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Assay Detail

CHEMBL855486

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

Binding
Inhibition of human recombinant PDE4B
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

3',5'-cyclic-AMP phosphodiesterase 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Duplantier AJ, Bachert EL, Cheng JB, Cohan VL, Jenkinson TH, Kraus KG, McKechney MW, Pillar JD, Watson JW.
J Med Chem (2007) 50 : 344 -349
PubMed 17228876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 8.52
CHEMBL218103 1 8.10
CHEMBL217899 TOFIMILAST 2.0 1 7.89
CHEMBL218653 1 7.70
CHEMBL511115 CILOMILAST 3.0 1 7.08
CHEMBL218990 1 6.68
CHEMBL430893 (-)-ROLIPRAM 1 6.64
CHEMBL218793 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 3.0 nM 8.52
CHEMBL218103 IC50 = 8.0 nM 8.10
CHEMBL217899 TOFIMILAST IC50 = 13.0 nM 7.89
CHEMBL218653 IC50 = 20.0 nM 7.70
CHEMBL511115 CILOMILAST IC50 = 84.0 nM 7.08
CHEMBL218990 IC50 = 210.0 nM 6.68
CHEMBL430893 (-)-ROLIPRAM IC50 = 231.0 nM 6.64
CHEMBL218793 IC50 = 430.0 nM 6.37