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Assay Detail

CHEMBL761440

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

Binding
Inhibition of human nonpancreatic secretory Phospholipase A2 through chromogenic assay
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

Phospholipase A2, membrane associated (CHEMBL3474)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
Draheim SE, Bach NJ, Dillard RD, Berry DR, Carlson DG, Chirgadze NY, Clawson DK, Hartley LW, Johnson LM, Jones ND, McKinney ER, Mihelich ED, Olkowski JL, Schevitz RW, Smith AC, Snyder DW, Sommers CD, Wery JP.
J Med Chem (1996) 39 : 5159 -5175
PubMed 8978844 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 7.15 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436456 1 8.40
CHEMBL345488 1 8.22
CHEMBL347957 1 8.22
CHEMBL357979 1 8.22
CHEMBL356606 1 8.22
CHEMBL345986 1 8.15
CHEMBL433701 1 8.10
CHEMBL347748 1 8.10
CHEMBL148674 VARESPLADIB 2.0 1 8.05
CHEMBL148795 1 8.05
CHEMBL355944 1 8.05
CHEMBL357804 1 8.05
CHEMBL422667 1 8.00
CHEMBL359005 1 7.96
CHEMBL346196 1 7.96
CHEMBL148649 1 7.96
CHEMBL423219 1 7.82
CHEMBL358872 1 7.60
CHEMBL358163 1 7.55
CHEMBL148452 1 7.52
CHEMBL148861 1 7.37
CHEMBL358155 1 7.34
CHEMBL146924 1 7.31
CHEMBL347052 1 7.09
CHEMBL149952 1 7.09
CHEMBL148665 1 7.02
CHEMBL149434 1 6.91
CHEMBL345987 1 6.85
CHEMBL149206 1 6.84
CHEMBL149779 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436456 IC50 = 4.0 nM 8.40
CHEMBL345488 IC50 = 6.0 nM 8.22
CHEMBL356606 IC50 = 6.0 nM 8.22
CHEMBL347957 IC50 = 6.0 nM 8.22
CHEMBL357979 IC50 = 6.0 nM 8.22
CHEMBL345986 IC50 = 7.0 nM 8.15
CHEMBL433701 IC50 = 8.0 nM 8.10
CHEMBL347748 IC50 = 8.0 nM 8.10
CHEMBL148674 VARESPLADIB IC50 = 9.0 nM 8.05
CHEMBL148795 IC50 = 9.0 nM 8.05
CHEMBL355944 IC50 = 9.0 nM 8.05
CHEMBL357804 IC50 = 9.0 nM 8.05
CHEMBL422667 IC50 = 10.0 nM 8.00
CHEMBL148649 IC50 = 11.0 nM 7.96
CHEMBL359005 IC50 = 11.0 nM 7.96
CHEMBL346196 IC50 = 11.0 nM 7.96
CHEMBL423219 IC50 = 15.0 nM 7.82
CHEMBL358872 IC50 = 25.0 nM 7.60
CHEMBL358163 IC50 = 28.0 nM 7.55
CHEMBL148452 IC50 = 30.0 nM 7.52
CHEMBL148861 IC50 = 43.0 nM 7.37
CHEMBL358155 IC50 = 46.0 nM 7.34
CHEMBL146924 IC50 = 49.0 nM 7.31
CHEMBL149952 IC50 = 82.0 nM 7.09
CHEMBL347052 IC50 = 81.0 nM 7.09
CHEMBL148665 IC50 = 96.0 nM 7.02
CHEMBL149434 IC50 = 124.0 nM 6.91
CHEMBL345987 IC50 = 141.0 nM 6.85
CHEMBL149206 IC50 = 145.0 nM 6.84
CHEMBL149779 IC50 = 145.0 nM 6.84
CHEMBL345275 IC50 = 188.0 nM 6.73
CHEMBL148807 IC50 = 210.0 nM 6.68
CHEMBL359148 IC50 = 243.0 nM 6.61
CHEMBL359308 IC50 = 551.0 nM 6.26
CHEMBL445135 IC50 = 1000.0 nM 6.00
CHEMBL430348 IC50 = 1180.0 nM 5.93
CHEMBL356133 IC50 = 1600.0 nM 5.80
CHEMBL356691 IC50 = 1620.0 nM 5.79
CHEMBL434131 IC50 = 2070.0 nM 5.68
CHEMBL347543 IC50 = 2560.0 nM 5.59
CHEMBL149271 IC50 = 46000.0 nM 4.34
CHEMBL345962 IC50 = 62000.0 nM 4.21
CHEMBL346641 IC50 > 100000.0 nM -
CHEMBL348462 IC50 > 100000.0 nM -