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Assay Detail

CHEMBL4026895

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Binding
Agonist activity at recombinant human muscarinic M2 receptor expressed in HEK293 cells co-expressing beta-arrestin assessed as increase in beta-arrestin recruitment after 24 hrs by Bright-Glo luminescence assay
6
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Based Design and Discovery of New M2 Receptor Agonists.
Fish I, Stößel A, Eitel K, Valant C, Albold S, Huebner H, Möller D, Clark MJ, Sunahara RK, Christopoulos A, Shoichet BK, Gmeiner P.
J Med Chem (2017) 60 : 9239 -9250
PubMed 29094937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.11 5.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL667 ACETYLCHOLINE 4.0 2 5.72
CHEMBL4091934 2 4.85
CHEMBL4060823 2 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL667 ACETYLCHOLINE EC50 = 1905.46 nM 5.72
CHEMBL667 ACETYLCHOLINE EC50 = 1900.0 nM 5.72
CHEMBL4091934 EC50 = 14125.38 nM 4.85
CHEMBL4091934 EC50 = 14000.0 nM 4.85
CHEMBL4060823 EC50 = 17000.0 nM 4.77
CHEMBL4060823 EC50 = 17378.01 nM 4.76