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Assay Detail

CHEMBL760585

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

Binding
In vitro inhibition of phosphodiesterase (PDE V).
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazotriazinone inhibitors of the Ca2+-calmodulin sensitive phosphodiesterase (PDE I)
Hlasta DJ, Bode DC, Court JJ, Desai RC, Pagani ED, Silver PJ
Bioorg Med Chem Lett (1997) 7 : 89 -94
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.03 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL28079 ZAPRINAST 2.0 1 6.52
CHEMBL173510 1 5.77
CHEMBL173317 1 5.54
CHEMBL367927 1 5.51
CHEMBL366938 1 5.41
CHEMBL426946 1 5.01
CHEMBL174270 1 4.92
CHEMBL176346 1 4.83
CHEMBL354843 1 4.75
CHEMBL355748 1 4.74
CHEMBL366999 1 4.71
CHEMBL366491 1 4.67
CHEMBL368198 1 4.64
CHEMBL368322 1 4.25
CHEMBL369431 1 4.18
CHEMBL369172 1 -
CHEMBL367221 1 -
CHEMBL173275 1 -
CHEMBL369830 1 -
CHEMBL170449 1 -
CHEMBL426937 1 -
CHEMBL170228 1 -
CHEMBL440593 CI-930 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL28079 ZAPRINAST IC50 = 300.0 nM 6.52
CHEMBL173510 IC50 = 1700.0 nM 5.77
CHEMBL173317 IC50 = 2900.0 nM 5.54
CHEMBL367927 IC50 = 3100.0 nM 5.51
CHEMBL366938 IC50 = 3900.0 nM 5.41
CHEMBL426946 IC50 = 9700.0 nM 5.01
CHEMBL174270 IC50 = 12100.0 nM 4.92
CHEMBL176346 IC50 = 14900.0 nM 4.83
CHEMBL354843 IC50 = 17700.0 nM 4.75
CHEMBL355748 IC50 = 18200.0 nM 4.74
CHEMBL366999 IC50 = 19700.0 nM 4.71
CHEMBL366491 IC50 = 21200.0 nM 4.67
CHEMBL368198 IC50 = 22700.0 nM 4.64
CHEMBL368322 IC50 = 56100.0 nM 4.25
CHEMBL369431 IC50 = 66700.0 nM 4.18
CHEMBL369172 IC50 > 100000.0 nM -
CHEMBL367221 IC50 > 10000.0 nM -
CHEMBL173275 IC50 > 10000.0 nM -
CHEMBL369830 IC50 > 30000.0 nM -
CHEMBL170449 IC50 > 10000.0 nM -
CHEMBL426937 IC50 > 30000.0 nM -
CHEMBL170228 IC50 > 10000.0 nM -
CHEMBL440593 CI-930 IC50 > 10000.0 nM -