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Assay Detail

CHEMBL762829

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

Binding
Inhibitory activity against human platelet Phosphodiesterase 5 (PDE5)
43
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

8-Aryl xanthines potent inhibitors of phosphodiesterase 5.
Arnold R, Beer D, Bhalay G, Baettig U, Collingwood SP, Craig S, Devereux N, Dunstan A, Glen A, Gomez S, Haberthuer S, Howe T, Jelfs S, Moser H, Naef R, Nicklin P, Sandham D, Stringer R, Turner K, Watson S, Zurini M.
Bioorg Med Chem Lett (2002) 12 : 2587 -2590
PubMed 12182866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 7.30 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86512 1 8.52
CHEMBL314849 1 8.46
CHEMBL327772 1 8.46
CHEMBL433418 1 8.30
CHEMBL315477 1 8.26
CHEMBL89248 1 8.05
CHEMBL87202 2 8.00
CHEMBL90164 1 7.96
CHEMBL89670 1 7.92
CHEMBL89239 1 7.80
CHEMBL86785 1 7.80
CHEMBL314891 1 7.72
CHEMBL85350 1 7.70
CHEMBL313197 1 7.62
CHEMBL89151 1 7.58
CHEMBL87304 1 7.55
CHEMBL84731 1 7.23
CHEMBL87901 1 7.22
CHEMBL86673 1 7.20
CHEMBL410057 1 7.14
CHEMBL314667 1 7.11
CHEMBL86743 1 7.04
CHEMBL86578 1 7.03
CHEMBL86602 1 7.00
CHEMBL87777 1 7.00
CHEMBL316372 1 6.98
CHEMBL313561 1 6.89
CHEMBL87954 1 6.87
CHEMBL313482 1 6.80
CHEMBL314981 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86512 IC50 = 3.0 nM 8.52
CHEMBL314849 IC50 = 3.5 nM 8.46
CHEMBL327772 IC50 = 3.5 nM 8.46
CHEMBL433418 IC50 = 5.0 nM 8.30
CHEMBL315477 IC50 = 5.5 nM 8.26
CHEMBL89248 IC50 = 9.0 nM 8.05
CHEMBL87202 IC50 = 10.0 nM 8.00
CHEMBL87202 IC50 = 10.0 nM 8.00
CHEMBL90164 IC50 = 11.0 nM 7.96
CHEMBL89670 IC50 = 12.0 nM 7.92
CHEMBL86785 IC50 = 16.0 nM 7.80
CHEMBL89239 IC50 = 16.0 nM 7.80
CHEMBL314891 IC50 = 19.0 nM 7.72
CHEMBL85350 IC50 = 20.0 nM 7.70
CHEMBL313197 IC50 = 24.0 nM 7.62
CHEMBL89151 IC50 = 26.0 nM 7.58
CHEMBL87304 IC50 = 28.0 nM 7.55
CHEMBL84731 IC50 = 59.0 nM 7.23
CHEMBL87901 IC50 = 60.0 nM 7.22
CHEMBL86673 IC50 = 63.0 nM 7.20
CHEMBL410057 IC50 = 73.0 nM 7.14
CHEMBL314667 IC50 = 77.0 nM 7.11
CHEMBL86743 IC50 = 91.0 nM 7.04
CHEMBL86578 IC50 = 93.0 nM 7.03
CHEMBL86602 IC50 = 100.0 nM 7.00
CHEMBL87777 IC50 = 100.0 nM 7.00
CHEMBL316372 IC50 = 105.0 nM 6.98
CHEMBL313561 IC50 = 130.0 nM 6.89
CHEMBL87954 IC50 = 135.0 nM 6.87
CHEMBL313482 IC50 = 160.0 nM 6.80
CHEMBL314981 IC50 = 315.0 nM 6.50
CHEMBL86982 IC50 = 551.0 nM 6.26
CHEMBL420599 IC50 = 1360.0 nM 5.87
CHEMBL327666 IC50 = 1500.0 nM 5.82
CHEMBL316209 IC50 = 1810.0 nM 5.74
CHEMBL85230 IC50 = 5420.0 nM 5.27
CHEMBL87925 IC50 > 10000.0 nM -
CHEMBL421163 IC50 > 10000.0 nM -
CHEMBL87106 IC50 > 10000.0 nM -
CHEMBL86598 IC50 > 10000.0 nM -
CHEMBL86501 IC50 > 10000.0 nM -
CHEMBL316185 IC50 > 10000.0 nM -
CHEMBL89381 IC50 > 10000.0 nM -