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Assay Detail

CHEMBL757893

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

Binding
Inhibition of rolipram binding to PDE4 from human neutrophils
12
Total Activities
12
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
Ki 12 7.37 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 8.82
CHEMBL63 ROLIPRAM 2.0 1 8.80
CHEMBL74631 1 7.89
CHEMBL308407 1 7.80
CHEMBL308158 1 7.34
CHEMBL74404 1 7.15
CHEMBL70903 1 7.02
CHEMBL72362 1 6.92
CHEMBL70391 1 6.83
CHEMBL309341 1 6.79
CHEMBL73640 1 6.54
CHEMBL419814 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST Ki = 1.5 nM 8.82
CHEMBL63 ROLIPRAM Ki = 1.6 nM 8.80
CHEMBL74631 Ki = 13.0 nM 7.89
CHEMBL308407 Ki = 16.0 nM 7.80
CHEMBL308158 Ki = 46.0 nM 7.34
CHEMBL74404 Ki = 71.0 nM 7.15
CHEMBL70903 Ki = 95.0 nM 7.02
CHEMBL72362 Ki = 121.0 nM 6.92
CHEMBL70391 Ki = 149.0 nM 6.83
CHEMBL309341 Ki = 164.0 nM 6.79
CHEMBL73640 Ki = 286.0 nM 6.54
CHEMBL419814 Ki = 320.0 nM 6.50