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Assay Detail

CHEMBL5264797

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

Binding
Inhibition of human N-terminal His-GST-tagged recombinant PDE3A (669-end residues) using fluorescent labelled cAMP as substrate
7
Total Activities
7
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-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing.
Lewis TA, de Waal L, Wu X, Youngsaye W, Wengner A, Kopitz C, Lange M, Gradl S, Ellermann M, Lienau P, Schreiber SL, Greulich H, Meyerson M.
ACS Med Chem Lett (2019) 10 : 1537 -1542
PubMed 31749907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 7.43 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5283715 1 8.10
CHEMBL5286823 1 8.10
CHEMBL5280568 1 8.00
CHEMBL340785 1 7.62
CHEMBL1495092 1 7.60
CHEMBL5267447 1 6.92
CHEMBL5275420 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5283715 IC50 = 8.0 nM 8.10
CHEMBL5286823 IC50 = 8.0 nM 8.10
CHEMBL5280568 IC50 = 10.0 nM 8.00
CHEMBL340785 IC50 = 24.0 nM 7.62
CHEMBL1495092 IC50 = 25.0 nM 7.60
CHEMBL5267447 IC50 = 120.0 nM 6.92
CHEMBL5275420 IC50 = 2000.0 nM 5.70