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Assay Detail

CHEMBL763947

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

Binding
Inhibition of Phosphodiesterase 4 from human neutrophils
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

The synthesis and biological evaluation of a novel series of phthalazine PDE4 inhibitors I.
Napoletano M, Norcini G, Pellacini F, Marchini F, Morazzoni G, Ferlenga P, Pradella L.
Bioorg Med Chem Lett (2000) 10 : 2235 -2238
PubMed 11012037 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.36 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.00
CHEMBL74404 1 8.00
CHEMBL309341 1 7.72
CHEMBL308407 1 7.52
CHEMBL419814 1 7.52
CHEMBL308158 1 7.41
CHEMBL72362 1 7.38
CHEMBL70391 1 7.28
CHEMBL74631 1 7.24
CHEMBL70903 1 7.23
CHEMBL73640 1 6.82
CHEMBL303880 1 6.73
CHEMBL63 ROLIPRAM 2.0 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 1.0 nM 9.00
CHEMBL74404 IC50 = 10.0 nM 8.00
CHEMBL309341 IC50 = 19.0 nM 7.72
CHEMBL308407 IC50 = 30.0 nM 7.52
CHEMBL419814 IC50 = 30.0 nM 7.52
CHEMBL308158 IC50 = 39.0 nM 7.41
CHEMBL72362 IC50 = 42.0 nM 7.38
CHEMBL70391 IC50 = 53.0 nM 7.28
CHEMBL74631 IC50 = 57.0 nM 7.24
CHEMBL70903 IC50 = 59.0 nM 7.23
CHEMBL73640 IC50 = 153.0 nM 6.82
CHEMBL303880 IC50 = 186.0 nM 6.73
CHEMBL63 ROLIPRAM IC50 = 1680.0 nM 5.78