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Assay Detail

CHEMBL3888565

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).
ChEMBL ↗
130
Total Activities
130
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Substituted pyridizinone derivatives as PDE10 inhibitors
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 130 9.34 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4111794 — — 1 11.00
CHEMBL4108340 — — 1 10.96
CHEMBL4111052 — — 1 10.89
CHEMBL4107863 — — 1 10.85
CHEMBL4110637 — — 1 10.82
CHEMBL4107675 — — 1 10.72
CHEMBL4108308 — — 1 10.72
CHEMBL4110725 — — 1 10.70
CHEMBL4112137 — — 1 10.68
CHEMBL4106926 — — 1 10.68
CHEMBL4115367 — — 1 10.64
CHEMBL4115428 — — 1 10.60
CHEMBL4107437 — — 1 10.57
CHEMBL4111148 — — 1 10.55
CHEMBL4115264 — — 1 10.49
CHEMBL4113390 — — 1 10.48
CHEMBL4107436 — — 1 10.47
CHEMBL4115613 — — 1 10.43
CHEMBL4108702 — — 1 10.41
CHEMBL4112972 — — 1 10.36
CHEMBL4111447 — — 1 10.35
CHEMBL4111512 — — 1 10.34
CHEMBL4109869 — — 1 10.32
CHEMBL4111868 — — 1 10.32
CHEMBL4110322 — — 1 10.31
CHEMBL4106874 — — 1 10.29
CHEMBL4111601 — — 1 10.28
CHEMBL4110881 — — 1 10.25
CHEMBL4110720 — — 1 10.24
CHEMBL4107850 — — 1 10.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4111794 — Ki = 0.01 nM 11.00
CHEMBL4108340 — Ki = 0.011 nM 10.96
CHEMBL4111052 — Ki = 0.013 nM 10.89
CHEMBL4107863 — Ki = 0.014 nM 10.85
CHEMBL4110637 — Ki = 0.015 nM 10.82
CHEMBL4108308 — Ki = 0.019 nM 10.72
CHEMBL4107675 — Ki = 0.019 nM 10.72
CHEMBL4110725 — Ki = 0.02 nM 10.70
CHEMBL4112137 — Ki = 0.021 nM 10.68
CHEMBL4106926 — Ki = 0.021 nM 10.68
CHEMBL4115367 — Ki = 0.023 nM 10.64
CHEMBL4115428 — Ki = 0.025 nM 10.60
CHEMBL4107437 — Ki = 0.027 nM 10.57
CHEMBL4111148 — Ki = 0.028 nM 10.55
CHEMBL4115264 — Ki = 0.032 nM 10.49
CHEMBL4113390 — Ki = 0.033 nM 10.48
CHEMBL4107436 — Ki = 0.034 nM 10.47
CHEMBL4115613 — Ki = 0.037 nM 10.43
CHEMBL4108702 — Ki = 0.039 nM 10.41
CHEMBL4112972 — Ki = 0.044 nM 10.36
CHEMBL4111447 — Ki = 0.045 nM 10.35
CHEMBL4111512 — Ki = 0.046 nM 10.34
CHEMBL4111868 — Ki = 0.048 nM 10.32
CHEMBL4109869 — Ki = 0.048 nM 10.32
CHEMBL4110322 — Ki = 0.049 nM 10.31
CHEMBL4106874 — Ki = 0.051 nM 10.29
CHEMBL4111601 — Ki = 0.053 nM 10.28
CHEMBL4110881 — Ki = 0.056 nM 10.25
CHEMBL4110720 — Ki = 0.058 nM 10.24
CHEMBL4107850 — Ki = 0.064 nM 10.19
CHEMBL4109682 — Ki = 0.066 nM 10.18
CHEMBL4110243 — Ki = 0.072 nM 10.14
CHEMBL4108758 — Ki = 0.074 nM 10.13
CHEMBL3894579 — Ki = 0.077 nM 10.11
CHEMBL4113054 — Ki = 0.0819 nM 10.09
CHEMBL4109656 — Ki = 0.089 nM 10.05
CHEMBL4113684 — Ki = 0.089 nM 10.05
CHEMBL4107617 — Ki = 0.097 nM 10.01
CHEMBL4108300 — Ki = 0.099 nM 10.00
CHEMBL4110565 — Ki = 0.1 nM 10.00
CHEMBL4109417 — Ki = 0.109 nM 9.96
CHEMBL3892294 — Ki = 0.118 nM 9.93
CHEMBL4107568 — Ki = 0.121 nM 9.92
CHEMBL4113100 — Ki = 0.122 nM 9.91
CHEMBL4107208 — Ki = 0.138 nM 9.86
CHEMBL4112170 — Ki = 0.144 nM 9.84
CHEMBL4106622 — Ki = 0.157 nM 9.80
CHEMBL4107418 — Ki = 0.175 nM 9.76
CHEMBL4107666 — Ki = 0.176 nM 9.75
CHEMBL4114936 — Ki = 0.192 nM 9.72