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Assay Detail

CHEMBL3227039

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

Binding
Displacement of [3H]-N-methyl scopolamine from human cloned muscarinic M3 receptor
27
Total Activities
27
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

Optimized glucuronidation of dual pharmacology -2 agonists/M3 antagonists for the treatment of COPD
Hilton L, Osborne R, Kenyon AS, Baldock H, Bunnage ME, Burrows J, Clarke N, Coghlan M, Entwistle D, Fairman D, Feeder N, James K, Jones RM, Laouar N, Lunn G, Marshall S, Newman SD, Patel S, Selby MD, Spence F, Stuart EF, Summerhill S, Trevethick MA, Wright KN, Yeadon M, Price DA, Jones LH
Medchemcomm (2011) 2 : 870 -876
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.32 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3219031 1 9.41
CHEMBL3219042 1 9.14
CHEMBL1683934 1 9.09
CHEMBL3219048 1 8.96
CHEMBL3219046 1 8.96
CHEMBL3219053 1 8.89
CHEMBL3219049 1 8.70
CHEMBL3219044 1 8.70
CHEMBL3219032 1 8.66
CHEMBL3219056 1 8.51
CHEMBL3219033 1 8.43
CHEMBL3219052 1 8.37
CHEMBL3219047 1 8.36
CHEMBL3219050 1 8.36
CHEMBL3219043 1 8.32
CHEMBL3219040 1 8.30
CHEMBL3219041 1 8.08
CHEMBL3219054 1 8.05
CHEMBL3219051 1 8.04
CHEMBL3219036 1 8.00
CHEMBL3219034 1 7.75
CHEMBL3219038 1 7.66
CHEMBL3219035 1 7.58
CHEMBL3219055 1 7.44
CHEMBL3219045 1 7.42
CHEMBL3219039 1 7.12
CHEMBL3219037 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3219031 Ki = 0.39 nM 9.41
CHEMBL3219042 Ki = 0.73 nM 9.14
CHEMBL1683934 Ki = 0.82 nM 9.09
CHEMBL3219048 Ki = 1.1 nM 8.96
CHEMBL3219046 Ki = 1.1 nM 8.96
CHEMBL3219053 Ki = 1.3 nM 8.89
CHEMBL3219049 Ki = 2.0 nM 8.70
CHEMBL3219044 Ki = 2.0 nM 8.70
CHEMBL3219032 Ki = 2.2 nM 8.66
CHEMBL3219056 Ki = 3.1 nM 8.51
CHEMBL3219033 Ki = 3.7 nM 8.43
CHEMBL3219052 Ki = 4.3 nM 8.37
CHEMBL3219047 Ki = 4.4 nM 8.36
CHEMBL3219050 Ki = 4.4 nM 8.36
CHEMBL3219043 Ki = 4.8 nM 8.32
CHEMBL3219040 Ki = 5.0 nM 8.30
CHEMBL3219041 Ki = 8.3 nM 8.08
CHEMBL3219054 Ki = 8.9 nM 8.05
CHEMBL3219051 Ki = 9.2 nM 8.04
CHEMBL3219036 Ki = 10.0 nM 8.00
CHEMBL3219034 Ki = 18.0 nM 7.75
CHEMBL3219038 Ki = 22.0 nM 7.66
CHEMBL3219035 Ki = 26.0 nM 7.58
CHEMBL3219055 Ki = 36.0 nM 7.44
CHEMBL3219045 Ki = 38.0 nM 7.42
CHEMBL3219039 Ki = 76.0 nM 7.12
CHEMBL3219037 Ki > 73.0 nM -