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Assay Detail

CHEMBL744231

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

Binding
In Vitro evaluation activity at the cloned Human Muscarinic acetylcholine receptor M1 determined by receptor selection and amplification technology (R-SAT)
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors.
Bräuner-Osborne H, Ebert B, Brann MR, Falch E, Krogsgaard-Larsen P.
J Med Chem (1995) 38 : 2188 -2195
PubMed 7783150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.32 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69305 1 7.02
CHEMBL69306 1 6.85
CHEMBL305264 1 6.77
CHEMBL7634 OXOTREMORINE 1 6.41
CHEMBL304142 1 6.34
CHEMBL7303 ARECOLINE -1.0 1 5.50
CHEMBL14 CARBACHOL 4.0 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69305 EC50 = 95.0 nM 7.02
CHEMBL69306 EC50 = 140.0 nM 6.85
CHEMBL305264 EC50 = 170.0 nM 6.77
CHEMBL7634 OXOTREMORINE EC50 = 390.0 nM 6.41
CHEMBL304142 EC50 = 460.0 nM 6.34
CHEMBL7303 ARECOLINE EC50 = 3200.0 nM 5.50
CHEMBL14 CARBACHOL EC50 = 4600.0 nM 5.34