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Assay Detail

CHEMBL1220784

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

Binding
Inhibition of human PLD1 assessed as release of methyl-[3H]choline from choline-methyl-[3H]dipalmitoylphosphatidylcholine after 30 mins by exogenous substrate assay
28
Total Activities
28
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

Phospholipase D1 (CHEMBL2536)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness.
Scott SA, Selvy PE, Buck JR, Cho HP, Criswell TL, Thomas AL, Armstrong MD, Arteaga CL, Lindsley CW, Brown HA.
Nat Chem Biol (2009) 5 : 108 -117
PubMed 19136975 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.41 8.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398567 1 8.02
CHEMBL492572 1 7.34
CHEMBL1213069 1 7.34
CHEMBL1213097 1 7.26
CHEMBL1213144 1 7.23
CHEMBL1213066 1 7.10
CHEMBL492797 1 7.09
CHEMBL398568 1 7.00
CHEMBL245621 HALOPEMIDE 2.0 1 6.66
CHEMBL1213068 1 6.58
CHEMBL1213099 1 6.52
CHEMBL1213143 1 6.50
CHEMBL1213141 1 6.44
CHEMBL1213190 1 6.40
CHEMBL1213067 1 6.32
CHEMBL1213142 1 6.27
CHEMBL524008 1 6.18
CHEMBL1213140 1 6.11
CHEMBL1213191 1 5.92
CHEMBL1213100 1 5.85
CHEMBL1213193 1 5.50
CHEMBL81 RALOXIFENE 4.0 1 5.37
CHEMBL511475 1 5.29
CHEMBL1213192 1 5.13
CHEMBL1213098 1 4.82
CHEMBL1213274 1 -
CHEMBL1213275 1 -
CHEMBL1213325 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398567 IC50 = 9.5 nM 8.02
CHEMBL492572 IC50 = 46.0 nM 7.34
CHEMBL1213069 IC50 = 46.0 nM 7.34
CHEMBL1213097 IC50 = 55.0 nM 7.26
CHEMBL1213144 IC50 = 59.0 nM 7.23
CHEMBL1213066 IC50 = 79.0 nM 7.10
CHEMBL492797 IC50 = 81.0 nM 7.09
CHEMBL398568 IC50 = 100.0 nM 7.00
CHEMBL245621 HALOPEMIDE IC50 = 220.0 nM 6.66
CHEMBL1213068 IC50 = 260.0 nM 6.58
CHEMBL1213099 IC50 = 300.0 nM 6.52
CHEMBL1213143 IC50 = 316.0 nM 6.50
CHEMBL1213141 IC50 = 360.0 nM 6.44
CHEMBL1213190 IC50 = 400.0 nM 6.40
CHEMBL1213067 IC50 = 480.0 nM 6.32
CHEMBL1213142 IC50 = 540.0 nM 6.27
CHEMBL524008 IC50 = 660.0 nM 6.18
CHEMBL1213140 IC50 = 780.0 nM 6.11
CHEMBL1213191 IC50 = 1200.0 nM 5.92
CHEMBL1213100 IC50 = 1400.0 nM 5.85
CHEMBL1213193 IC50 = 3200.0 nM 5.50
CHEMBL81 RALOXIFENE IC50 = 4300.0 nM 5.37
CHEMBL511475 IC50 = 5100.0 nM 5.29
CHEMBL1213192 IC50 = 7400.0 nM 5.13
CHEMBL1213098 IC50 = 15000.0 nM 4.82
CHEMBL1213274 IC50 > 20000.0 nM -
CHEMBL1213275 IC50 > 20000.0 nM -
CHEMBL1213325 IC50 - -