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Assay Detail

CHEMBL899142

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

Binding
Displacement of [3H]QNB from human muscarinic M1 receptor expressed in CHO cells
12
Total Activities
12
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 M1 (CHEMBL216)
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 12 5.69 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9967 PIRENZEPINE 2.0 1 7.67
CHEMBL398043 1 6.09
CHEMBL275104 1 6.04
CHEMBL239038 1 5.47
CHEMBL239866 1 5.34
CHEMBL428916 1 5.21
CHEMBL396845 1 5.16
CHEMBL239436 1 5.13
CHEMBL238825 1 5.12
CHEMBL239017 1 -
CHEMBL394329 1 -
CHEMBL239655 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9967 PIRENZEPINE Ki = 21.38 nM 7.67
CHEMBL398043 Ki = 819.0 nM 6.09
CHEMBL275104 Ki = 905.0 nM 6.04
CHEMBL239038 Ki = 3376.0 nM 5.47
CHEMBL239866 Ki = 4550.0 nM 5.34
CHEMBL428916 Ki = 6141.0 nM 5.21
CHEMBL396845 Ki = 6958.0 nM 5.16
CHEMBL239436 Ki = 7367.0 nM 5.13
CHEMBL238825 Ki = 7680.0 nM 5.12
CHEMBL239017 Ki > 10000.0 nM -
CHEMBL394329 Ki > 10000.0 nM -
CHEMBL239655 Ki > 10000.0 nM -