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Assay Detail

CHEMBL5364539

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

Binding
Displacement of [3H]N-methylscopolamine chloride from human muscarinic M3 receptor incubated for 2 hrs by radioligand binding assay
21
Total Activities
15
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

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of M<sub>3</sub> Antagonist-PDE4 Inhibitor (MAPI) Dual Pharmacology Molecules for the Treatment of COPD.
Rizzi A, Amari G, Pivetti F, Delcanale M, Amadei F, Pappani A, Fornasari L, Villetti G, Marchini G, Pisano AR, Pitozzi V, Pittelli MG, Trevisani M, Salvadori M, Cenacchi V, Fioni A, Puccini P, Civelli M, Patacchini R, Baker-Glenn C, Van de Poël H, Blackaby W, Nash K, Armani E.
J Med Chem (2023) 66 : 11476 -11497
PubMed 37561958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 9.06 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5426968 1 10.20
CHEMBL5395712 2 9.80
CHEMBL5408238 2 9.70
CHEMBL5402697 1 9.60
CHEMBL5409010 1 9.60
CHEMBL5399363 2 9.60
CHEMBL5410533 2 9.50
CHEMBL5397387 1 9.20
CHEMBL5417689 1 9.20
CHEMBL5433640 1 9.00
CHEMBL5439180 1 8.60
CHEMBL5430170 2 8.50
CHEMBL5419862 1 8.50
CHEMBL5420551 1 7.60
CHEMBL5404020 2 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5426968 Ki = 0.0631 nM 10.20
CHEMBL5395712 Ki = 0.1585 nM 9.80
CHEMBL5395712 Ki = 0.1995 nM 9.70
CHEMBL5408238 Ki = 0.1995 nM 9.70
CHEMBL5399363 Ki = 0.2512 nM 9.60
CHEMBL5409010 Ki = 0.2512 nM 9.60
CHEMBL5402697 Ki = 0.2512 nM 9.60
CHEMBL5410533 Ki = 0.3162 nM 9.50
CHEMBL5399363 Ki = 0.3981 nM 9.40
CHEMBL5417689 Ki = 0.631 nM 9.20
CHEMBL5408238 Ki = 0.631 nM 9.20
CHEMBL5397387 Ki = 0.631 nM 9.20
CHEMBL5433640 Ki = 1.0 nM 9.00
CHEMBL5439180 Ki = 2.512 nM 8.60
CHEMBL5430170 Ki = 3.162 nM 8.50
CHEMBL5419862 Ki = 3.162 nM 8.50
CHEMBL5410533 Ki = 3.981 nM 8.40
CHEMBL5430170 Ki = 5.012 nM 8.30
CHEMBL5420551 Ki = 25.12 nM 7.60
CHEMBL5404020 Ki = 31.62 nM 7.50
CHEMBL5404020 Ki > 50.12 nM -