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Assay Detail

CHEMBL4716042

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

Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M2 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K9
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M2R affinity
Gruber, Corinna G., Pegoli, Andrea, Muller, Christoph, Gratz, Lukas, She, Xueke, Keller, Max
RSC Med Chem (2020) 11 : 823 -832
PubMed 33479678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 9.15 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634333 1 10.40
CHEMBL4756833 1 9.62
CHEMBL4636083 1 9.25
CHEMBL4645845 1 9.23
CHEMBL4742721 1 9.16
CHEMBL4754371 1 9.04
CHEMBL4748004 1 9.02
CHEMBL4744233 1 8.87
CHEMBL4794548 1 8.80
CHEMBL4789147 1 8.75
CHEMBL4650998 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634333 Ki = 0.03981 nM 10.40
CHEMBL4756833 Ki = 0.2399 nM 9.62
CHEMBL4636083 Ki = 0.5623 nM 9.25
CHEMBL4645845 Ki = 0.5888 nM 9.23
CHEMBL4742721 Ki = 0.6918 nM 9.16
CHEMBL4754371 Ki = 0.912 nM 9.04
CHEMBL4748004 Ki = 0.955 nM 9.02
CHEMBL4744233 Ki = 1.349 nM 8.87
CHEMBL4794548 Ki = 1.585 nM 8.80
CHEMBL4789147 Ki = 1.778 nM 8.75
CHEMBL4650998 Ki = 3.02 nM 8.52