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Assay Detail

CHEMBL4026883

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

Binding
Displacement of [3H]N-methyl-scopolamine from human recombinant muscarinic M1 receptor expressed in CHO-FlpIn cells after 6 hrs by liquid scintillation counting method
6
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 M1 (CHEMBL216)
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
Ki 6 4.70 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4060823 2 5.17
CHEMBL667 ACETYLCHOLINE 4.0 2 4.64
CHEMBL4091934 2 4.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4060823 Ki = 6760.83 nM 5.17
CHEMBL4060823 Ki = 6800.0 nM 5.17
CHEMBL667 ACETYLCHOLINE Ki = 22908.68 nM 4.64
CHEMBL667 ACETYLCHOLINE Ki = 23000.0 nM 4.64
CHEMBL4091934 Ki = 52480.75 nM 4.28
CHEMBL4091934 Ki = 52000.0 nM 4.28