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Assay Detail

CHEMBL764361

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Binding
In vitro inhibitory activity against Phosphodiesterase 4A (PDE4)
13
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

3',5'-cyclic-AMP phosphodiesterase 4A (CHEMBL254)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.
Ducharme Y, Friesen RW, Blouin M, Côté B, Dubé D, Ethier D, Frenette R, Laliberté F, Mancini JA, Masson P, Styhler A, Young RN, Girard Y.
Bioorg Med Chem Lett (2003) 13 : 1923 -1926
PubMed 12749899 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.41 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61191 4 9.22
CHEMBL299931 1 9.10
CHEMBL294717 1 9.10
CHEMBL301441 1 8.92
CHEMBL56971 1 8.62
CHEMBL57757 1 8.52
CHEMBL56575 1 8.22
CHEMBL57131 1 8.22
CHEMBL417776 1 7.40
CHEMBL57767 1 6.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61191 IC50 = 0.6 nM 9.22
CHEMBL299931 IC50 = 0.8 nM 9.10
CHEMBL294717 IC50 = 0.8 nM 9.10
CHEMBL61191 IC50 = 1.0 nM 9.00
CHEMBL301441 IC50 = 1.2 nM 8.92
CHEMBL61191 IC50 = 2.0 nM 8.70
CHEMBL56971 IC50 = 2.4 nM 8.62
CHEMBL57757 IC50 = 3.0 nM 8.52
CHEMBL56575 IC50 = 6.0 nM 8.22
CHEMBL57131 IC50 = 6.0 nM 8.22
CHEMBL417776 IC50 = 40.0 nM 7.40
CHEMBL61191 IC50 = 48.0 nM 7.32
CHEMBL57767 IC50 = 102.0 nM 6.99