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Assay Detail

CHEMBL757892

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

Binding
Inhibition of PDE4 in the cytosol of human neutrophils
27
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

Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
Van der Mey M, Hatzelmann A, Van der Laan IJ, Sterk GJ, Thibaut U, Timmerman H.
J Med Chem (2001) 44 : 2511 -2522
PubMed 11472205 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.60 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL421528 1 8.40
CHEMBL315815 PYRIDOPYRIDAZINONE 1 8.30
CHEMBL313170 1 8.10
CHEMBL314722 1 7.90
CHEMBL85278 1 7.60
CHEMBL315981 1 7.30
CHEMBL313111 1 7.10
CHEMBL440878 1 7.00
CHEMBL511115 CILOMILAST 3.0 1 7.00
CHEMBL83484 1 6.90
CHEMBL313842 ZARDAVERINE 2.0 1 6.80
CHEMBL84702 1 6.80
CHEMBL316413 2 6.70
CHEMBL84861 1 6.50
CHEMBL85617 1 6.50
CHEMBL85424 1 6.40
CHEMBL85556 1 6.40
CHEMBL2367714 1 6.10
CHEMBL84874 1 5.90
CHEMBL275448 1 5.80
CHEMBL84860 1 5.80
CHEMBL314167 1 5.80
CHEMBL316442 1 5.30
CHEMBL314183 1 5.30
CHEMBL81921 1 5.20
CHEMBL2367717 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL421528 IC50 = 3.981 nM 8.40
CHEMBL315815 PYRIDOPYRIDAZINONE IC50 = 5.012 nM 8.30
CHEMBL313170 IC50 = 7.943 nM 8.10
CHEMBL314722 IC50 = 12.59 nM 7.90
CHEMBL85278 IC50 = 25.12 nM 7.60
CHEMBL315981 IC50 = 50.12 nM 7.30
CHEMBL313111 IC50 = 79.43 nM 7.10
CHEMBL440878 IC50 = 100.0 nM 7.00
CHEMBL511115 CILOMILAST IC50 = 100.0 nM 7.00
CHEMBL83484 IC50 = 125.89 nM 6.90
CHEMBL313842 ZARDAVERINE IC50 = 158.49 nM 6.80
CHEMBL84702 IC50 = 158.49 nM 6.80
CHEMBL316413 IC50 = 199.53 nM 6.70
CHEMBL84861 IC50 = 316.23 nM 6.50
CHEMBL85617 IC50 = 316.23 nM 6.50
CHEMBL85424 IC50 = 398.11 nM 6.40
CHEMBL85556 IC50 = 398.11 nM 6.40
CHEMBL316413 IC50 = 630.96 nM 6.20
CHEMBL2367714 IC50 = 794.33 nM 6.10
CHEMBL84874 IC50 = 1258.93 nM 5.90
CHEMBL275448 IC50 = 1584.89 nM 5.80
CHEMBL84860 IC50 = 1584.89 nM 5.80
CHEMBL314167 IC50 = 1584.89 nM 5.80
CHEMBL316442 IC50 = 5011.87 nM 5.30
CHEMBL314183 IC50 = 5011.87 nM 5.30
CHEMBL81921 IC50 = 6309.57 nM 5.20
CHEMBL2367717 IC50 = 7943.28 nM 5.10