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Assay Detail

CHEMBL899148

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Functional
Agonist activity at muscarinic M2 receptor in electrically stimulated guinea-pig left atrium
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Cardiac atrium
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 6.34 8.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239655 1 8.18
CHEMBL239436 1 7.34
CHEMBL238825 1 6.60
CHEMBL239017 1 6.29
CHEMBL1482 BETHANECHOL 4.0 1 6.19
CHEMBL239866 1 5.96
CHEMBL240763 1 5.51
CHEMBL428916 1 4.66
CHEMBL240764 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239655 EC50 = 6.607 nM 8.18
CHEMBL239436 EC50 = 45.71 nM 7.34
CHEMBL238825 EC50 = 251.19 nM 6.60
CHEMBL239017 EC50 = 512.86 nM 6.29
CHEMBL1482 BETHANECHOL EC50 = 645.65 nM 6.19
CHEMBL239866 EC50 = 1096.48 nM 5.96
CHEMBL240763 EC50 = 3090.3 nM 5.51
CHEMBL428916 EC50 = 21877.62 nM 4.66
CHEMBL240764 EC50 < 100000.0 nM -