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Assay Detail

CHEMBL747619

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Binding
Binding affinity against Muscarinic acetylcholine receptor M2
15
Total Activities
15
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 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diphenylsulfone muscarinic antagonists: piperidine derivatives with high M2 selectivity and improved potency.
Billard W, Binch H, Bratzler K, Chen LY, Crosby G, Duffy RA, Dugar S, Lachowicz J, McQuade R, Pushpavanam P, Ruperto VB, Taylor LA, Clader JW.
Bioorg Med Chem Lett (2000) 10 : 2209 -2212
PubMed 11012031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.89 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2114068 1 10.52
CHEMBL2115128 1 10.24
CHEMBL71124 1 9.85
CHEMBL71147 1 9.77
CHEMBL70828 1 9.43
CHEMBL307810 1 9.00
CHEMBL69595 1 8.89
CHEMBL2111540 1 8.56
CHEMBL71531 1 8.51
CHEMBL2114067 1 8.45
CHEMBL2115126 1 8.15
CHEMBL71971 1 8.14
CHEMBL2114064 1 8.12
CHEMBL2115127 1 7.97
CHEMBL2114066 1 7.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2114068 Ki = 0.03 nM 10.52
CHEMBL2115128 Ki = 0.057 nM 10.24
CHEMBL71124 Ki = 0.14 nM 9.85
CHEMBL71147 Ki = 0.17 nM 9.77
CHEMBL70828 Ki = 0.37 nM 9.43
CHEMBL307810 Ki = 1.0 nM 9.00
CHEMBL69595 Ki = 1.3 nM 8.89
CHEMBL2111540 Ki = 2.78 nM 8.56
CHEMBL71531 Ki = 3.07 nM 8.51
CHEMBL2114067 Ki = 3.58 nM 8.45
CHEMBL2115126 Ki = 7.14 nM 8.15
CHEMBL71971 Ki = 7.3 nM 8.14
CHEMBL2114064 Ki = 7.67 nM 8.12
CHEMBL2115127 Ki = 10.8 nM 7.97
CHEMBL2114066 Ki = 17.3 nM 7.76