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Assay Detail

CHEMBL3285489

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

Binding
Inhibition of phosphodiesterase (peak-2) isolated from pig coronary artery assessed as inhibition of cAMP hydrolysis using 1 uM cAMP substrate in presence of 3% Me2SO
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Inhibition of separated forms of phosphodiesterases from pig coronary arteries by uracils and by 7-substituted derivatives of 1-methyl-3-isobutylxanthine.
Garst JE, Kramer GL, Wu YJ, Wells JN.
J Med Chem (1976) 19 : 499 -503
PubMed 177782 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 4.53 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3272808 1 5.17
CHEMBL275084 ISOBUTYLMETHYLXANTHINE 1 4.82
CHEMBL3272818 1 4.70
CHEMBL3272811 1 4.55
CHEMBL3272817 1 4.37
CHEMBL3272816 1 4.32
CHEMBL24444 1 4.19
CHEMBL3272815 1 4.12
CHEMBL25096 1 -
CHEMBL3272809 1 -
CHEMBL3272810 1 -
CHEMBL26606 1 -
CHEMBL3272812 1 -
CHEMBL3272813 1 -
CHEMBL3272814 1 -
CHEMBL3272819 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3272808 IC50 = 6800.0 nM 5.17
CHEMBL275084 ISOBUTYLMETHYLXANTHINE IC50 = 15000.0 nM 4.82
CHEMBL3272818 IC50 = 20000.0 nM 4.70
CHEMBL3272811 IC50 = 28000.0 nM 4.55
CHEMBL3272817 IC50 = 43000.0 nM 4.37
CHEMBL3272816 IC50 = 48000.0 nM 4.32
CHEMBL24444 IC50 = 65000.0 nM 4.19
CHEMBL3272815 IC50 = 75000.0 nM 4.12
CHEMBL25096 IC50 = 126000.0 nM -
CHEMBL3272809 IC50 > 100000.0 nM -
CHEMBL3272810 IC50 > 100000.0 nM -
CHEMBL26606 IC50 = 108000.0 nM -
CHEMBL3272812 IC50 > 100000.0 nM -
CHEMBL3272813 IC50 > 100000.0 nM -
CHEMBL3272814 IC50 = 142000.0 nM -
CHEMBL3272819 IC50 > 300000.0 nM -