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Assay Detail

CHEMBL763949

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Binding
Inhibition of human Phosphodiesterase 4
10
Total Activities
10
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 2: the synthesis and biological evaluation of 6-methoxy-1,4-disubstituted derivatives.
Napoletano M, Norcini G, Pellacini F, Marchini F, Morazzoni G, Ferlenga P, Pradella L.
Bioorg Med Chem Lett (2001) 11 : 33 -37
PubMed 11140727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.47 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 9.00
CHEMBL79902 1 8.40
CHEMBL79471 1 7.85
CHEMBL310387 1 7.43
CHEMBL79535 1 7.42
CHEMBL80107 1 7.32
CHEMBL70391 1 7.28
CHEMBL511115 CILOMILAST 3.0 1 7.14
CHEMBL312375 1 7.03
CHEMBL63 ROLIPRAM 2.0 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 1.0 nM 9.00
CHEMBL79902 IC50 = 4.0 nM 8.40
CHEMBL79471 IC50 = 14.0 nM 7.85
CHEMBL310387 IC50 = 37.0 nM 7.43
CHEMBL79535 IC50 = 38.0 nM 7.42
CHEMBL80107 IC50 = 48.0 nM 7.32
CHEMBL70391 IC50 = 53.0 nM 7.28
CHEMBL511115 CILOMILAST IC50 = 73.0 nM 7.14
CHEMBL312375 IC50 = 93.0 nM 7.03
CHEMBL63 ROLIPRAM IC50 = 1680.0 nM 5.78