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Assay Detail

CHEMBL2380039

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

Binding
Displacement of [3H] N-methylscopolamine from muscarinic M2 receptor in guinea pig brain homogenate after 30 mins by scintillation counting analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4 6.96 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26505 APROFENE 2.0 1 7.58
CHEMBL37372 1 7.36
CHEMBL2377384 1 6.59
CHEMBL2110892 BIETAMIVERINE 2.0 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26505 APROFENE Ki = 26.5 nM 7.58
CHEMBL37372 Ki = 44.0 nM 7.36
CHEMBL2377384 Ki = 254.0 nM 6.59
CHEMBL2110892 BIETAMIVERINE Ki = 517.0 nM 6.29