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Assay Detail

CHEMBL803572

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

Binding
Displacement of [3H]rolipram from rat brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2094267)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
Dal Piaz V, Giovannoni MP, Castellana C, Palacios JM, Beleta J, Doménech T, Segarra V.
J Med Chem (1997) 40 : 1417 -1421
PubMed 9154964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.32 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414613 1 8.32
CHEMBL63 ROLIPRAM 2.0 1 8.22
CHEMBL283179 1 6.40
CHEMBL33501 1 6.00
CHEMBL31725 1 6.00
CHEMBL30894 1 5.80
CHEMBL29546 1 5.75
CHEMBL285457 1 5.70
CHEMBL30593 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414613 IC50 = 4.8 nM 8.32
CHEMBL63 ROLIPRAM IC50 = 6.0 nM 8.22
CHEMBL283179 IC50 = 400.0 nM 6.40
CHEMBL33501 IC50 = 1000.0 nM 6.00
CHEMBL31725 IC50 = 1000.0 nM 6.00
CHEMBL30894 IC50 = 1600.0 nM 5.80
CHEMBL29546 IC50 = 1800.0 nM 5.75
CHEMBL285457 IC50 = 2000.0 nM 5.70
CHEMBL30593 IC50 = 22000.0 nM 4.66