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Assay Detail

CHEMBL5239841

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

Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M4 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Muscarinic acetylcholine receptor M4 (CHEMBL1821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, Characterization, and Application of Muscarinergic M<sub>3</sub> Receptor Ligands Linked to Fluorescent Dyes.
Köckenberger J, Fischer O, Konopa A, Bergwinkl S, Mühlich S, Gmeiner P, Kutta RJ, Hübner H, Keller M, Heinrich MR.
J Med Chem (2022) 65 : 16494 -16509
PubMed 36484801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.78 9.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5289601 1 9.25
CHEMBL5289667 1 9.07
CHEMBL5271406 1 9.06
CHEMBL5273907 1 9.05
CHEMBL5285607 1 8.85
CHEMBL5289083 1 8.77
CHEMBL5268503 1 8.59
CHEMBL5283759 1 8.48
CHEMBL5267836 1 8.42
CHEMBL5277670 1 8.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5289601 Ki = 0.56 nM 9.25
CHEMBL5289667 Ki = 0.86 nM 9.07
CHEMBL5271406 Ki = 0.87 nM 9.06
CHEMBL5273907 Ki = 0.9 nM 9.05
CHEMBL5285607 Ki = 1.4 nM 8.85
CHEMBL5289083 Ki = 1.7 nM 8.77
CHEMBL5268503 Ki = 2.6 nM 8.59
CHEMBL5283759 Ki = 3.3 nM 8.48
CHEMBL5267836 Ki = 3.8 nM 8.42
CHEMBL5277670 Ki = 5.4 nM 8.27