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Assay Detail

CHEMBL5129799

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

Binding
Displacement of [3H]-methylscopolamine from human muscarinic M3 receptor expressed in CHO-K1 cell membrane measured after 2 hr by Cheng-prusoff equation analysis
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Subcellular 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 Clinical Candidate CHF-6366: A Novel Super-soft Dual Pharmacology Muscarinic Antagonist and β<sub>2</sub> Agonist (MABA) for the Inhaled Treatment of Respiratory Diseases.
Carzaniga L, Linney ID, Rizzi A, Delcanale M, Schmidt W, Knight CK, Pastore F, Miglietta D, Carnini C, Cesari N, Riccardi B, Mileo V, Venturi L, Moretti E, Blackaby WP, Patacchini R, Accetta A, Biagetti M, Bassani F, Tondelli M, Murgo A, Battipaglia L, Villetti G, Puccini P, Catinella S, Civelli M, Rancati F.
J Med Chem (2022) 65 : 10233 -10250
PubMed 35901125 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.71 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5172865 1 10.20
CHEMBL5190387 1 10.20
CHEMBL5193853 1 10.10
CHEMBL4854091 1 9.90
CHEMBL5184455 1 9.90
CHEMBL5208957 1 9.80
CHEMBL5200887 1 9.70
CHEMBL5208201 1 9.50
CHEMBL5200448 1 9.10
CHEMBL5184598 1 9.10
CHEMBL5177499 1 9.00
CHEMBL5195203 1 8.80
CHEMBL5179380 1 8.50
CHEMBL5178217 1 8.50
CHEMBL5187593 1 8.40
CHEMBL5194569 1 8.40
CHEMBL5193776 1 8.30
CHEMBL5202045 1 8.20
CHEMBL5195224 1 8.10
CHEMBL5181855 1 8.10
CHEMBL5202787 1 8.10
CHEMBL5202567 1 8.10
CHEMBL5207792 1 8.00
CHEMBL5170720 1 7.60
CHEMBL5193865 1 7.60
CHEMBL5203937 1 7.40
CHEMBL5180420 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5172865 Ki = 0.0631 nM 10.20
CHEMBL5190387 Ki = 0.0631 nM 10.20
CHEMBL5193853 Ki = 0.07943 nM 10.10
CHEMBL4854091 Ki = 0.1259 nM 9.90
CHEMBL5184455 Ki = 0.1259 nM 9.90
CHEMBL5208957 Ki = 0.1585 nM 9.80
CHEMBL5200887 Ki = 0.1995 nM 9.70
CHEMBL5208201 Ki = 0.3162 nM 9.50
CHEMBL5200448 Ki = 0.7943 nM 9.10
CHEMBL5184598 Ki = 0.7943 nM 9.10
CHEMBL5177499 Ki = 1.0 nM 9.00
CHEMBL5195203 Ki = 1.585 nM 8.80
CHEMBL5179380 Ki = 3.162 nM 8.50
CHEMBL5178217 Ki = 3.162 nM 8.50
CHEMBL5187593 Ki = 3.981 nM 8.40
CHEMBL5194569 Ki = 3.981 nM 8.40
CHEMBL5193776 Ki = 5.012 nM 8.30
CHEMBL5202045 Ki = 6.31 nM 8.20
CHEMBL5195224 Ki = 7.943 nM 8.10
CHEMBL5181855 Ki = 7.943 nM 8.10
CHEMBL5202787 Ki = 7.943 nM 8.10
CHEMBL5202567 Ki = 7.943 nM 8.10
CHEMBL5207792 Ki = 10.0 nM 8.00
CHEMBL5170720 Ki = 25.12 nM 7.60
CHEMBL5193865 Ki = 25.12 nM 7.60
CHEMBL5203937 Ki = 39.81 nM 7.40
CHEMBL5180420 Ki = 199.53 nM 6.70