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Assay Detail

CHEMBL2433339

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Binding
Inhibition of human PDE3
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.
Cui JJ, Shen H, Tran-Dubé M, Nambu M, McTigue M, Grodsky N, Ryan K, Yamazaki S, Aguirre S, Parker M, Li Q, Zou H, Christensen J.
J Med Chem (2013) 56 : 6651 -6665
PubMed 23944843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.33 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2431819 1 6.77
CHEMBL2001019 PF-04217903 1.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2431819 IC50 = 170.0 nM 6.77
CHEMBL2001019 PF-04217903 IC50 = 1300.0 nM 5.89