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Assay Detail

CHEMBL5129844

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

Functional
In vivo bifunctional antagonist activity at muscarinic M3 receptor /agonist activity at beta-2 adrenoceptor in Dunkin-Hartley guinea pig trachea assessed as inhibition of carbachol induced contraction
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Trachea
Confidence 1 — Organism
Curated By Autocuration

Target

Trachea (CHEMBL4296541)
Type TISSUE
Organism Cavia porcellus

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
IC50 8 9.50 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208201 1 10.10
CHEMBL5184455 1 10.00
CHEMBL5190387 1 9.70
CHEMBL5208957 1 9.60
CHEMBL5172865 1 9.50
CHEMBL5193853 1 9.30
CHEMBL5200887 1 8.90
CHEMBL5184598 1 8.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208201 IC50 = 0.07943 nM 10.10
CHEMBL5184455 IC50 = 0.1 nM 10.00
CHEMBL5190387 IC50 = 0.1995 nM 9.70
CHEMBL5208957 IC50 = 0.2512 nM 9.60
CHEMBL5172865 IC50 = 0.3162 nM 9.50
CHEMBL5193853 IC50 = 0.5012 nM 9.30
CHEMBL5200887 IC50 = 1.259 nM 8.90
CHEMBL5184598 IC50 = 1.259 nM 8.90