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Assay Detail

CHEMBL4729265

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

Binding
Inhibition of human PDE5A1 D563A mutant expressed in Escherichia coli BL21 incubated for 15 mins using [3H]-cGMP as substrate by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery of Evodiamine Derivatives as Highly Selective PDE5 Inhibitors Targeting a Unique Allosteric Pocket.
Zhang T,Lai Z,Yuan S,Huang YY,Dong G,Sheng C,Ke H,Luo HB
J Med Chem (2020) 63 : 9828 -9837
PubMed 32794708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.27 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL192 SILDENAFIL 4.0 1 8.92
CHEMBL4745832 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL192 SILDENAFIL IC50 = 1.2 nM 8.92
CHEMBL4745832 IC50 = 2482.0 nM 5.61