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Assay Detail

CHEMBL746846

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

Binding
Allosteric potency against the dissociation of radioligand [3H]N-methylscopolamine from the porcine cardiac Muscarinic acetylcholine receptor M2
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL4781)
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Bisquaternary ligands of the common allosteric site of M2 acetylcholine receptors: search for the minimum essential distances between the pharmacophoric elements.
Nassif-Makki T, Tränkle C, Zlotos D, Bejeuhr G, Cambareri A, Pfletschinger C, Kostenis E, Mohr K, Holzgrabe U.
J Med Chem (1999) 42 : 849 -858
PubMed 10072682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 5.84 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169638 1 6.46
CHEMBL168840 1 6.43
CHEMBL169633 1 6.35
CHEMBL352486 1 6.33
CHEMBL169342 1 6.29
CHEMBL354103 1 6.29
CHEMBL169475 1 6.28
CHEMBL352323 1 6.28
CHEMBL169001 1 6.24
CHEMBL168613 1 6.20
CHEMBL168760 1 5.86
CHEMBL171664 1 5.85
CHEMBL266295 1 5.84
CHEMBL171388 1 5.72
CHEMBL171776 1 5.63
CHEMBL165814 1 5.57
CHEMBL352356 1 5.46
CHEMBL353262 1 5.42
CHEMBL354750 1 5.33
CHEMBL354673 1 5.31
CHEMBL171215 1 5.05
CHEMBL169133 1 4.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169638 EC50 = 350.0 nM 6.46
CHEMBL168840 EC50 = 370.0 nM 6.43
CHEMBL169633 EC50 = 450.0 nM 6.35
CHEMBL352486 EC50 = 470.0 nM 6.33
CHEMBL169342 EC50 = 510.0 nM 6.29
CHEMBL354103 EC50 = 510.0 nM 6.29
CHEMBL169475 EC50 = 520.0 nM 6.28
CHEMBL352323 EC50 = 530.0 nM 6.28
CHEMBL169001 EC50 = 570.0 nM 6.24
CHEMBL168613 EC50 = 630.0 nM 6.20
CHEMBL168760 EC50 = 1390.0 nM 5.86
CHEMBL171664 EC50 = 1400.0 nM 5.85
CHEMBL266295 EC50 = 1440.0 nM 5.84
CHEMBL171388 EC50 = 1900.0 nM 5.72
CHEMBL171776 EC50 = 2340.0 nM 5.63
CHEMBL165814 EC50 = 2690.0 nM 5.57
CHEMBL352356 EC50 = 3490.0 nM 5.46
CHEMBL353262 EC50 = 3800.0 nM 5.42
CHEMBL354750 EC50 = 4650.0 nM 5.33
CHEMBL354673 EC50 = 4870.0 nM 5.31
CHEMBL171215 EC50 = 8820.0 nM 5.05
CHEMBL169133 EC50 = 50800.0 nM 4.29