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Assay Detail

CHEMBL5503901

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Functional
Inhibition of carbachol-induced smooth muscle contraction in male albino Dunkin-Hartley guinea pig trachea
19
Total Activities
18
Compounds Tested
2
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, Multiparametric Optimization, and Solid-State Driven Identification of CHF-6550, a Novel 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, Schmidt W, Knight CK, Mileo V, Amadei F, Pastore F, Miglietta D, Cesari N, Riccardi B, Mazzucato R, Ghidini E, Blackaby WP, Patacchini R, Battipaglia L, Villetti G, Puccini P, Catinella S, Civelli M, Rancati F.
J Med Chem (2024) 67 : 9816 -9841
PubMed 38857426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 9.55 10.70
pIC50 6 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5555744 1 10.70
CHEMBL5505816 2 10.30
CHEMBL5532029 1 9.90
CHEMBL5558368 1 9.90
CHEMBL5550055 1 9.80
CHEMBL6067687 1 9.60
CHEMBL5172865 1 9.50
CHEMBL5555665 1 9.30
CHEMBL5527960 1 9.30
CHEMBL5517637 1 9.10
CHEMBL5505925 1 9.00
CHEMBL5542735 1 9.00
CHEMBL5512435 1 8.80
CHEMBL5523458 1 -
CHEMBL5556153 1 -
CHEMBL5523340 1 -
CHEMBL5542602 1 -
CHEMBL5556756 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5555744 IC50 = 0.01995 nM 10.70
CHEMBL5505816 IC50 = 0.05012 nM 10.30
CHEMBL5532029 IC50 = 0.1259 nM 9.90
CHEMBL5558368 IC50 = 0.1259 nM 9.90
CHEMBL5550055 IC50 = 0.1585 nM 9.80
CHEMBL6067687 IC50 = 0.2512 nM 9.60
CHEMBL5172865 IC50 = 0.3162 nM 9.50
CHEMBL5555665 IC50 = 0.5012 nM 9.30
CHEMBL5527960 IC50 = 0.5012 nM 9.30
CHEMBL5517637 IC50 = 0.7943 nM 9.10
CHEMBL5505925 IC50 = 1.0 nM 9.00
CHEMBL5542735 IC50 = 1.0 nM 9.00
CHEMBL5512435 IC50 = 1.585 nM 8.80
CHEMBL5523458 pIC50 - -
CHEMBL5556153 pIC50 - -
CHEMBL5505816 pIC50 - -
CHEMBL5523340 pIC50 - -
CHEMBL5542602 pIC50 - -
CHEMBL5556756 pIC50 - -