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Assay Detail

CHEMBL768861

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

Binding
Displacement of [3H]rolipram binding to Phosphodiesterase 4 in rat brain
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Phosphodiesterase 4 (CHEMBL2094267)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationship of quinazolinedione inhibitors of calcium-independent phosphodiesterase.
Lowe JA, Archer RL, Chapin DS, Chen JB, Helweg D, Johnson JL, Koe BK, Lebel LA, Moore PF, Nielsen JA.
J Med Chem (1991) 34 : 624 -628
PubMed 1995886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.26 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL156140 1 8.89
CHEMBL351567 1 8.60
CHEMBL63 ROLIPRAM 2.0 1 8.59
CHEMBL345917 1 8.49
CHEMBL351568 1 6.75
CHEMBL156328 1 -
CHEMBL88990 NITRAQUAZONE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL156140 IC50 = 1.3 nM 8.89
CHEMBL351567 IC50 = 2.5 nM 8.60
CHEMBL63 ROLIPRAM IC50 = 2.6 nM 8.59
CHEMBL345917 IC50 = 3.2 nM 8.49
CHEMBL351568 IC50 = 180.0 nM 6.75
CHEMBL156328 IC50 > 1000.0 nM -
CHEMBL88990 NITRAQUAZONE IC50 = 14.0 nM -