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Assay Detail

CHEMBL873456

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

Binding
inhibition of cAMP-specific phosphodiesterase 4 (PDE4) was determined in cytosol from human neutrophils
19
Total Activities
19
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

Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents.
Van der Mey M, Bommelé KM, Boss H, Hatzelmann A, Van Slingerland M, Sterk GJ, Timmerman H.
J Med Chem (2003) 46 : 2008 -2016
PubMed 12723963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.90 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL61699 1 8.70
CHEMBL304715 1 8.60
CHEMBL60026 1 8.40
CHEMBL62131 1 8.40
CHEMBL64824 1 8.40
CHEMBL64544 1 8.20
CHEMBL64052 1 8.20
CHEMBL294327 1 8.10
CHEMBL293589 1 8.10
CHEMBL59953 1 8.10
CHEMBL60839 1 7.90
CHEMBL61116 1 7.80
CHEMBL60999 1 7.80
CHEMBL61822 1 7.80
CHEMBL303550 1 7.70
CHEMBL59996 1 7.10
CHEMBL61667 1 7.00
CHEMBL511115 CILOMILAST 3.0 1 7.00
CHEMBL313842 ZARDAVERINE 2.0 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL61699 IC50 = 1.995 nM 8.70
CHEMBL304715 IC50 = 2.512 nM 8.60
CHEMBL60026 IC50 = 3.981 nM 8.40
CHEMBL62131 IC50 = 3.981 nM 8.40
CHEMBL64824 IC50 = 3.981 nM 8.40
CHEMBL64544 IC50 = 6.31 nM 8.20
CHEMBL64052 IC50 = 6.31 nM 8.20
CHEMBL294327 IC50 = 7.943 nM 8.10
CHEMBL293589 IC50 = 7.943 nM 8.10
CHEMBL59953 IC50 = 7.943 nM 8.10
CHEMBL60839 IC50 = 12.59 nM 7.90
CHEMBL61116 IC50 = 15.85 nM 7.80
CHEMBL60999 IC50 = 15.85 nM 7.80
CHEMBL61822 IC50 = 15.85 nM 7.80
CHEMBL303550 IC50 = 19.95 nM 7.70
CHEMBL59996 IC50 = 79.43 nM 7.10
CHEMBL61667 IC50 = 100.0 nM 7.00
CHEMBL511115 CILOMILAST IC50 = 100.0 nM 7.00
CHEMBL313842 ZARDAVERINE IC50 = 158.49 nM 6.80