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Assay Detail

CHEMBL4028064

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

Binding
Displacement of radiolabeled 4-(azetidin-1-yl)-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-1-(tritritiomethyl)pyrazolo[3,4-d]pyrimidine from PDE2A in monkey striatal membranes after 30 mins by liquid scintillation counting method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Tissue Striatum
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX.
J Med Chem (2018) 61 : 1001 -1018
PubMed 29293004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.26 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092562 PF-05180999 1.0 1 8.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092562 PF-05180999 Ki = 5.5 nM 8.26