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Assay Detail

CHEMBL5034532

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

Binding
Displacement of [3H]-N-methyl Scopolamine Chloride from human M3 receptor membranes incubated for 2 hrs by scintillation counting analysis
ChEMBL ↗
48
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245) ↗
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
Ki 48 9.27 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5074599 — — 2 10.20
CHEMBL5076637 — — 2 10.00
CHEMBL5070876 — — 1 10.00
CHEMBL5091461 — — 1 9.90
CHEMBL4650755 — — 1 9.90
CHEMBL5074216 — — 2 9.90
CHEMBL5076558 — — 3 9.80
CHEMBL5077161 — — 1 9.80
CHEMBL5075132 — — 1 9.80
CHEMBL5076445 — — 2 9.70
CHEMBL5076266 — — 1 9.70
CHEMBL5084383 — — 1 9.70
CHEMBL5090464 — — 1 9.70
CHEMBL5086393 — — 2 9.60
CHEMBL5090179 — — 1 9.60
CHEMBL5086769 — — 1 9.50
CHEMBL5088742 — — 1 9.50
CHEMBL5081816 — — 2 9.50
CHEMBL5076680 — — 1 9.50
CHEMBL5085717 — — 1 9.50
CHEMBL5084829 — — 1 9.50
CHEMBL5087564 — — 1 9.40
CHEMBL5076535 — — 2 9.40
CHEMBL5085166 — — 1 9.30
CHEMBL5078006 — — 2 9.30
CHEMBL5076886 — — 2 9.30
CHEMBL5077424 — — 2 9.20
CHEMBL5094110 — — 1 9.20
CHEMBL5086895 — — 1 9.20
CHEMBL5086272 — — 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5074599 — Ki = 0.0631 nM 10.20
CHEMBL5076637 — Ki = 0.1 nM 10.00
CHEMBL5070876 — Ki = 0.1 nM 10.00
CHEMBL5074216 — Ki = 0.1259 nM 9.90
CHEMBL4650755 — Ki = 0.1259 nM 9.90
CHEMBL5074599 — Ki = 0.1259 nM 9.90
CHEMBL5091461 — Ki = 0.1259 nM 9.90
CHEMBL5076558 — Ki = 0.1585 nM 9.80
CHEMBL5076637 — Ki = 0.1585 nM 9.80
CHEMBL5077161 — Ki = 0.1585 nM 9.80
CHEMBL5075132 — Ki = 0.1585 nM 9.80
CHEMBL5076266 — Ki = 0.1995 nM 9.70
CHEMBL5076445 — Ki = 0.1995 nM 9.70
CHEMBL5076558 — Ki = 0.1995 nM 9.70
CHEMBL5084383 — Ki = 0.1995 nM 9.70
CHEMBL5090464 — Ki = 0.1995 nM 9.70
CHEMBL5090179 — Ki = 0.2512 nM 9.60
CHEMBL5086393 — Ki = 0.2512 nM 9.60
CHEMBL5085717 — Ki = 0.3162 nM 9.50
CHEMBL5084829 — Ki = 0.3162 nM 9.50
CHEMBL5081816 — Ki = 0.3162 nM 9.50
CHEMBL5086769 — Ki = 0.3162 nM 9.50
CHEMBL5076680 — Ki = 0.3162 nM 9.50
CHEMBL5088742 — Ki = 0.3162 nM 9.50
CHEMBL5076535 — Ki = 0.3981 nM 9.40
CHEMBL5087564 — Ki = 0.3981 nM 9.40
CHEMBL5076558 — Ki = 0.3981 nM 9.40
CHEMBL5085166 — Ki = 0.5012 nM 9.30
CHEMBL5076886 — Ki = 0.5012 nM 9.30
CHEMBL5078006 — Ki = 0.5012 nM 9.30
CHEMBL5094110 — Ki = 0.631 nM 9.20
CHEMBL5077424 — Ki = 0.631 nM 9.20
CHEMBL5077424 — Ki = 0.631 nM 9.20
CHEMBL5086895 — Ki = 0.631 nM 9.20
CHEMBL1621597 IPRATROPIUM Ki = 0.7943 nM 9.10
CHEMBL5078680 — Ki = 0.7943 nM 9.10
CHEMBL5086272 — Ki = 0.7943 nM 9.10
CHEMBL5080391 — Ki = 1.259 nM 8.90
CHEMBL5081214 — Ki = 1.259 nM 8.90
CHEMBL5076445 — Ki = 2.512 nM 8.60
CHEMBL5077250 — Ki = 3.162 nM 8.50
CHEMBL5078006 — Ki = 6.31 nM 8.20
CHEMBL5074216 — Ki = 7.943 nM 8.10
CHEMBL5069430 — Ki = 7.943 nM 8.10
CHEMBL5086393 — Ki = 10.0 nM 8.00
CHEMBL5076886 — Ki = 10.0 nM 8.00
CHEMBL5081816 — Ki = 10.0 nM 8.00
CHEMBL5076535 — Ki = 12.59 nM 7.90