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Assay Detail

CHEMBL4026901

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

Binding
Agonist activity at recombinant human muscarinic M3 receptor expressed in CHO cells assessed as upregulation in ERK1/2 phosphorylation after 5 mins by alphascreen assay
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
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 4 7.64 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL667 ACETYLCHOLINE 4.0 2 7.64
CHEMBL4091934 1 -
CHEMBL4060823 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL667 ACETYLCHOLINE EC50 = 22.91 nM 7.64
CHEMBL667 ACETYLCHOLINE EC50 = 23.0 nM 7.64
CHEMBL4091934 EC50 - -
CHEMBL4060823 EC50 - -