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Assay Detail

CHEMBL3383097

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

Functional
In-vivo occupancy at PDE2 in sc dosed Wistar rat brain using [3H]labeled compound in presence of 2.5 mg/kg, sc PDE10 inhibitor MP10
2
Total Activities
1
Compounds Tested
2
Activity Types
2
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Autocuration

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.
Buijnsters P, De Angelis M, Langlois X, Rombouts FJ, Sanderson W, Tresadern G, Ritchie A, Trabanco AA, VanHoof G, Roosbroeck YV, Andrés JI.
ACS Med Chem Lett (2014) 5 : 1049 -1053
PubMed 25221665 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
ED50 1 - -
EC50 1 7.68 7.68

Assay Parameters

Parameter Type Value Units Text
DOSE DOSE 2.5 mg.kg-1
ROUTE ROUTE - Subcutaneous

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3331521 2 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3331521 EC50 = 21.0 nM 7.68
CHEMBL3331521 ED50 = 4.3 mg.kg-1 -