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Assay Detail

CHEMBL1250951

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

Binding
Inhibition of human GST-tagged PLD2A in human HEK293 cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phospholipase D2 (CHEMBL2734)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of halogenated N-(2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4.5]decan-8-yl)ethyl)benzamides: discovery of an isoform-selective small molecule phospholipase D2 inhibitor.
Lavieri RR, Scott SA, Selvy PE, Kim K, Jadhav S, Morrison RD, Daniels JS, Brown HA, Lindsley CW.
J Med Chem (2010) 53 : 6706 -6719
PubMed 20735042 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.71 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1254577 1 7.70
CHEMBL1254736 1 7.60
CHEMBL1253900 1 7.52
CHEMBL1253820 1 7.40
CHEMBL1254081 1 7.30
CHEMBL1254495 1 7.22
CHEMBL1254653 1 7.20
CHEMBL1254823 1 7.16
CHEMBL1254996 1 7.16
CHEMBL1254908 1 7.14
CHEMBL1255082 1 7.10
CHEMBL1254176 1 7.00
CHEMBL1255081 1 7.00
CHEMBL511475 1 6.96
CHEMBL1254909 1 6.92
CHEMBL471056 1 6.85
CHEMBL1254822 1 6.78
CHEMBL1253988 1 6.70
CHEMBL1254737 1 6.54
CHEMBL1254082 1 6.46
CHEMBL1254576 1 6.44
CHEMBL1253821 1 6.21
CHEMBL1254997 1 6.18
CHEMBL1253901 1 6.18
CHEMBL492572 1 5.75
CHEMBL1253989 1 5.25
CHEMBL1254654 1 5.17
CHEMBL1254175 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1254577 IC50 = 20.0 nM 7.70
CHEMBL1254736 IC50 = 25.0 nM 7.60
CHEMBL1253900 IC50 = 30.0 nM 7.52
CHEMBL1253820 IC50 = 40.0 nM 7.40
CHEMBL1254081 IC50 = 50.0 nM 7.30
CHEMBL1254495 IC50 = 60.0 nM 7.22
CHEMBL1254653 IC50 = 63.0 nM 7.20
CHEMBL1254823 IC50 = 70.0 nM 7.16
CHEMBL1254996 IC50 = 70.0 nM 7.16
CHEMBL1254908 IC50 = 73.0 nM 7.14
CHEMBL1255082 IC50 = 80.0 nM 7.10
CHEMBL1254176 IC50 = 100.0 nM 7.00
CHEMBL1255081 IC50 = 100.0 nM 7.00
CHEMBL511475 IC50 = 110.0 nM 6.96
CHEMBL1254909 IC50 = 120.0 nM 6.92
CHEMBL471056 IC50 = 140.0 nM 6.85
CHEMBL1254822 IC50 = 165.0 nM 6.78
CHEMBL1253988 IC50 = 200.0 nM 6.70
CHEMBL1254737 IC50 = 290.0 nM 6.54
CHEMBL1254082 IC50 = 350.0 nM 6.46
CHEMBL1254576 IC50 = 360.0 nM 6.44
CHEMBL1253821 IC50 = 610.0 nM 6.21
CHEMBL1254997 IC50 = 660.0 nM 6.18
CHEMBL1253901 IC50 = 655.0 nM 6.18
CHEMBL492572 IC50 = 1800.0 nM 5.75
CHEMBL1253989 IC50 = 5670.0 nM 5.25
CHEMBL1254654 IC50 = 6700.0 nM 5.17
CHEMBL1254175 IC50 = 8000.0 nM 5.10