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Assay Detail

CHEMBL5732355

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

Binding
Fluorescence Polarization Assay: The fluorescence polarization assay for cyclic nucleotide phosphodiesterases was performed using an IMAP® FP kit supplied by Molecular Devices, Sunnyvale, Calif. (product # R8139). IMAP® technology has been applied previously to phosphodiesterase assays (Huang, W., et al., J. Biomol Screen, 2002, 7: 215). Assays were performed at room temperature in 384-well microtiter plates with an incubation volume of 20.2 μL. Solutions of test compounds were prepared in DMSO and serially diluted with DMSO to yield 8 μL of each of 10 solutions differing by 3-fold in concentration, at 32 serial dilutions per plate. 100% inhibition is determined using a known PDE10 inhibitor, which can be any compound that is present at 5,000 times its Ki value in the assay described as follows, such as papaverine (see Siuciak, et al. Neuropharmacology (2006) 51:386-396; Becker, et al. Behav Brain Res (2008) 186(2):155-60;
ChEMBL ↗
771
Total Activities
223
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A (CHEMBL4409) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrimidine PDE10 inhibitors
(2017)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 257 8.91 11.00
kon 257 - -
k_off 257 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5795042 — — 6 11.00
CHEMBL5976716 — — 3 11.00
CHEMBL5996071 — — 3 11.00
CHEMBL5897423 — — 3 11.00
CHEMBL5856126 — — 3 11.00
CHEMBL5874748 — — 6 11.00
CHEMBL5891871 — — 6 10.70
CHEMBL5758106 — — 3 10.70
CHEMBL5845887 — — 3 10.70
CHEMBL6051772 — — 3 10.70
CHEMBL5831353 — — 6 10.70
CHEMBL6021729 — — 3 10.70
CHEMBL6040794 — — 6 10.52
CHEMBL5819141 — — 3 10.40
CHEMBL5992443 — — 12 10.40
CHEMBL5793385 — — 3 10.40
CHEMBL5997844 — — 6 10.40
CHEMBL6057423 — — 6 10.30
CHEMBL5935596 — — 6 10.22
CHEMBL5792969 — — 3 10.22
CHEMBL5799504 — — 3 10.22
CHEMBL5841556 — — 3 10.22
CHEMBL5955757 — — 3 10.22
CHEMBL5929346 — — 3 10.22
CHEMBL5888469 — — 3 10.15
CHEMBL5996245 — — 6 10.10
CHEMBL5985502 — — 6 10.05
CHEMBL5746690 — — 6 10.00
CHEMBL5860083 — — 6 10.00
CHEMBL5972620 — — 3 10.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5996071 — Ki = 0.01 nM 11.00
CHEMBL5897423 — Ki = 0.01 nM 11.00
CHEMBL5874748 — Ki = 0.01 nM 11.00
CHEMBL5795042 — Ki = 0.01 nM 11.00
CHEMBL5976716 — Ki = 0.01 nM 11.00
CHEMBL5856126 — Ki = 0.01 nM 11.00
CHEMBL5845887 — Ki = 0.02 nM 10.70
CHEMBL5758106 — Ki = 0.02 nM 10.70
CHEMBL6021729 — Ki = 0.02 nM 10.70
CHEMBL5831353 — Ki = 0.02 nM 10.70
CHEMBL6051772 — Ki = 0.02 nM 10.70
CHEMBL5891871 — Ki = 0.02 nM 10.70
CHEMBL6040794 — Ki = 0.03 nM 10.52
CHEMBL5819141 — Ki = 0.04 nM 10.40
CHEMBL5992443 — Ki = 0.04 nM 10.40
CHEMBL5793385 — Ki = 0.04 nM 10.40
CHEMBL5997844 — Ki = 0.04 nM 10.40
CHEMBL6057423 — Ki = 0.05 nM 10.30
CHEMBL5992443 — Ki = 0.05 nM 10.30
CHEMBL5792969 — Ki = 0.06 nM 10.22
CHEMBL5955757 — Ki = 0.06 nM 10.22
CHEMBL5929346 — Ki = 0.06 nM 10.22
CHEMBL5935596 — Ki = 0.06 nM 10.22
CHEMBL5841556 — Ki = 0.06 nM 10.22
CHEMBL5799504 — Ki = 0.06 nM 10.22
CHEMBL5888469 — Ki = 0.07 nM 10.15
CHEMBL5996245 — Ki = 0.08 nM 10.10
CHEMBL5985502 — Ki = 0.09 nM 10.05
CHEMBL5746690 — Ki = 0.1 nM 10.00
CHEMBL6055492 — Ki = 0.1 nM 10.00
CHEMBL5972620 — Ki = 0.1 nM 10.00
CHEMBL5860083 — Ki = 0.1 nM 10.00
CHEMBL5802534 — Ki = 0.12 nM 9.92
CHEMBL5759057 — Ki = 0.12 nM 9.92
CHEMBL5971687 — Ki = 0.12 nM 9.92
CHEMBL6026354 — Ki = 0.13 nM 9.89
CHEMBL5781827 — Ki = 0.13 nM 9.89
CHEMBL6053246 — Ki = 0.14 nM 9.85
CHEMBL5835403 — Ki = 0.14 nM 9.85
CHEMBL5920732 — Ki = 0.15 nM 9.82
CHEMBL5769566 — Ki = 0.15 nM 9.82
CHEMBL6045583 — Ki = 0.16 nM 9.80
CHEMBL5921583 — Ki = 0.16 nM 9.80
CHEMBL6021229 — Ki = 0.18 nM 9.74
CHEMBL5953108 — Ki = 0.2 nM 9.70
CHEMBL5802405 — Ki = 0.2 nM 9.70
CHEMBL5969406 — Ki = 0.23 nM 9.64
CHEMBL6026354 — Ki = 0.24 nM 9.62
CHEMBL6053246 — Ki = 0.24 nM 9.62
CHEMBL6013103 — Ki = 0.25 nM 9.60