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Assay Detail

CHEMBL758018

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

Binding
Inhibitory activity against rat heart Phosphodiesterase 1(PDE1)
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Phosphodiesterase 1 (CHEMBL2111322)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.
Ukita T, Nakamura Y, Kubo A, Yamamoto Y, Moritani Y, Saruta K, Higashijima T, Kotera J, Takagi M, Kikkawa K, Omori K.
J Med Chem (2001) 44 : 2204 -2218
PubMed 11405657 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 5.79 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192 SILDENAFIL 4.0 1 6.52
CHEMBL538498 1 6.34
CHEMBL542394 1 6.26
CHEMBL543818 1 6.00
CHEMBL541818 1 5.96
CHEMBL553371 1 5.89
CHEMBL70432 1 5.68
CHEMBL540539 1 5.68
CHEMBL423125 1 5.58
CHEMBL305028 1 5.51
CHEMBL544289 1 5.41
CHEMBL538505 1 5.41
CHEMBL553786 1 5.02
CHEMBL539779 1 -
CHEMBL70382 1 -
CHEMBL545221 1 -
CHEMBL68106 1 -
CHEMBL305014 1 -
CHEMBL71949 1 -
CHEMBL305206 1 -
CHEMBL72423 1 -
CHEMBL544057 1 -
CHEMBL539010 1 -
CHEMBL543351 1 -
CHEMBL542878 1 -
CHEMBL430421 1 -
CHEMBL72875 1 -
CHEMBL305427 1 -
CHEMBL69502 1 -
CHEMBL544995 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192 SILDENAFIL IC50 = 300.0 nM 6.52
CHEMBL538498 IC50 = 460.0 nM 6.34
CHEMBL542394 IC50 = 550.0 nM 6.26
CHEMBL543818 IC50 = 1000.0 nM 6.00
CHEMBL541818 IC50 = 1100.0 nM 5.96
CHEMBL553371 IC50 = 1300.0 nM 5.89
CHEMBL70432 IC50 = 2100.0 nM 5.68
CHEMBL540539 IC50 = 2100.0 nM 5.68
CHEMBL423125 IC50 = 2600.0 nM 5.58
CHEMBL305028 IC50 = 3100.0 nM 5.51
CHEMBL538505 IC50 = 3900.0 nM 5.41
CHEMBL544289 IC50 = 3900.0 nM 5.41
CHEMBL553786 IC50 = 9500.0 nM 5.02
CHEMBL539519 IC50 > 10000.0 nM -
CHEMBL553083 IC50 > 10000.0 nM -
CHEMBL71478 IC50 > 10000.0 nM -
CHEMBL68388 IC50 > 10000.0 nM -
CHEMBL539779 IC50 > 10000.0 nM -
CHEMBL70382 IC50 > 10000.0 nM -
CHEMBL545221 IC50 > 10000.0 nM -
CHEMBL68106 IC50 > 10000.0 nM -
CHEMBL305014 IC50 > 10000.0 nM -
CHEMBL71949 IC50 > 10000.0 nM -
CHEMBL305206 IC50 > 10000.0 nM -
CHEMBL72423 IC50 > 10000.0 nM -
CHEMBL544057 IC50 > 10000.0 nM -
CHEMBL539010 IC50 > 10000.0 nM -
CHEMBL543351 IC50 > 10000.0 nM -
CHEMBL542878 IC50 > 10000.0 nM -
CHEMBL430421 IC50 > 10000.0 nM -
CHEMBL72875 IC50 > 10000.0 nM -
CHEMBL305427 IC50 > 10000.0 nM -
CHEMBL69502 IC50 > 10000.0 nM -
CHEMBL544995 IC50 > 10000.0 nM -