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Assay Detail

CHEMBL882441

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

Binding
In vitro inhibition of cyclic AMP phosphodiesterase from human platelets.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.
Jones GH, Venuti MC, Alvarez R, Bruno JJ, Berks AH, Prince A.
J Med Chem (1987) 30 : 295 -303
PubMed 3027338 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.76 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69139 LIXAZINONE 2.0 1 8.00
CHEMBL760 ANAGRELIDE 4.0 1 7.10
CHEMBL34431 CILOSTAMIDE 2.0 1 6.77
CHEMBL420838 1 6.72
CHEMBL67513 1 6.54
CHEMBL102920 1 5.94
CHEMBL105666 1 5.94
CHEMBL103495 1 5.89
CHEMBL102273 1 5.87
CHEMBL65882 1 5.82
CHEMBL316542 1 5.75
CHEMBL102657 1 5.47
CHEMBL101969 1 5.44
CHEMBL102852 1 5.36
CHEMBL103863 1 5.00
CHEMBL316590 1 4.89
CHEMBL103878 1 4.68
CHEMBL100112 1 4.28
CHEMBL103557 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69139 LIXAZINONE IC50 = 10.0 nM 8.00
CHEMBL760 ANAGRELIDE IC50 = 80.0 nM 7.10
CHEMBL34431 CILOSTAMIDE IC50 = 170.0 nM 6.77
CHEMBL420838 IC50 = 190.0 nM 6.72
CHEMBL67513 IC50 = 290.0 nM 6.54
CHEMBL102920 IC50 = 1150.0 nM 5.94
CHEMBL105666 IC50 = 1150.0 nM 5.94
CHEMBL103495 IC50 = 1300.0 nM 5.89
CHEMBL102273 IC50 = 1350.0 nM 5.87
CHEMBL65882 IC50 = 1500.0 nM 5.82
CHEMBL316542 IC50 = 1800.0 nM 5.75
CHEMBL102657 IC50 = 3400.0 nM 5.47
CHEMBL101969 IC50 = 3600.0 nM 5.44
CHEMBL102852 IC50 = 4400.0 nM 5.36
CHEMBL103863 IC50 = 10000.0 nM 5.00
CHEMBL316590 IC50 = 13000.0 nM 4.89
CHEMBL103878 IC50 = 21000.0 nM 4.68
CHEMBL100112 IC50 = 53000.0 nM 4.28
CHEMBL103557 IC50 = 100000.0 nM 4.00