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Assay Detail

CHEMBL899150

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Functional
Agonist activity at muscarinic M3 receptor in guinea-pig ileum
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Ileum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M3 (CHEMBL5498)
Type SINGLE PROTEIN
Organism Cavia porcellus

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
EC50 9 6.16 8.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239655 1 8.14
CHEMBL239436 1 6.57
CHEMBL1482 BETHANECHOL 4.0 1 6.37
CHEMBL238825 1 6.26
CHEMBL239017 1 6.10
CHEMBL240763 1 5.99
CHEMBL239866 1 5.75
CHEMBL240764 1 5.45
CHEMBL397083 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239655 EC50 = 7.244 nM 8.14
CHEMBL239436 EC50 = 269.15 nM 6.57
CHEMBL1482 BETHANECHOL EC50 = 426.58 nM 6.37
CHEMBL238825 EC50 = 549.54 nM 6.26
CHEMBL239017 EC50 = 794.33 nM 6.10
CHEMBL240763 EC50 = 1023.29 nM 5.99
CHEMBL239866 EC50 = 1778.28 nM 5.75
CHEMBL240764 EC50 = 3548.13 nM 5.45
CHEMBL397083 EC50 = 15135.61 nM 4.82