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Assay Detail

CHEMBL899143

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

Binding
Displacement of [3H]QNB from human muscarinic M2 receptor expressed in CHO cells
24
Total Activities
24
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 M2 (CHEMBL211)
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 24 6.54 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1256938 1 7.98
CHEMBL398043 1 7.40
CHEMBL239655 1 7.30
CHEMBL275104 1 7.16
CHEMBL239436 1 6.66
CHEMBL396845 1 6.32
CHEMBL239866 1 6.06
CHEMBL238825 1 5.69
CHEMBL239017 1 5.42
CHEMBL394329 1 5.39
CHEMBL239657 1 -
CHEMBL239652 1 -
CHEMBL239438 1 -
CHEMBL239865 1 -
CHEMBL239644 1 -
CHEMBL397538 1 -
CHEMBL395114 1 -
CHEMBL239426 1 -
CHEMBL240764 1 -
CHEMBL239038 1 -
CHEMBL238827 1 -
CHEMBL397083 1 -
CHEMBL240763 1 -
CHEMBL428916 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1256938 Ki = 10.38 nM 7.98
CHEMBL398043 Ki = 40.0 nM 7.40
CHEMBL239655 Ki = 50.0 nM 7.30
CHEMBL275104 Ki = 70.0 nM 7.16
CHEMBL239436 Ki = 219.0 nM 6.66
CHEMBL396845 Ki = 474.0 nM 6.32
CHEMBL239866 Ki = 876.0 nM 6.06
CHEMBL238825 Ki = 2041.0 nM 5.69
CHEMBL239017 Ki = 3796.0 nM 5.42
CHEMBL394329 Ki = 4099.0 nM 5.39
CHEMBL239657 Ki > 10000.0 nM -
CHEMBL239652 Ki > 10000.0 nM -
CHEMBL239438 Ki > 10000.0 nM -
CHEMBL239865 Ki > 10000.0 nM -
CHEMBL239644 Ki > 10000.0 nM -
CHEMBL397538 Ki > 10000.0 nM -
CHEMBL395114 Ki > 10000.0 nM -
CHEMBL239426 Ki > 10000.0 nM -
CHEMBL240764 Ki > 10000.0 nM -
CHEMBL239038 Ki > 10000.0 nM -
CHEMBL238827 Ki > 10000.0 nM -
CHEMBL397083 Ki > 10000.0 nM -
CHEMBL240763 Ki - -
CHEMBL428916 Ki > 10000.0 nM -