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Assay Detail

CHEMBL933709

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

Binding
Inhibition of PDE3B
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 3B (CHEMBL290)
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 6.49 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL263642 1 7.25
CHEMBL219451 1 7.06
CHEMBL220185 1 6.71
CHEMBL263641 1 6.70
CHEMBL260006 1 6.68
CHEMBL409651 1 6.65
CHEMBL409613 1 6.62
CHEMBL408977 1 6.62
CHEMBL409862 1 6.58
CHEMBL219445 1 6.56
CHEMBL261711 1 6.55
CHEMBL218855 1 6.55
CHEMBL218955 1 6.52
CHEMBL375200 1 6.48
CHEMBL385754 1 6.48
CHEMBL441704 1 6.33
CHEMBL410834 1 6.33
CHEMBL429686 1 6.32
CHEMBL259295 1 6.16
CHEMBL374993 1 6.13
CHEMBL430071 1 5.74
CHEMBL387167 1 5.72
CHEMBL428445 1 -
CHEMBL408978 1 -
CHEMBL409484 1 -
CHEMBL427777 1 -
CHEMBL262088 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL263642 Ki = 56.0 nM 7.25
CHEMBL219451 Ki = 88.0 nM 7.06
CHEMBL220185 Ki = 196.0 nM 6.71
CHEMBL263641 Ki = 201.0 nM 6.70
CHEMBL260006 Ki = 207.0 nM 6.68
CHEMBL409651 Ki = 223.0 nM 6.65
CHEMBL409613 Ki = 240.0 nM 6.62
CHEMBL408977 Ki = 237.0 nM 6.62
CHEMBL409862 Ki = 260.0 nM 6.58
CHEMBL219445 Ki = 273.0 nM 6.56
CHEMBL261711 Ki = 280.0 nM 6.55
CHEMBL218855 Ki = 280.0 nM 6.55
CHEMBL218955 Ki = 305.0 nM 6.52
CHEMBL375200 Ki = 328.0 nM 6.48
CHEMBL385754 Ki = 332.0 nM 6.48
CHEMBL441704 Ki = 471.0 nM 6.33
CHEMBL410834 Ki = 463.0 nM 6.33
CHEMBL429686 Ki = 474.0 nM 6.32
CHEMBL259295 Ki = 685.0 nM 6.16
CHEMBL374993 Ki = 748.0 nM 6.13
CHEMBL430071 Ki = 1820.0 nM 5.74
CHEMBL387167 Ki = 1890.0 nM 5.72
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 -