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Assay Detail

CHEMBL3742723

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

Binding
Inhibition of human recombinant PDE10A1 expressed in baculovirus infected insect SF21 cells using [3H]cAMP as substrate after 30 mins by scintillation proximity assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf21
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Development of highly potent phosphodiesterase 10A (PDE10A) inhibitors: Synthesis and in vitro evaluation of 1,8-dipyridinyl- and 1-pyridinyl-substituted imidazo[1,5-a]quinoxalines.
Wagner S, Scheunemann M, Dipper K, Egerland U, Hoefgen N, Steinbach J, Brust P.
Eur J Med Chem (2016) 107 : 97 -108
PubMed 26562545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.95 10.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3741573 1 10.43
CHEMBL3741841 1 10.32
CHEMBL3742354 1 9.96
CHEMBL3741950 1 9.92
CHEMBL3739783 1 9.48
CHEMBL3741781 1 9.39
CHEMBL3741660 1 9.34
CHEMBL3741492 1 9.06
CHEMBL3741207 1 9.00
CHEMBL3741064 1 8.80
CHEMBL3741518 1 8.77
CHEMBL3739662 1 8.53
CHEMBL3741528 1 8.50
CHEMBL3741850 1 8.48
CHEMBL3741836 1 7.99
CHEMBL219445 1 7.80
CHEMBL3742381 1 7.69
CHEMBL3741213 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3741573 IC50 = 0.037 nM 10.43
CHEMBL3741841 IC50 = 0.048 nM 10.32
CHEMBL3742354 IC50 = 0.11 nM 9.96
CHEMBL3741950 IC50 = 0.12 nM 9.92
CHEMBL3739783 IC50 = 0.33 nM 9.48
CHEMBL3741781 IC50 = 0.41 nM 9.39
CHEMBL3741660 IC50 = 0.46 nM 9.34
CHEMBL3741492 IC50 = 0.87 nM 9.06
CHEMBL3741207 IC50 = 0.99 nM 9.00
CHEMBL3741064 IC50 = 1.57 nM 8.80
CHEMBL3741518 IC50 = 1.69 nM 8.77
CHEMBL3739662 IC50 = 2.95 nM 8.53
CHEMBL3741528 IC50 = 3.18 nM 8.50
CHEMBL3741850 IC50 = 3.3 nM 8.48
CHEMBL3741836 IC50 = 10.3 nM 7.99
CHEMBL219445 IC50 = 16.0 nM 7.80
CHEMBL3742381 IC50 = 20.4 nM 7.69
CHEMBL3741213 IC50 = 26.3 nM 7.58