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Assay Detail

CHEMBL857568

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

Binding
Inhibition of partially-purified PDE 4 from human monocytes
4
Total Activities
4
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

The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.
Baures PW, Eggleston DS, Erhard KF, Cieslinski LB, Torphy TJ, Christensen SB.
J Med Chem (1993) 36 : 3274 -3277
PubMed 8230117 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.14 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109965 1 6.77
CHEMBL326068 1 6.13
CHEMBL430893 (-)-ROLIPRAM 1 5.85
CHEMBL325795 S-ROLIPRAM 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109965 IC50 = 170.0 nM 6.77
CHEMBL326068 IC50 = 740.0 nM 6.13
CHEMBL430893 (-)-ROLIPRAM IC50 = 1400.0 nM 5.85
CHEMBL325795 S-ROLIPRAM IC50 = 1600.0 nM 5.80