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Assay Detail

CHEMBL4817490

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Binding
Agonist activity at muscarinic M3 receptor in guinea pig trachea assessed as inhibition of carbachol-induced contraction
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Trachea
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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
IC50 11 8.71 9.80
pIC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4863525 1 9.80
CHEMBL4871517 1 9.80
CHEMBL4866806 1 9.50
CHEMBL4854091 1 9.10
CHEMBL4878138 1 9.10
CHEMBL4874819 1 9.00
CHEMBL4871702 1 9.00
CHEMBL4854418 1 8.10
CHEMBL4852629 1 7.80
CHEMBL4878395 1 7.30
CHEMBL4846536 1 7.30
CHEMBL4857743 1 -
CHEMBL4847910 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4863525 IC50 = 0.1585 nM 9.80
CHEMBL4871517 IC50 = 0.1585 nM 9.80
CHEMBL4866806 IC50 = 0.3162 nM 9.50
CHEMBL4854091 IC50 = 0.7943 nM 9.10
CHEMBL4878138 IC50 = 0.7943 nM 9.10
CHEMBL4874819 IC50 = 1.0 nM 9.00
CHEMBL4871702 IC50 = 1.0 nM 9.00
CHEMBL4854418 IC50 = 7.943 nM 8.10
CHEMBL4852629 IC50 = 15.85 nM 7.80
CHEMBL4878395 IC50 = 50.12 nM 7.30
CHEMBL4846536 IC50 = 50.12 nM 7.30
CHEMBL4857743 pIC50 - -
CHEMBL4847910 pIC50 - -