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Assay Detail

CHEMBL2024713

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

Binding
Inhibition of bovine PDE5 after 24 hrs by time-resolved fluorescence resonance energy transfer assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL3478)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Drug-to-genome-to-drug, step 2: reversing selectivity in a series of antiplasmodial compounds.
Beghyn TB, Charton J, Leroux F, Henninot A, Reboule I, Cos P, Maes L, Deprez B.
J Med Chem (2012) 55 : 1274 -1286
PubMed 22204607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2022215 1 9.00
CHEMBL2022213 1 9.00
CHEMBL2022212 1 8.70
CHEMBL2022214 1 8.52
CHEMBL779 TADALAFIL 4.0 1 8.30
CHEMBL32255 1 8.30
CHEMBL2022209 1 8.15
CHEMBL2022219 1 7.55
CHEMBL2022222 1 7.25
CHEMBL284745 1 5.28
CHEMBL2024109 1 5.25
CHEMBL2024110 1 -
CHEMBL2024108 1 -
CHEMBL2024107 1 -
CHEMBL2022223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2022215 IC50 = 1.0 nM 9.00
CHEMBL2022213 IC50 = 1.0 nM 9.00
CHEMBL2022212 IC50 = 2.0 nM 8.70
CHEMBL2022214 IC50 = 3.0 nM 8.52
CHEMBL779 TADALAFIL IC50 = 5.0 nM 8.30
CHEMBL32255 IC50 = 5.0 nM 8.30
CHEMBL2022209 IC50 = 7.0 nM 8.15
CHEMBL2022219 IC50 = 28.0 nM 7.55
CHEMBL2022222 IC50 = 56.0 nM 7.25
CHEMBL284745 IC50 = 5200.0 nM 5.28
CHEMBL2024109 IC50 = 5600.0 nM 5.25
CHEMBL2024110 IC50 > 10000.0 nM -
CHEMBL2024108 IC50 > 10000.0 nM -
CHEMBL2024107 IC50 > 10000.0 nM -
CHEMBL2022223 IC50 > 1000.0 nM -