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Assay Detail

CHEMBL760953

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

Binding
Inhibitory activity against recombinant human secretory phospholipase A2 (s-PLA2) by phosphatidylcholine/deoxycholate assay (PC/DOC).
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Phospholipase A2 (CHEMBL4426)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent inhibitors of secretory phospholipase A2: synthesis and inhibitory activities of indolizine and indene derivatives.
Hagishita S, Yamada M, Shirahase K, Okada T, Murakami Y, Ito Y, Matsuura T, Wada M, Kato T, Ueno M, Chikazawa Y, Yamada K, Ono T, Teshirogi I, Ohtani M.
J Med Chem (1996) 39 : 3636 -3658
PubMed 8809154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.70 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331755 1 8.89
CHEMBL121627 1 8.85
CHEMBL120112 1 8.52
CHEMBL332547 1 8.52
CHEMBL121245 1 8.52
CHEMBL332993 1 8.52
CHEMBL332957 1 8.38
CHEMBL123774 1 8.30
CHEMBL121617 1 8.30
CHEMBL121645 1 8.22
CHEMBL121422 1 8.14
CHEMBL123182 1 7.96
CHEMBL122736 1 7.89
CHEMBL420169 1 7.89
CHEMBL332393 1 7.89
CHEMBL121481 1 7.85
CHEMBL414424 1 7.82
CHEMBL334242 1 7.72
CHEMBL331184 1 7.70
CHEMBL330987 1 7.66
CHEMBL121609 1 7.62
CHEMBL121030 1 7.58
CHEMBL123384 1 7.55
CHEMBL120553 1 7.52
CHEMBL120909 1 7.52
CHEMBL120899 1 7.31
CHEMBL121199 1 7.28
CHEMBL123394 1 7.11
CHEMBL120884 1 7.10
CHEMBL120850 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331755 IC50 = 1.3 nM 8.89
CHEMBL121627 IC50 = 1.4 nM 8.85
CHEMBL332547 IC50 = 3.0 nM 8.52
CHEMBL121245 IC50 = 3.0 nM 8.52
CHEMBL332993 IC50 = 3.0 nM 8.52
CHEMBL120112 IC50 = 3.0 nM 8.52
CHEMBL332957 IC50 = 4.2 nM 8.38
CHEMBL123774 IC50 = 5.0 nM 8.30
CHEMBL121617 IC50 = 5.0 nM 8.30
CHEMBL121645 IC50 = 6.0 nM 8.22
CHEMBL121422 IC50 = 7.3 nM 8.14
CHEMBL123182 IC50 = 11.0 nM 7.96
CHEMBL122736 IC50 = 13.0 nM 7.89
CHEMBL420169 IC50 = 13.0 nM 7.89
CHEMBL332393 IC50 = 13.0 nM 7.89
CHEMBL121481 IC50 = 14.0 nM 7.85
CHEMBL414424 IC50 = 15.0 nM 7.82
CHEMBL334242 IC50 = 19.0 nM 7.72
CHEMBL331184 IC50 = 20.0 nM 7.70
CHEMBL330987 IC50 = 22.0 nM 7.66
CHEMBL121609 IC50 = 24.0 nM 7.62
CHEMBL121030 IC50 = 26.0 nM 7.58
CHEMBL123384 IC50 = 28.0 nM 7.55
CHEMBL120553 IC50 = 30.0 nM 7.52
CHEMBL120909 IC50 = 30.0 nM 7.52
CHEMBL120899 IC50 = 49.0 nM 7.31
CHEMBL121199 IC50 = 52.0 nM 7.28
CHEMBL123394 IC50 = 78.0 nM 7.11
CHEMBL120884 IC50 = 80.0 nM 7.10
CHEMBL120850 IC50 = 88.0 nM 7.06
CHEMBL330844 IC50 = 100.0 nM 7.00
CHEMBL119969 IC50 = 120.0 nM 6.92
CHEMBL123343 IC50 = 130.0 nM 6.89
CHEMBL338054 IC50 = 135.0 nM 6.87
CHEMBL121664 IC50 = 160.0 nM 6.80
CHEMBL332532 IC50 = 200.0 nM 6.70
CHEMBL122718 IC50 = 210.0 nM 6.68