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Assay Detail

CHEMBL5034533

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

Binding
Antagonist activity at muscarinic M3 receptor in guinea pig trachea assessed as inhibition of carbachol-induced contraction
28
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Trachea
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 28 8.40 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5088742 1 9.20
CHEMBL5091461 1 9.10
CHEMBL5076558 3 9.10
CHEMBL5074599 2 9.00
CHEMBL5086769 1 9.00
CHEMBL5076266 1 9.00
CHEMBL5077250 1 8.80
CHEMBL5085166 1 8.70
CHEMBL5077161 1 8.70
CHEMBL5076637 2 8.60
CHEMBL5075132 1 8.60
CHEMBL5086272 1 8.40
CHEMBL5070876 1 8.40
CHEMBL5084829 1 8.30
CHEMBL5094110 1 8.20
CHEMBL5090179 1 8.20
CHEMBL5090464 1 8.20
CHEMBL5084383 1 8.10
CHEMBL5087564 1 7.70
CHEMBL5086895 1 7.60
CHEMBL5085717 1 7.50
CHEMBL5081214 1 7.30
CHEMBL5080391 1 6.50
CHEMBL5078680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5088742 IC50 = 0.631 nM 9.20
CHEMBL5076558 IC50 = 0.7943 nM 9.10
CHEMBL5091461 IC50 = 0.7943 nM 9.10
CHEMBL5074599 IC50 = 1.0 nM 9.00
CHEMBL5076558 IC50 = 1.0 nM 9.00
CHEMBL5086769 IC50 = 1.0 nM 9.00
CHEMBL5076266 IC50 = 1.0 nM 9.00
CHEMBL5074599 IC50 = 1.259 nM 8.90
CHEMBL5077250 IC50 = 1.585 nM 8.80
CHEMBL5077161 IC50 = 1.995 nM 8.70
CHEMBL5085166 IC50 = 1.995 nM 8.70
CHEMBL5076637 IC50 = 2.512 nM 8.60
CHEMBL5075132 IC50 = 2.512 nM 8.60
CHEMBL5076637 IC50 = 3.162 nM 8.50
CHEMBL5086272 IC50 = 3.981 nM 8.40
CHEMBL5070876 IC50 = 3.981 nM 8.40
CHEMBL5084829 IC50 = 5.012 nM 8.30
CHEMBL5076558 IC50 = 6.31 nM 8.20
CHEMBL5090179 IC50 = 6.31 nM 8.20
CHEMBL5090464 IC50 = 6.31 nM 8.20
CHEMBL5094110 IC50 = 6.31 nM 8.20
CHEMBL5084383 IC50 = 7.943 nM 8.10
CHEMBL5087564 IC50 = 19.95 nM 7.70
CHEMBL5086895 IC50 = 25.12 nM 7.60
CHEMBL5085717 IC50 = 31.62 nM 7.50
CHEMBL5081214 IC50 = 50.12 nM 7.30
CHEMBL5080391 IC50 = 316.23 nM 6.50
CHEMBL5078680 IC50 > 1000.0 nM -