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Assay Detail

CHEMBL4716041

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

Binding
Displacement of [3H]NMS from human recombinant muscarinic receptor M1 expressed in CHO-K9 cell membranes measured after 3 hrs by radioligand competition binding assay
9
Total Activities
9
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 9 8.69 10.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634333 1 10.50
CHEMBL4794548 1 9.30
CHEMBL4742721 1 9.00
CHEMBL4756833 1 8.59
CHEMBL4748004 1 8.32
CHEMBL4754371 1 8.31
CHEMBL4789147 1 8.21
CHEMBL4744233 1 8.15
CHEMBL4650998 1 7.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634333 Ki = 0.03162 nM 10.50
CHEMBL4794548 Ki = 0.5012 nM 9.30
CHEMBL4742721 Ki = 1.0 nM 9.00
CHEMBL4756833 Ki = 2.57 nM 8.59
CHEMBL4748004 Ki = 4.786 nM 8.32
CHEMBL4754371 Ki = 4.898 nM 8.31
CHEMBL4789147 Ki = 6.166 nM 8.21
CHEMBL4744233 Ki = 7.079 nM 8.15
CHEMBL4650998 Ki = 13.8 nM 7.86