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Assay Detail

CHEMBL5654461

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

Binding
Inhibition of rat PDE10A2 assessed as inhibition of cAMP hydrolysis by fluorescence polarization assay
2
Total Activities
1
Compounds Tested
2
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type AD293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

The novel phosphodiesterase 10A inhibitor THPP-1 has antipsychotic-like effects in rat and improves cognition in rat and rhesus monkey.
Smith SM, Uslaner JM, Cox CD, Huszar SL, Cannon CE, Vardigan JD, Eddins D, Toolan DM, Kandebo M, Yao L, Raheem IT, Schreier JD, Breslin MJ, Coleman PJ, Renger JJ.
Neuropharmacology (2013) 64 : 215 -223
PubMed 22750078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.89 8.89
Inhibition 1 - -

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - MONDO:0005090
EFO_TERM EFO_TERM - schizophrenia

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204538 THPP-1 2 8.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204538 THPP-1 Ki = 1.3 nM 8.89
CHEMBL2204538 THPP-1 Inhibition - % -