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Assay Detail

CHEMBL875217

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

Binding
In vitro inhibitory activity against cloned human M2 muscarinic receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Chackalamannil S, Doller D, McQuade R, Ruperto V.
Bioorg Med Chem Lett (2004) 14 : 3967 -3970
PubMed 15225708 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.35 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355854 1 8.37
CHEMBL277642 HIMBACINE 1 8.35
CHEMBL183903 1 7.91
CHEMBL182761 1 7.88
CHEMBL427145 1 7.80
CHEMBL184843 1 7.37
CHEMBL181447 1 7.17
CHEMBL363895 1 6.75
CHEMBL360988 1 6.69
CHEMBL183331 1 6.35
CHEMBL362864 1 6.24
CHEMBL433566 1 -
CHEMBL360904 1 -
CHEMBL182777 1 -
CHEMBL359847 1 -
CHEMBL360154 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355854 Ki = 4.3 nM 8.37
CHEMBL277642 HIMBACINE Ki = 4.5 nM 8.35
CHEMBL183903 Ki = 12.2 nM 7.91
CHEMBL182761 Ki = 13.3 nM 7.88
CHEMBL427145 Ki = 16.0 nM 7.80
CHEMBL184843 Ki = 43.0 nM 7.37
CHEMBL181447 Ki = 68.0 nM 7.17
CHEMBL363895 Ki = 180.0 nM 6.75
CHEMBL360988 Ki = 203.0 nM 6.69
CHEMBL183331 Ki = 449.0 nM 6.35
CHEMBL362864 Ki = 571.0 nM 6.24
CHEMBL433566 Ki > 1400.0 nM -
CHEMBL360904 Ki > 1400.0 nM -
CHEMBL182777 Ki > 1400.0 nM -
CHEMBL359847 Ki > 1400.0 nM -
CHEMBL360154 Ki > 1400.0 nM -