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Assay Detail

CHEMBL4817487

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

Binding
Displacement of [3H]-N-methylscopolamine from human muscarinic M3 receptor
14
Total Activities
14
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

Discovery of a novel class of inhaled dual pharmacology muscarinic antagonist and β<sub>2</sub> agonist (MABA) for the treatment of chronic obstructive pulmonary disease (COPD).
Rancati F, Linney ID, Rizzi A, Delcanale M, Knight CK, Schmidt W, Pastore F, Riccardi B, Mileo V, Carnini C, Cesari N, Blackaby WP, Patacchini R, Carzaniga L.
Bioorg Med Chem Lett (2021) 41 : 127975 -127975
PubMed 33753262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 9.34 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4871517 1 10.00
CHEMBL4847910 1 9.90
CHEMBL4871702 1 9.90
CHEMBL4854091 1 9.90
CHEMBL4852629 1 9.80
CHEMBL4846536 1 9.60
CHEMBL4866806 1 9.60
CHEMBL4863525 1 9.50
CHEMBL4874819 1 9.40
CHEMBL4854418 1 9.40
CHEMBL4869096 1 8.90
CHEMBL4857743 1 8.40
CHEMBL4878138 1 8.40
CHEMBL4878395 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4871517 Ki = 0.1 nM 10.00
CHEMBL4847910 Ki = 0.1259 nM 9.90
CHEMBL4871702 Ki = 0.1259 nM 9.90
CHEMBL4854091 Ki = 0.1259 nM 9.90
CHEMBL4852629 Ki = 0.1585 nM 9.80
CHEMBL4846536 Ki = 0.2512 nM 9.60
CHEMBL4866806 Ki = 0.2512 nM 9.60
CHEMBL4863525 Ki = 0.3162 nM 9.50
CHEMBL4874819 Ki = 0.3981 nM 9.40
CHEMBL4854418 Ki = 0.3981 nM 9.40
CHEMBL4869096 Ki = 1.259 nM 8.90
CHEMBL4857743 Ki = 3.981 nM 8.40
CHEMBL4878138 Ki = 3.981 nM 8.40
CHEMBL4878395 Ki = 10.0 nM 8.00