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Assay Detail

CHEMBL5239840

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

Binding
Displacement of [3H]N-methylscopolamine from human muscarinic M3 receptor expressed in human HEK293T cell membranes by radioligand competition binding based analysis
20
Total Activities
20
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 M3 (CHEMBL245)
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 20 8.80 10.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4636528 1 10.19
CHEMBL5281043 1 10.09
CHEMBL5270870 1 9.82
CHEMBL5284000 1 9.55
CHEMBL5265833 1 9.49
CHEMBL5289667 1 9.22
CHEMBL5279174 1 9.11
CHEMBL5270925 1 9.00
CHEMBL5285607 1 8.92
CHEMBL5287315 1 8.74
CHEMBL5282659 1 8.59
CHEMBL5268503 1 8.51
CHEMBL5289601 1 8.49
CHEMBL5274390 1 8.37
CHEMBL5273907 1 8.20
CHEMBL5283759 1 8.17
CHEMBL5289083 1 8.11
CHEMBL5267836 1 7.92
CHEMBL5271406 1 7.85
CHEMBL5277670 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4636528 Ki = 0.064 nM 10.19
CHEMBL5281043 Ki = 0.081 nM 10.09
CHEMBL5270870 Ki = 0.15 nM 9.82
CHEMBL5284000 Ki = 0.28 nM 9.55
CHEMBL5265833 Ki = 0.32 nM 9.49
CHEMBL5289667 Ki = 0.6 nM 9.22
CHEMBL5279174 Ki = 0.77 nM 9.11
CHEMBL5270925 Ki = 1.0 nM 9.00
CHEMBL5285607 Ki = 1.2 nM 8.92
CHEMBL5287315 Ki = 1.8 nM 8.74
CHEMBL5282659 Ki = 2.6 nM 8.59
CHEMBL5268503 Ki = 3.1 nM 8.51
CHEMBL5289601 Ki = 3.2 nM 8.49
CHEMBL5274390 Ki = 4.3 nM 8.37
CHEMBL5273907 Ki = 6.3 nM 8.20
CHEMBL5283759 Ki = 6.8 nM 8.17
CHEMBL5289083 Ki = 7.7 nM 8.11
CHEMBL5267836 Ki = 12.0 nM 7.92
CHEMBL5271406 Ki = 14.0 nM 7.85
CHEMBL5277670 Ki = 27.0 nM 7.57