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Assay Detail

CHEMBL899145

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

Binding
Displacement of [3H]QNB from human muscarinic M4 receptor expressed in CHO cells
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 Intermediate

Target

Muscarinic acetylcholine receptor M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.
Dallanoce C, De Amici M, Barocelli E, Bertoni S, Roth BL, Ernsberger P, De Micheli C.
Bioorg Med Chem (2007) 15 : 7626 -7637
PubMed 17889543 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.72 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275104 1 6.65
CHEMBL239655 1 6.17
CHEMBL398043 1 6.10
CHEMBL239017 1 5.96
CHEMBL239436 1 5.77
CHEMBL396845 1 5.64
CHEMBL428916 1 5.26
CHEMBL238825 1 5.23
CHEMBL239866 1 5.22
CHEMBL239038 1 5.22
CHEMBL394329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275104 Ki = 222.0 nM 6.65
CHEMBL239655 Ki = 682.0 nM 6.17
CHEMBL398043 Ki = 792.0 nM 6.10
CHEMBL239017 Ki = 1095.0 nM 5.96
CHEMBL239436 Ki = 1681.0 nM 5.77
CHEMBL396845 Ki = 2265.0 nM 5.64
CHEMBL428916 Ki = 5478.0 nM 5.26
CHEMBL238825 Ki = 5932.0 nM 5.23
CHEMBL239866 Ki = 6041.0 nM 5.22
CHEMBL239038 Ki = 5986.0 nM 5.22
CHEMBL394329 Ki > 10000.0 nM -