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Assay Detail

CHEMBL933708

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

Binding
Inhibition of PDE3A
27
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

cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241)
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 27 6.72 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263642 1 7.32
CHEMBL219451 1 7.21
CHEMBL260006 1 7.11
CHEMBL263641 1 6.98
CHEMBL409862 1 6.92
CHEMBL408977 1 6.85
CHEMBL409651 1 6.82
CHEMBL220185 1 6.82
CHEMBL375200 1 6.79
CHEMBL385754 1 6.79
CHEMBL261711 1 6.70
CHEMBL219445 1 6.68
CHEMBL409613 1 6.68
CHEMBL441704 1 6.67
CHEMBL259295 1 6.65
CHEMBL218855 1 6.57
CHEMBL218955 1 6.56
CHEMBL410834 1 6.55
CHEMBL374993 1 6.52
CHEMBL429686 1 6.43
CHEMBL387167 1 6.14
CHEMBL430071 1 6.13
CHEMBL428445 1 -
CHEMBL408978 1 -
CHEMBL409484 1 -
CHEMBL427777 1 -
CHEMBL262088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263642 Ki = 48.0 nM 7.32
CHEMBL219451 Ki = 61.0 nM 7.21
CHEMBL260006 Ki = 77.0 nM 7.11
CHEMBL263641 Ki = 104.0 nM 6.98
CHEMBL409862 Ki = 121.0 nM 6.92
CHEMBL408977 Ki = 141.0 nM 6.85
CHEMBL409651 Ki = 152.0 nM 6.82
CHEMBL220185 Ki = 151.0 nM 6.82
CHEMBL375200 Ki = 161.0 nM 6.79
CHEMBL385754 Ki = 162.0 nM 6.79
CHEMBL261711 Ki = 199.0 nM 6.70
CHEMBL219445 Ki = 211.0 nM 6.68
CHEMBL409613 Ki = 209.0 nM 6.68
CHEMBL441704 Ki = 214.0 nM 6.67
CHEMBL259295 Ki = 226.0 nM 6.65
CHEMBL218855 Ki = 271.0 nM 6.57
CHEMBL218955 Ki = 273.0 nM 6.56
CHEMBL410834 Ki = 283.0 nM 6.55
CHEMBL374993 Ki = 302.0 nM 6.52
CHEMBL429686 Ki = 370.0 nM 6.43
CHEMBL387167 Ki = 720.0 nM 6.14
CHEMBL430071 Ki = 739.0 nM 6.13
CHEMBL428445 Ki < 100.0 nM -
CHEMBL408978 Ki < 100.0 nM -
CHEMBL409484 Ki < 100.0 nM -
CHEMBL427777 Ki < 100.0 nM -
CHEMBL262088 Ki < 100.0 nM -