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Assay Detail

CHEMBL2067887

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

Binding
Positive allosteric modulation activity at muscarinic M1 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.
Melancon BJ, Hopkins CR, Wood MR, Emmitte KA, Niswender CM, Christopoulos A, Conn PJ, Lindsley CW.
J Med Chem (2012) 55 : 1445 -1464
PubMed 22148748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.41 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2063422 1 7.39
CHEMBL596507 1 7.08
CHEMBL596508 1 6.57
CHEMBL596506 1 6.42
CHEMBL608112 1 6.09
CHEMBL1083203 1 6.08
CHEMBL523685 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2063422 EC50 = 41.0 nM 7.39
CHEMBL596507 EC50 = 84.0 nM 7.08
CHEMBL596508 EC50 = 270.0 nM 6.57
CHEMBL596506 EC50 = 380.0 nM 6.42
CHEMBL608112 EC50 = 820.0 nM 6.09
CHEMBL1083203 EC50 = 830.0 nM 6.08
CHEMBL523685 EC50 = 6000.0 nM 5.22