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Assay Detail

CHEMBL2380040

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Binding
Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor after 30 mins by scintillation counting analysis
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

Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.
Bhattacharjee AK, Pomponio JW, Evans SA, Pervitsky D, Gordon RK.
Bioorg Med Chem (2013) 21 : 2651 -2662
PubMed 23523385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.77 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26505 APROFENE 2.0 1 7.58
CHEMBL37372 1 7.36
CHEMBL2377383 1 7.18
CHEMBL2377385 1 6.79
CHEMBL2377384 1 6.59
CHEMBL2110892 BIETAMIVERINE 2.0 1 6.29
CHEMBL2377262 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26505 APROFENE Ki = 26.5 nM 7.58
CHEMBL37372 Ki = 44.0 nM 7.36
CHEMBL2377383 Ki = 65.5 nM 7.18
CHEMBL2377385 Ki = 164.0 nM 6.79
CHEMBL2377384 Ki = 254.0 nM 6.59
CHEMBL2110892 BIETAMIVERINE Ki = 517.0 nM 6.29
CHEMBL2377262 Ki = 2670.0 nM 5.57