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Assay Detail

CHEMBL769678

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

Binding
Inhibitory activity on human eosinophil phosphodiesterase 4.
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Phosphodiesterase 4 (CHEMBL2093863)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

7-Oxo-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridines as novel inhibitors of human eosinophil phosphodiesterase.
Duplantier AJ, Andresen CJ, Cheng JB, Cohan VL, Decker C, DiCapua FM, Kraus KG, Johnson KL, Turner CR, UmLand JP, Watson JW, Wester RT, Williams AS, Williams JA.
J Med Chem (1998) 41 : 2268 -2277
PubMed 9632360 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.22 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42126 PICLAMILAST 2.0 1 8.05
CHEMBL307678 1 7.47
CHEMBL309803 1 7.41
CHEMBL76066 1 7.32
CHEMBL74597 1 7.20
CHEMBL75247 1 6.82
CHEMBL307286 1 6.80
CHEMBL308784 1 6.80
CHEMBL511115 CILOMILAST 3.0 1 6.77
CHEMBL75722 1 6.57
CHEMBL305806 1 6.38
CHEMBL75819 1 6.36
CHEMBL76065 1 6.34
CHEMBL406941 1 6.31
CHEMBL310509 1 6.18
CHEMBL32442 CDP840 1 6.17
CHEMBL74251 1 6.05
CHEMBL72688 1 5.97
CHEMBL307144 1 5.79
CHEMBL73894 1 5.79
CHEMBL308180 1 5.65
CHEMBL63 ROLIPRAM 2.0 1 5.48
CHEMBL74774 1 5.22
CHEMBL74361 1 4.80
CHEMBL307511 1 4.07
CHEMBL306335 1 4.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42126 PICLAMILAST IC50 = 9.0 nM 8.05
CHEMBL307678 IC50 = 34.0 nM 7.47
CHEMBL309803 IC50 = 39.0 nM 7.41
CHEMBL76066 IC50 = 48.0 nM 7.32
CHEMBL74597 IC50 = 63.0 nM 7.20
CHEMBL75247 IC50 = 150.0 nM 6.82
CHEMBL307286 IC50 = 160.0 nM 6.80
CHEMBL308784 IC50 = 160.0 nM 6.80
CHEMBL511115 CILOMILAST IC50 = 170.0 nM 6.77
CHEMBL75722 IC50 = 270.0 nM 6.57
CHEMBL305806 IC50 = 420.0 nM 6.38
CHEMBL75819 IC50 = 440.0 nM 6.36
CHEMBL76065 IC50 = 460.0 nM 6.34
CHEMBL406941 IC50 = 490.0 nM 6.31
CHEMBL310509 IC50 = 660.0 nM 6.18
CHEMBL32442 CDP840 IC50 = 670.0 nM 6.17
CHEMBL74251 IC50 = 890.0 nM 6.05
CHEMBL72688 IC50 = 1080.0 nM 5.97
CHEMBL307144 IC50 = 1640.0 nM 5.79
CHEMBL73894 IC50 = 1640.0 nM 5.79
CHEMBL308180 IC50 = 2240.0 nM 5.65
CHEMBL63 ROLIPRAM IC50 = 3340.0 nM 5.48
CHEMBL74774 IC50 = 6040.0 nM 5.22
CHEMBL74361 IC50 = 15700.0 nM 4.80
CHEMBL307511 IC50 = 84700.0 nM 4.07
CHEMBL306335 IC50 = 84900.0 nM 4.07