12
CHEMBL121478 1 6.00
CHEMBL331478 1 5.77
CHEMBL119997 1 5.75
CHEMBL120222 1 5.28
CHEMBL330806 1 4.92
CHEMBL121438 1 4.70
CHEMBL123823 1 4.47
CHEMBL122657 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30108 IC50 = 30.0 nM 7.52
CHEMBL121193 IC50 = 40.0 nM 7.40
CHEMBL124359 IC50 = 50.0 nM 7.30
CHEMBL29838 IC50 = 80.0 nM 7.10
CHEMBL121133 IC50 = 80.0 nM 7.10
CHEMBL333523 IC50 = 90.0 nM 7.05
CHEMBL124286 IC50 = 140.0 nM 6.85
CHEMBL330853 IC50 = 180.0 nM 6.75
CHEMBL122728 IC50 = 250.0 nM 6.60
CHEMBL122828 IC50 = 270.0 nM 6.57
CHEMBL30130 IC50 = 460.0 nM 6.34
CHEMBL120051 IC50 = 560.0 nM 6.25
CHEMBL332095 IC50 = 590.0 nM 6.23
CHEMBL121684 IC50 = 760.0 nM 6.12
CHEMBL121478 IC50 = 1000.0 nM 6.00
CHEMBL331478 IC50 = 1700.0 nM 5.77
CHEMBL119997 IC50 = 1800.0 nM 5.75
CHEMBL120222 IC50 = 5200.0 nM 5.28
CHEMBL330806 IC50 = 12000.0 nM 4.92
CHEMBL121438 IC50 = 20000.0 nM 4.70
CHEMBL123823 IC50 = 34000.0 nM 4.47
CHEMBL122657 IC50 = 63000.0 nM 4.20