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Assay Detail

CHEMBL3607152

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Binding
Inhibition of human PDE4D
11
Total Activities
11
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 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 11 7.78 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77826 1 8.82
CHEMBL3605513 1 8.52
CHEMBL3605510 1 8.10
CHEMBL3605511 1 7.89
CHEMBL2172370 1 7.72
CHEMBL3605512 1 7.66
CHEMBL3605509 1 7.52
CHEMBL2172374 1 7.50
CHEMBL2172375 1 7.39
CHEMBL2172368 1 7.29
CHEMBL2172372 1 7.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77826 IC50 = 1.5 nM 8.82
CHEMBL3605513 IC50 = 3.0 nM 8.52
CHEMBL3605510 IC50 = 8.0 nM 8.10
CHEMBL3605511 IC50 = 13.0 nM 7.89
CHEMBL2172370 IC50 = 19.0 nM 7.72
CHEMBL3605512 IC50 = 22.0 nM 7.66
CHEMBL3605509 IC50 = 30.0 nM 7.52
CHEMBL2172374 IC50 = 32.0 nM 7.50
CHEMBL2172375 IC50 = 41.0 nM 7.39
CHEMBL2172368 IC50 = 51.0 nM 7.29
CHEMBL2172372 IC50 = 64.0 nM 7.19