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Assay Detail

CHEMBL933707

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

Binding
Inhibition of PDE10A
ChEMBL ↗
54
Total Activities
27
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

CoMFA and HQSAR studies on 6,7-dimethoxy-4-pyrrolidylquinazoline derivatives as phosphodiesterase10A inhibitors.
Kulkarni SS, Patel MR, Talele TT.
Bioorg Med Chem (2008) 16 : 3675 -3686
PubMed 18299198 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 7.18 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219445 — — 2 8.40
CHEMBL410834 — — 2 7.92
CHEMBL263641 — — 2 7.92
CHEMBL409613 — — 2 7.92
CHEMBL218955 — — 2 7.77
CHEMBL409651 — — 2 7.75
CHEMBL261711 — — 2 7.75
CHEMBL220185 — — 2 7.72
CHEMBL385754 — — 2 7.36
CHEMBL375200 — — 2 7.27
CHEMBL441704 — — 2 7.25
CHEMBL408977 — — 2 7.17
CHEMBL409862 — — 2 7.17
CHEMBL219451 — — 2 7.03
CHEMBL387167 — — 2 7.00
CHEMBL259295 — — 2 6.95
CHEMBL260006 — — 2 6.91
CHEMBL374993 — — 2 6.89
CHEMBL409484 — — 2 6.89
CHEMBL218855 — — 2 6.87
CHEMBL429686 — — 2 6.77
CHEMBL430071 — — 2 6.73
CHEMBL408978 — — 2 6.70
CHEMBL263642 — — 2 6.68
CHEMBL427777 — — 2 6.62
CHEMBL262088 — — 2 6.49
CHEMBL428445 — — 2 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219445 — Ki = 4.0 nM 8.40
CHEMBL410834 — Ki = 12.0 nM 7.92
CHEMBL409613 — Ki = 12.0 nM 7.92
CHEMBL263641 — Ki = 12.0 nM 7.92
CHEMBL218955 — Ki = 17.0 nM 7.77
CHEMBL409651 — Ki = 18.0 nM 7.75
CHEMBL261711 — Ki = 18.0 nM 7.75
CHEMBL220185 — Ki = 19.0 nM 7.72
CHEMBL385754 — Ki = 44.0 nM 7.36
CHEMBL375200 — Ki = 54.0 nM 7.27
CHEMBL441704 — Ki = 56.0 nM 7.25
CHEMBL408977 — Ki = 68.0 nM 7.17
CHEMBL409862 — Ki = 67.0 nM 7.17
CHEMBL219451 — Ki = 94.0 nM 7.03
CHEMBL387167 — Ki = 100.0 nM 7.00
CHEMBL259295 — Ki = 112.0 nM 6.95
CHEMBL260006 — Ki = 123.0 nM 6.91
CHEMBL374993 — Ki = 128.0 nM 6.89
CHEMBL409484 — Ki = 130.0 nM 6.89
CHEMBL218855 — Ki = 136.0 nM 6.87
CHEMBL429686 — Ki = 171.0 nM 6.77
CHEMBL430071 — Ki = 185.0 nM 6.73
CHEMBL408978 — Ki = 198.0 nM 6.70
CHEMBL263642 — Ki = 210.0 nM 6.68
CHEMBL427777 — Ki = 240.0 nM 6.62
CHEMBL262088 — Ki = 326.0 nM 6.49
CHEMBL428445 — Ki = 811.0 nM 6.09
CHEMBL218955 — Ki = 16982436.52 nM -
CHEMBL441704 — Ki = 54954087.39 nM -
CHEMBL430071 — Ki = 181970085.86 nM -
CHEMBL387167 — Ki = 100000000.0 nM -
CHEMBL375200 — Ki = 53703179.64 nM -
CHEMBL218855 — Ki = 134896288.26 nM -
CHEMBL219451 — Ki = 93325430.08 nM -
CHEMBL409862 — Ki = 66069344.8 nM -
CHEMBL385754 — Ki = 43651583.22 nM -
CHEMBL263642 — Ki = 208929613.09 nM -
CHEMBL259295 — Ki = 109647819.61 nM -
CHEMBL410834 — Ki = 11748975.55 nM -
CHEMBL263641 — Ki = 11748975.55 nM -
CHEMBL409613 — Ki = 11748975.55 nM -
CHEMBL220185 — Ki = 18620871.37 nM -
CHEMBL219445 — Ki = 3981071.71 nM -
CHEMBL408978 — Ki = 194984459.98 nM -
CHEMBL429686 — Ki = 169824365.25 nM -
CHEMBL408977 — Ki = 67608297.54 nM -
CHEMBL260006 — Ki = 120226443.46 nM -
CHEMBL261711 — Ki = 17782794.1 nM -
CHEMBL409651 — Ki = 17782794.1 nM -
CHEMBL374993 — Ki = 125892541.18 nM -