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Assay Detail

CHEMBL745631

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

Binding
Binding affinity towards Muscarinic acetylcholine receptor M2
25
Total Activities
25
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 (CHEMBL309)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
Boyle CD, Vice SF, Campion J, Chackalamannil S, Lankin CM, McCombie SW, Billard W, Binch H, Crosby G, Williams MC, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE.
Bioorg Med Chem Lett (2002) 12 : 3479 -3482
PubMed 12419388 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.95 10.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119294 1 10.19
CHEMBL332703 1 9.41
CHEMBL324484 1 9.40
CHEMBL117351 1 9.36
CHEMBL118391 1 9.29
CHEMBL331214 1 9.28
CHEMBL119131 1 9.28
CHEMBL116777 1 9.27
CHEMBL117414 1 9.17
CHEMBL326561 1 9.14
CHEMBL324116 1 9.11
CHEMBL326057 1 9.07
CHEMBL326990 1 9.05
CHEMBL117817 1 9.00
CHEMBL332702 1 8.96
CHEMBL323850 1 8.92
CHEMBL116781 1 8.85
CHEMBL117797 1 8.82
CHEMBL115681 1 8.80
CHEMBL119168 1 8.74
CHEMBL325451 1 8.64
CHEMBL115807 1 8.60
CHEMBL324832 1 8.32
CHEMBL115642 1 7.75
CHEMBL116404 1 7.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119294 Ki = 0.065 nM 10.19
CHEMBL332703 Ki = 0.39 nM 9.41
CHEMBL324484 Ki = 0.4 nM 9.40
CHEMBL117351 Ki = 0.44 nM 9.36
CHEMBL118391 Ki = 0.51 nM 9.29
CHEMBL331214 Ki = 0.53 nM 9.28
CHEMBL119131 Ki = 0.53 nM 9.28
CHEMBL116777 Ki = 0.54 nM 9.27
CHEMBL117414 Ki = 0.68 nM 9.17
CHEMBL326561 Ki = 0.72 nM 9.14
CHEMBL324116 Ki = 0.78 nM 9.11
CHEMBL326057 Ki = 0.86 nM 9.07
CHEMBL326990 Ki = 0.9 nM 9.05
CHEMBL117817 Ki = 1.0 nM 9.00
CHEMBL332702 Ki = 1.1 nM 8.96
CHEMBL323850 Ki = 1.2 nM 8.92
CHEMBL116781 Ki = 1.4 nM 8.85
CHEMBL117797 Ki = 1.5 nM 8.82
CHEMBL115681 Ki = 1.6 nM 8.80
CHEMBL119168 Ki = 1.8 nM 8.74
CHEMBL325451 Ki = 2.3 nM 8.64
CHEMBL115807 Ki = 2.5 nM 8.60
CHEMBL324832 Ki = 4.8 nM 8.32
CHEMBL115642 Ki = 18.0 nM 7.75
CHEMBL116404 Ki = 51.0 nM 7.29