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Assay Detail

CHEMBL765686

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

Binding
Inhibition of human neutrophil phosphodiesterase type IV (PDE4)
14
Total Activities
14
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
IC50 14 7.47 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL84350 1 8.70
CHEMBL450274 1 7.92
CHEMBL79661 1 7.68
CHEMBL82882 1 7.60
CHEMBL311025 1 7.55
CHEMBL421343 1 7.52
CHEMBL83872 1 7.52
CHEMBL82934 1 7.44
CHEMBL84115 1 7.29
CHEMBL70391 1 7.28
CHEMBL79739 1 7.14
CHEMBL309420 1 7.07
CHEMBL81226 1 6.95
CHEMBL81020 1 6.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL84350 IC50 = 2.0 nM 8.70
CHEMBL450274 IC50 = 12.0 nM 7.92
CHEMBL79661 IC50 = 21.0 nM 7.68
CHEMBL82882 IC50 = 25.0 nM 7.60
CHEMBL311025 IC50 = 28.0 nM 7.55
CHEMBL421343 IC50 = 30.0 nM 7.52
CHEMBL83872 IC50 = 30.0 nM 7.52
CHEMBL82934 IC50 = 36.0 nM 7.44
CHEMBL84115 IC50 = 51.0 nM 7.29
CHEMBL70391 IC50 = 53.0 nM 7.28
CHEMBL79739 IC50 = 72.0 nM 7.14
CHEMBL309420 IC50 = 85.0 nM 7.07
CHEMBL81226 IC50 = 113.0 nM 6.95
CHEMBL81020 IC50 = 131.0 nM 6.88