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Assay Detail

CHEMBL3375590

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

Binding
Inhibition of human recombinant PDE4D after 1 hr by SPA in presence of radioactively labeled cAMP
22
Total Activities
22
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

3',5'-cyclic-AMP phosphodiesterase 4D (CHEMBL288)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and early clinical development of 2-{6-[2-(3,5-dichloro-4-pyridyl)acetyl]-2,3-dimethoxyphenoxy}-N-propylacetamide (LEO 29102), a soft-drug inhibitor of phosphodiesterase 4 for topical treatment of atopic dermatitis.
Felding J, Sørensen MD, Poulsen TD, Larsen J, Andersson C, Refer P, Engell K, Ladefoged LG, Thormann T, Vinggaard AM, Hegardt P, Søhoel A, Nielsen SF.
J Med Chem (2014) 57 : 5893 -5903
PubMed 24984230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.45 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3315084 1 9.00
CHEMBL3315083 1 8.52
CHEMBL3315089 1 8.30
CHEMBL3315088 1 8.30
CHEMBL3315079 1 8.10
CHEMBL3315080 1 7.96
CHEMBL3315072 1 7.89
CHEMBL3315087 1 7.89
CHEMBL3315077 1 7.82
CHEMBL3315081 1 7.77
CHEMBL3315086 1 7.77
CHEMBL48017 1 7.77
CHEMBL3315090 1 7.70
CHEMBL3315078 1 7.35
CHEMBL3315085 1 7.21
CHEMBL3315076 1 7.20
CHEMBL3313943 1 7.09
CHEMBL3315073 1 6.96
CHEMBL3315074 1 6.67
CHEMBL3315075 1 5.70
CHEMBL3315082 1 5.42
CHEMBL3315071 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3315084 IC50 = 1.0 nM 9.00
CHEMBL3315083 IC50 = 3.0 nM 8.52
CHEMBL3315089 IC50 = 5.0 nM 8.30
CHEMBL3315088 IC50 = 5.0 nM 8.30
CHEMBL3315079 IC50 = 8.0 nM 8.10
CHEMBL3315080 IC50 = 11.0 nM 7.96
CHEMBL3315072 IC50 = 13.0 nM 7.89
CHEMBL3315087 IC50 = 13.0 nM 7.89
CHEMBL3315077 IC50 = 15.0 nM 7.82
CHEMBL3315081 IC50 = 17.0 nM 7.77
CHEMBL3315086 IC50 = 17.0 nM 7.77
CHEMBL48017 IC50 = 17.0 nM 7.77
CHEMBL3315090 IC50 = 20.0 nM 7.70
CHEMBL3315078 IC50 = 45.0 nM 7.35
CHEMBL3315085 IC50 = 61.0 nM 7.21
CHEMBL3315076 IC50 = 63.0 nM 7.20
CHEMBL3313943 IC50 = 81.0 nM 7.09
CHEMBL3315073 IC50 = 110.0 nM 6.96
CHEMBL3315074 IC50 = 212.0 nM 6.67
CHEMBL3315075 IC50 = 2010.0 nM 5.70
CHEMBL3315082 IC50 = 3760.0 nM 5.42
CHEMBL3315071 IC50 = 3790.0 nM 5.42