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Assay Detail

CHEMBL764847

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Binding
Inhibition of rolipram binding to Phosphodiesterase 4
3
Total Activities
3
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

Phthalazine PDE4 inhibitors. Part 3: the synthesis and in vitro evaluation of derivatives with a hydrogen bond acceptor.
Napoletano M, Norcini G, Pellacini F, Marchini F, Morazzoni G, Fattori R, Ferlenga P, Pradella L.
Bioorg Med Chem Lett (2002) 12 : 5 -8
PubMed 11738561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.35 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 8.82
CHEMBL63 ROLIPRAM 2.0 1 8.80
CHEMBL511115 CILOMILAST 3.0 1 7.42

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
CHEMBL511115 CILOMILAST Ki = 38.0 nM 7.42