Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3887631

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

Binding
Fluorescence Polarization Assay: In a typical experiment the PDE10 inhibitory activity of the compounds of the present invention was determined in accordance with the following experimental method. PDE10A2 was amplified from human fetal brain cDNA (Clontech, Mountain View, Calif.) using a forward primer corresponding to nucleotides 56-77 of human PDE10A2 (Accession No. AF127480, Genbank Identifier 4894716), containing a Kozak consensus sequence, and a reverse primer corresponding to nucleotides 2406-2413 of human PDE10A2 (Accession No. AF127480, Genbank Identifier 4894716). Amplification with Easy-A polymerase (Stratagene, La Jolla, Calif.) was 95° C. for 2 minutes followed by thirty three cycles of 95° C. for 40 seconds, 55° C. for 30 seconds, and 72° C. for 2 minutes 48 seconds. Final extension was 72° C. for 7 minutes. The PCR product was TA cloned into pcDNA3.2-TOPO (Invitrogen, Carlsbad, Calif.) according to standard protocol. AD293 cells with 70-80% confluency were transiently transfected with human PDE10A2.
ChEMBL ↗
119
Total Activities
117
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type AD293
Confidence 8 — Homologous 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

Triazolyl PDE10 inhibitors
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 119 8.60 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3960405 — — 1 11.00
CHEMBL3955247 — — 1 10.64
CHEMBL3972719 — — 1 10.57
CHEMBL3926763 — — 1 10.57
CHEMBL3983406 — — 1 10.55
CHEMBL3896176 — — 1 10.25
CHEMBL3890836 — — 1 10.17
CHEMBL3958142 — — 1 10.14
CHEMBL4115603 — — 1 10.07
CHEMBL3895140 — — 1 9.96
CHEMBL3931733 — — 1 9.85
CHEMBL3957122 — — 1 9.85
CHEMBL3904978 — — 1 9.68
CHEMBL3936634 — — 1 9.68
CHEMBL4108151 — — 1 9.43
CHEMBL4109746 — — 1 9.43
CHEMBL3934159 — — 1 9.41
CHEMBL4107645 — — 1 9.40
CHEMBL4108605 — — 1 9.38
CHEMBL4108200 — — 1 9.31
CHEMBL3906186 — — 1 9.30
CHEMBL4108061 — — 1 9.27
CHEMBL4110889 — — 1 9.24
CHEMBL3978832 — — 1 9.21
CHEMBL4111026 — — 1 9.20
CHEMBL3956689 — — 1 9.17
CHEMBL4113388 — — 1 9.12
CHEMBL4107845 — — 1 9.11
CHEMBL3967410 — — 1 9.09
CHEMBL4109751 — — 1 9.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3960405 — Ki = 0.01 nM 11.00
CHEMBL3955247 — Ki = 0.023 nM 10.64
CHEMBL3926763 — Ki = 0.027 nM 10.57
CHEMBL3972719 — Ki = 0.027 nM 10.57
CHEMBL3983406 — Ki = 0.028 nM 10.55
CHEMBL3896176 — Ki = 0.056 nM 10.25
CHEMBL3890836 — Ki = 0.068 nM 10.17
CHEMBL3958142 — Ki = 0.073 nM 10.14
CHEMBL4115603 — Ki = 0.085 nM 10.07
CHEMBL3895140 — Ki = 0.11 nM 9.96
CHEMBL3931733 — Ki = 0.14 nM 9.85
CHEMBL3957122 — Ki = 0.14 nM 9.85
CHEMBL3904978 — Ki = 0.21 nM 9.68
CHEMBL3936634 — Ki = 0.21 nM 9.68
CHEMBL4108151 — Ki = 0.37 nM 9.43
CHEMBL4109746 — Ki = 0.37 nM 9.43
CHEMBL3934159 — Ki = 0.39 nM 9.41
CHEMBL4107645 — Ki = 0.4 nM 9.40
CHEMBL4108605 — Ki = 0.42 nM 9.38
CHEMBL4108200 — Ki = 0.49 nM 9.31
CHEMBL3906186 — Ki = 0.5 nM 9.30
CHEMBL4108061 — Ki = 0.54 nM 9.27
CHEMBL4110889 — Ki = 0.58 nM 9.24
CHEMBL3978832 — Ki = 0.62 nM 9.21
CHEMBL4111026 — Ki = 0.63 nM 9.20
CHEMBL3956689 — Ki = 0.68 nM 9.17
CHEMBL4113388 — Ki = 0.75 nM 9.12
CHEMBL4107845 — Ki = 0.77 nM 9.11
CHEMBL3967410 — Ki = 0.82 nM 9.09
CHEMBL4109751 — Ki = 0.84 nM 9.08
CHEMBL4112619 — Ki = 0.88 nM 9.06
CHEMBL3935319 — Ki = 0.9 nM 9.05
CHEMBL3923133 — Ki = 0.96 nM 9.02
CHEMBL4111261 — Ki = 1.08 nM 8.97
CHEMBL4110947 — Ki = 1.1 nM 8.96
CHEMBL4107952 — Ki = 1.1 nM 8.96
CHEMBL3970392 — Ki = 1.1 nM 8.96
CHEMBL4107251 — Ki = 1.09 nM 8.96
CHEMBL3890395 — Ki = 1.2 nM 8.92
CHEMBL3946887 — Ki = 1.2 nM 8.92
CHEMBL3982870 — Ki = 1.2 nM 8.92
CHEMBL3945473 — Ki = 1.2 nM 8.92
CHEMBL4111365 — Ki = 1.3 nM 8.89
CHEMBL3934608 — Ki = 1.3 nM 8.89
CHEMBL3902562 — Ki = 1.4 nM 8.85
CHEMBL4112502 — Ki = 1.4 nM 8.85
CHEMBL3912270 — Ki = 1.4 nM 8.85
CHEMBL3892748 — Ki = 1.5 nM 8.82
CHEMBL3971216 — Ki = 1.6 nM 8.80
CHEMBL3974865 — Ki = 1.7 nM 8.77