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Assay Detail

CHEMBL3607150

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

Binding
Inhibition of PDE4A (unknown origin)
2
Total Activities
2
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 4A (CHEMBL254)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Optimization of 4-(8-(3-Fluorophenyl)-1,7-naphthyridin-6-yl)transcyclohexanecarboxylic Acid, an Improved PDE4 Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease (COPD).
Press NJ, Taylor RJ, Fullerton JD, Tranter P, McCarthy C, Keller TH, Arnold N, Beer D, Brown L, Cheung R, Christie J, Denholm A, Haberthuer S, Hatto JD, Keenan M, Mercer MK, Oakman H, Sahri H, Tuffnell AR, Tweed M, Trifilieff A.
J Med Chem (2015) 58 : 6747 -6752
PubMed 26288344 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.57 6.91

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2172374 1 6.91
CHEMBL77826 1 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2172374 IC50 = 123.0 nM 6.91
CHEMBL77826 IC50 = 602.0 nM 6.22