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Assay Detail

CHEMBL5503897

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

Binding
Displacement of Scopolamine methyl chloride,[N-methyl-3H] from human muscarinic M3 receptor assessed as inhibition constant incubated for 2 hrs by Microbeta scintillation counter
ChEMBL ↗
51
Total Activities
50
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, 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
Ki 51 9.34 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5556228 — — 1 11.00
CHEMBL5527849 — — 1 11.00
CHEMBL5527960 — — 1 10.90
CHEMBL5557828 — — 1 10.70
CHEMBL5172865 — — 1 10.20
CHEMBL5559208 — — 1 10.20
CHEMBL6067691 — — 1 10.20
CHEMBL5517637 — — 1 10.20
CHEMBL5550055 — — 1 10.00
CHEMBL5512435 — — 1 9.90
CHEMBL5505762 — — 1 9.80
CHEMBL5557651 — — 1 9.80
CHEMBL5556348 — — 1 9.80
CHEMBL5558368 — — 1 9.60
CHEMBL5505925 — — 1 9.60
CHEMBL5558093 — — 1 9.60
CHEMBL5555388 — — 1 9.60
CHEMBL6067689 — — 1 9.50
CHEMBL5542735 — — 1 9.50
CHEMBL5555665 — — 1 9.40
CHEMBL5532469 — — 1 9.40
CHEMBL5558303 — — 1 9.40
CHEMBL6067688 — — 1 9.40
CHEMBL5555464 — — 1 9.40
CHEMBL5532029 — — 1 9.30
CHEMBL5518087 — — 1 9.30
CHEMBL5556694 — — 1 9.20
CHEMBL5557509 — — 1 9.10
CHEMBL6067690 — — 1 9.10
CHEMBL5512578 — — 1 9.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5556228 — Ki = 0.01 nM 11.00
CHEMBL5527849 — Ki = 0.01 nM 11.00
CHEMBL5527960 — Ki = 0.01259 nM 10.90
CHEMBL5557828 — Ki = 0.01995 nM 10.70
CHEMBL5172865 — Ki = 0.0631 nM 10.20
CHEMBL5559208 — Ki = 0.0631 nM 10.20
CHEMBL6067691 — Ki = 0.0631 nM 10.20
CHEMBL5517637 — Ki = 0.0631 nM 10.20
CHEMBL5550055 — Ki = 0.1 nM 10.00
CHEMBL5512435 — Ki = 0.1259 nM 9.90
CHEMBL5556348 — Ki = 0.1585 nM 9.80
CHEMBL5557651 — Ki = 0.1585 nM 9.80
CHEMBL5505762 — Ki = 0.1585 nM 9.80
CHEMBL5558368 — Ki = 0.2512 nM 9.60
CHEMBL5558093 — Ki = 0.2512 nM 9.60
CHEMBL5505925 — Ki = 0.2512 nM 9.60
CHEMBL5555388 — Ki = 0.2512 nM 9.60
CHEMBL6067689 — Ki = 0.3162 nM 9.50
CHEMBL5542735 — Ki = 0.3162 nM 9.50
CHEMBL6067688 — Ki = 0.3981 nM 9.40
CHEMBL5558303 — Ki = 0.3981 nM 9.40
CHEMBL5532469 — Ki = 0.3981 nM 9.40
CHEMBL5555665 — Ki = 0.3981 nM 9.40
CHEMBL5555464 — Ki = 0.3981 nM 9.40
CHEMBL5532029 — Ki = 0.5012 nM 9.30
CHEMBL5518087 — Ki = 0.5012 nM 9.30
CHEMBL5556694 — Ki = 0.631 nM 9.20
CHEMBL5557509 — Ki = 0.7943 nM 9.10
CHEMBL5512578 — Ki = 0.7943 nM 9.10
CHEMBL6067690 — Ki = 0.7943 nM 9.10
CHEMBL5542277 — Ki = 1.0 nM 9.00
CHEMBL5555669 — Ki = 1.0 nM 9.00
CHEMBL5559271 — Ki = 1.259 nM 8.90
CHEMBL5542534 — Ki = 1.259 nM 8.90
CHEMBL5558825 — Ki = 1.585 nM 8.80
CHEMBL5542602 — Ki = 1.585 nM 8.80
CHEMBL5523340 — Ki = 1.585 nM 8.80
CHEMBL5517803 — Ki = 1.995 nM 8.70
CHEMBL5505816 — Ki = 1.995 nM 8.70
CHEMBL5542670 — Ki = 2.512 nM 8.60
CHEMBL5555744 — Ki = 3.162 nM 8.50
CHEMBL5523438 — Ki = 3.162 nM 8.50
CHEMBL5505816 — Ki = 3.981 nM 8.40
CHEMBL5523404 — Ki = 5.012 nM 8.30
CHEMBL5556756 — Ki = 7.943 nM 8.10
CHEMBL6067687 — Ki = 10.0 nM 8.00
CHEMBL5556153 — Ki = 12.59 nM 7.90
CHEMBL5523458 — Ki > 50.12 nM -
CHEMBL5557820 — Ki > 50.12 nM -
CHEMBL5558239 — Ki > 39.81 nM -