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Assay Detail

CHEMBL962323

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

Binding
Inhibition of human corpus cavernosum PDE5 by scintillation proximity assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.
Bunnage ME, Mathias JP, Wood A, Miller D, Street SD.
Bioorg Med Chem Lett (2008) 18 : 6033 -6036
PubMed 18951784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.07 9.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL444157 1 9.21
CHEMBL514435 1 9.05
CHEMBL1928257 1 8.96
CHEMBL209157 1 8.89
CHEMBL455187 1 8.52
CHEMBL192 SILDENAFIL 4.0 1 8.46
CHEMBL460293 1 8.38
CHEMBL460294 1 8.25
CHEMBL455452 1 8.11
CHEMBL455412 1 7.11
CHEMBL459047 1 7.10
CHEMBL455413 1 7.00
CHEMBL445457 1 7.00
CHEMBL514433 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL444157 IC50 = 0.62 nM 9.21
CHEMBL514435 IC50 = 0.89 nM 9.05
CHEMBL1928257 IC50 = 1.1 nM 8.96
CHEMBL209157 IC50 = 1.3 nM 8.89
CHEMBL455187 IC50 = 3.0 nM 8.52
CHEMBL192 SILDENAFIL IC50 = 3.5 nM 8.46
CHEMBL460293 IC50 = 4.2 nM 8.38
CHEMBL460294 IC50 = 5.6 nM 8.25
CHEMBL455452 IC50 = 7.7 nM 8.11
CHEMBL455412 IC50 = 77.0 nM 7.11
CHEMBL459047 IC50 = 80.0 nM 7.10
CHEMBL455413 IC50 = 100.0 nM 7.00
CHEMBL445457 IC50 = 100.0 nM 7.00
CHEMBL514433 IC50 = 100.0 nM 7.00