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Assay Detail

CHEMBL5034535

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

Binding
Inhibition of human recombinant PDE4B2 assessed as reduction in cAMP level incubated for 2 hrs by LANCE Ultra cAMP TR-FRET assay
34
Total Activities
23
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 4B (CHEMBL275)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of M<sub>3</sub> Antagonist-PDE4 Inhibitor Dual Pharmacology Molecules for the Treatment of Chronic Obstructive Pulmonary Disease.
Armani E, Rizzi A, Capaldi C, De Fanti R, Delcanale M, Villetti G, Marchini G, Pisano AR, Pitozzi V, Pittelli MG, Trevisani M, Salvadori M, Cenacchi V, Puccini P, Amadei F, Pappani A, Civelli M, Patacchini R, Baker-Glenn CAG, Van de Poël H, Blackaby WP, Nash K, Amari G.
J Med Chem (2021) 64 : 9100 -9119
PubMed 34142835 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 8.84 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5077250 1 9.50
CHEMBL5086393 2 9.30
CHEMBL5091461 1 9.30
CHEMBL5081816 2 9.20
CHEMBL5076535 2 9.20
CHEMBL5085166 1 9.20
CHEMBL5086272 1 9.20
CHEMBL5076637 2 9.20
CHEMBL5086769 1 9.10
CHEMBL5076886 2 9.00
CHEMBL5084383 1 9.00
CHEMBL5070876 1 9.00
CHEMBL5076445 2 8.90
CHEMBL5074599 2 8.80
CHEMBL5074216 2 8.80
CHEMBL5078006 2 8.80
CHEMBL5077424 2 8.70
CHEMBL5077161 1 8.70
CHEMBL5075132 1 8.60
CHEMBL5076558 2 8.40
CHEMBL5088742 1 8.20
CHEMBL5076266 1 8.10
CHEMBL5076680 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5077250 IC50 = 0.3162 nM 9.50
CHEMBL5086393 IC50 = 0.5012 nM 9.30
CHEMBL5091461 IC50 = 0.5012 nM 9.30
CHEMBL5081816 IC50 = 0.631 nM 9.20
CHEMBL5076637 IC50 = 0.631 nM 9.20
CHEMBL5076637 IC50 = 0.631 nM 9.20
CHEMBL5086272 IC50 = 0.631 nM 9.20
CHEMBL5085166 IC50 = 0.631 nM 9.20
CHEMBL5076535 IC50 = 0.631 nM 9.20
CHEMBL5086769 IC50 = 0.7943 nM 9.10
CHEMBL5081816 IC50 = 0.7943 nM 9.10
CHEMBL5084383 IC50 = 1.0 nM 9.00
CHEMBL5070876 IC50 = 1.0 nM 9.00
CHEMBL5076535 IC50 = 1.0 nM 9.00
CHEMBL5086393 IC50 = 1.0 nM 9.00
CHEMBL5076886 IC50 = 1.0 nM 9.00
CHEMBL5076886 IC50 = 1.0 nM 9.00
CHEMBL5076445 IC50 = 1.259 nM 8.90
CHEMBL5074599 IC50 = 1.585 nM 8.80
CHEMBL5074599 IC50 = 1.585 nM 8.80
CHEMBL5074216 IC50 = 1.585 nM 8.80
CHEMBL5078006 IC50 = 1.585 nM 8.80
CHEMBL5077424 IC50 = 1.995 nM 8.70
CHEMBL5078006 IC50 = 1.995 nM 8.70
CHEMBL5077161 IC50 = 1.995 nM 8.70
CHEMBL5075132 IC50 = 2.512 nM 8.60
CHEMBL5076445 IC50 = 2.512 nM 8.60
CHEMBL5077424 IC50 = 3.162 nM 8.50
CHEMBL5074216 IC50 = 3.162 nM 8.50
CHEMBL5076558 IC50 = 3.981 nM 8.40
CHEMBL5088742 IC50 = 6.31 nM 8.20
CHEMBL5076558 IC50 = 7.943 nM 8.10
CHEMBL5076266 IC50 = 7.943 nM 8.10
CHEMBL5076680 IC50 = 10.0 nM 8.00