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Assay Detail

CHEMBL990836

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Binding
Inhibition of human group2X phospholipase A2 fluorimetric assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Group 10 secretory phospholipase A2 (CHEMBL4342)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly specific and broadly potent inhibitors of mammalian secreted phospholipases A2.
Oslund RC, Cermak N, Gelb MH.
J Med Chem (2008) 51 : 4708 -4714
PubMed 18605714 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.30 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477548 1 8.15
CHEMBL514705 1 8.00
CHEMBL514656 1 7.96
CHEMBL474874 1 7.85
CHEMBL514692 1 7.82
CHEMBL515637 1 7.70
CHEMBL148649 1 7.66
CHEMBL477549 1 7.52
CHEMBL506485 1 7.52
CHEMBL504813 1 7.30
CHEMBL477794 1 7.16
CHEMBL148674 VARESPLADIB 2.0 1 7.12
CHEMBL477156 1 7.10
CHEMBL446349 1 7.05
CHEMBL477157 1 6.85
CHEMBL475071 1 6.50
CHEMBL514846 1 6.27
CHEMBL514841 1 5.82
CHEMBL479251 1 -
CHEMBL332993 1 -
CHEMBL478820 1 -
CHEMBL517821 1 -
CHEMBL478821 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477548 IC50 = 7.0 nM 8.15
CHEMBL514705 IC50 = 10.0 nM 8.00
CHEMBL514656 IC50 = 11.0 nM 7.96
CHEMBL474874 IC50 = 14.0 nM 7.85
CHEMBL514692 IC50 = 15.0 nM 7.82
CHEMBL515637 IC50 = 20.0 nM 7.70
CHEMBL148649 IC50 = 22.0 nM 7.66
CHEMBL477549 IC50 = 30.0 nM 7.52
CHEMBL506485 IC50 = 30.0 nM 7.52
CHEMBL504813 IC50 = 50.0 nM 7.30
CHEMBL477794 IC50 = 70.0 nM 7.16
CHEMBL148674 VARESPLADIB IC50 = 75.0 nM 7.12
CHEMBL477156 IC50 = 80.0 nM 7.10
CHEMBL446349 IC50 = 90.0 nM 7.05
CHEMBL477157 IC50 = 140.0 nM 6.85
CHEMBL475071 IC50 = 320.0 nM 6.50
CHEMBL514846 IC50 = 540.0 nM 6.27
CHEMBL514841 IC50 = 1500.0 nM 5.82
CHEMBL479251 IC50 > 21.0 nM -
CHEMBL332993 IC50 > 1600.0 nM -
CHEMBL478820 IC50 > 1600.0 nM -
CHEMBL517821 IC50 > 1600.0 nM -
CHEMBL478821 IC50 > 1600.0 nM -