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Assay Detail

CHEMBL745193

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Functional
Antagonistic activity against muscarinic acetylcholine receptor M2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.
Boyle CD, Chackalamannil S, Clader JW, Greenlee WJ, Josien HB, Kaminski JJ, Kozlowski JA, McCombie SW, Nazareno DV, Tagat JR, Wang Y, Zhou G, Billard W, Binch H, Crosby G, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE.
Bioorg Med Chem Lett (2001) 11 : 2311 -2314
PubMed 11527721 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.28 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL305693 1 9.85
CHEMBL309720 1 9.70
CHEMBL311099 1 9.29
CHEMBL74141 1 9.29
CHEMBL78131 1 9.09
CHEMBL308166 1 8.92
CHEMBL311054 1 8.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL305693 Ki = 0.14 nM 9.85
CHEMBL309720 Ki = 0.2 nM 9.70
CHEMBL311099 Ki = 0.51 nM 9.29
CHEMBL74141 Ki = 0.51 nM 9.29
CHEMBL78131 Ki = 0.81 nM 9.09
CHEMBL308166 Ki = 1.2 nM 8.92
CHEMBL311054 Ki = 1.4 nM 8.85