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Assay Detail

CHEMBL4329649

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Binding
Inhibition of PLD1 in human Calu1 cells
17
Total Activities
17
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

Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives.
Waterson AG, Scott SA, Kett NR, Blobaum AL, Alex Brown H, Lindsley CW.
Bioorg Med Chem Lett (2018) 28 : 3670 -3673
PubMed 30528979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.58 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4453586 1 9.00
CHEMBL4514153 1 7.80
CHEMBL4448918 1 7.80
CHEMBL4475943 1 7.68
CHEMBL4570440 1 7.60
CHEMBL3902347 1 6.70
CHEMBL4581260 1 6.60
CHEMBL4436548 1 6.50
CHEMBL4591820 1 6.50
CHEMBL4594070 1 6.09
CHEMBL4515874 1 5.92
CHEMBL3923136 1 5.87
CHEMBL3943964 1 5.77
CHEMBL3983405 1 5.26
CHEMBL4584012 1 5.19
CHEMBL4109224 1 4.92
CHEMBL4109788 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4453586 IC50 = 1.0 nM 9.00
CHEMBL4514153 IC50 = 16.0 nM 7.80
CHEMBL4448918 IC50 = 16.0 nM 7.80
CHEMBL4475943 IC50 = 21.0 nM 7.68
CHEMBL4570440 IC50 = 25.0 nM 7.60
CHEMBL3902347 IC50 = 200.0 nM 6.70
CHEMBL4581260 IC50 = 250.0 nM 6.60
CHEMBL4436548 IC50 = 320.0 nM 6.50
CHEMBL4591820 IC50 = 320.0 nM 6.50
CHEMBL4594070 IC50 = 820.0 nM 6.09
CHEMBL4515874 IC50 = 1200.0 nM 5.92
CHEMBL3923136 IC50 = 1350.0 nM 5.87
CHEMBL3943964 IC50 = 1700.0 nM 5.77
CHEMBL3983405 IC50 = 5500.0 nM 5.26
CHEMBL4584012 IC50 = 6400.0 nM 5.19
CHEMBL4109224 IC50 = 12000.0 nM 4.92
CHEMBL4109788 IC50 > 20000.0 nM -