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Assay Detail

CHEMBL998623

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Binding
Inhibition of PLD1 in human Calu1 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Calu-1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Phospholipase D1 (CHEMBL2536)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
Lavieri R, Scott SA, Lewis JA, Selvy PE, Armstrong MD, Alex Brown H, Lindsley CW.
Bioorg Med Chem Lett (2009) 19 : 2240 -2243
PubMed 19299128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.93 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL471056 1 7.60
CHEMBL471257 1 6.82
CHEMBL511648 1 6.82
CHEMBL511475 1 6.00
CHEMBL471054 1 5.72
CHEMBL471055 1 5.68
CHEMBL471259 1 5.58
CHEMBL513060 1 5.47
CHEMBL339069 1 5.44
CHEMBL18094 1 5.44
CHEMBL471258 1 5.37
CHEMBL471261 1 5.23
CHEMBL470847 1 -
CHEMBL471463 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL471056 IC50 = 25.0 nM 7.60
CHEMBL471257 IC50 = 150.0 nM 6.82
CHEMBL511648 IC50 = 150.0 nM 6.82
CHEMBL511475 IC50 = 1000.0 nM 6.00
CHEMBL471054 IC50 = 1900.0 nM 5.72
CHEMBL471055 IC50 = 2100.0 nM 5.68
CHEMBL471259 IC50 = 2600.0 nM 5.58
CHEMBL513060 IC50 = 3400.0 nM 5.47
CHEMBL339069 IC50 = 3600.0 nM 5.44
CHEMBL18094 IC50 = 3600.0 nM 5.44
CHEMBL471258 IC50 = 4250.0 nM 5.37
CHEMBL471261 IC50 = 5900.0 nM 5.23
CHEMBL470847 IC50 > 20000.0 nM -
CHEMBL471463 IC50 > 20000.0 nM -