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Assay Detail

CHEMBL765475

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

Binding
Inhibitory activity against Phosphodiesterase 4A (PDE4A) from human source expressed in Saccharomyces cerevisiae
16
Total Activities
16
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

Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
Hersperger R, Bray-French K, Mazzoni L, Müller T.
J Med Chem (2000) 43 : 675 -682
PubMed 10691693 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.27 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL161115 1 7.23
CHEMBL74078 1 7.06
CHEMBL351613 1 6.92
CHEMBL161740 1 6.85
CHEMBL351500 1 6.55
CHEMBL161465 1 6.46
CHEMBL511115 CILOMILAST 3.0 1 6.39
CHEMBL158286 1 6.11
CHEMBL161714 1 5.85
CHEMBL63 ROLIPRAM 2.0 1 5.85
CHEMBL351900 1 5.75
CHEMBL345360 1 5.42
CHEMBL162188 1 5.02
CHEMBL351915 1 -
CHEMBL345812 1 -
CHEMBL161602 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL161115 IC50 = 59.0 nM 7.23
CHEMBL74078 IC50 = 88.0 nM 7.06
CHEMBL351613 IC50 = 120.0 nM 6.92
CHEMBL161740 IC50 = 140.0 nM 6.85
CHEMBL351500 IC50 = 279.0 nM 6.55
CHEMBL161465 IC50 = 350.0 nM 6.46
CHEMBL511115 CILOMILAST IC50 = 410.0 nM 6.39
CHEMBL158286 IC50 = 770.0 nM 6.11
CHEMBL161714 IC50 = 1400.0 nM 5.85
CHEMBL63 ROLIPRAM IC50 = 1400.0 nM 5.85
CHEMBL351900 IC50 = 1800.0 nM 5.75
CHEMBL345360 IC50 = 3800.0 nM 5.42
CHEMBL162188 IC50 = 9500.0 nM 5.02
CHEMBL351915 IC50 > 10000.0 nM -
CHEMBL345812 IC50 > 10000.0 nM -
CHEMBL161602 IC50 > 10000.0 nM -