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Assay Detail

CHEMBL1775313

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

Binding
Displacement of [3H]N-methyl Scopolamine from human muscarinic M3 receptor expressed in CHO cells by scintillation proximity assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhalation by design: dual pharmacology β-2 agonists/M3 antagonists for the treatment of COPD.
Jones LH, Baldock H, Bunnage ME, Burrows J, Clarke N, Coghlan M, Entwistle D, Fairman D, Feeder N, Fulton C, Hilton L, James K, Jones RM, Kenyon AS, Marshall S, Newman SD, Osborne R, Patel S, Selby MD, Stuart EF, Trevethick MA, Wright KN, Price DA.
Bioorg Med Chem Lett (2011) 21 : 2759 -2763
PubMed 21075627 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 9.06 10.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1773196 1 10.04
CHEMBL1773197 1 9.56
CHEMBL1773267 1 9.52
CHEMBL1773198 1 9.40
CHEMBL1773264 1 9.20
CHEMBL1773074 1 9.12
CHEMBL1773266 1 9.00
CHEMBL1773263 1 8.84
CHEMBL1382 TOLTERODINE 4.0 1 8.44
CHEMBL1773265 1 8.33
CHEMBL1773262 1 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1773196 Ki = 0.091 nM 10.04
CHEMBL1773197 Ki = 0.276 nM 9.56
CHEMBL1773267 Ki = 0.305 nM 9.52
CHEMBL1773198 Ki = 0.397 nM 9.40
CHEMBL1773264 Ki = 0.634 nM 9.20
CHEMBL1773074 Ki = 0.765 nM 9.12
CHEMBL1773266 Ki = 0.99 nM 9.00
CHEMBL1773263 Ki = 1.45 nM 8.84
CHEMBL1382 TOLTERODINE Ki = 3.6 nM 8.44
CHEMBL1773265 Ki = 4.7 nM 8.33
CHEMBL1773262 Ki = 6.1 nM 8.21