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Assay Detail

CHEMBL748899

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

Binding
Binding affinity towards the cloned human Muscarinic acetylcholine receptor M2
21
Total Activities
17
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

Diphenyl sulfoxides as selective antagonists of the muscarinic M2 receptor.
Kozlowski JA, Lowe DB, Guzik HS, Zhou G, Ruperto VB, Duffy RA, McQuade R, Crosby G, Taylor LA, Billard W, Binch H, Lachowicz JE.
Bioorg Med Chem Lett (2000) 10 : 2255 -2257
PubMed 11055332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.00 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL312085 1 9.70
CHEMBL75448 1 9.22
CHEMBL310912 1 9.22
CHEMBL72455 1 9.10
CHEMBL307810 1 9.00
CHEMBL2111540 5 8.57
CHEMBL70464 1 8.30
CHEMBL73341 1 8.10
CHEMBL421304 1 7.77
CHEMBL70531 1 7.58
CHEMBL73661 1 7.48
CHEMBL73410 1 7.47
CHEMBL72956 1 7.44
CHEMBL71088 1 7.43
CHEMBL431787 1 7.40
CHEMBL73145 1 6.87
CHEMBL303443 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL312085 Ki = 0.2 nM 9.70
CHEMBL75448 Ki = 0.6 nM 9.22
CHEMBL310912 Ki = 0.6 nM 9.22
CHEMBL72455 Ki = 0.8 nM 9.10
CHEMBL307810 Ki = 1.0 nM 9.00
CHEMBL2111540 Ki = 2.7 nM 8.57
CHEMBL2111540 Ki = 3.8 nM 8.42
CHEMBL70464 Ki = 5.0 nM 8.30
CHEMBL73341 Ki = 8.0 nM 8.10
CHEMBL2111540 Ki = 9.0 nM 8.05
CHEMBL421304 Ki = 17.0 nM 7.77
CHEMBL2111540 Ki = 17.0 nM 7.77
CHEMBL2111540 Ki = 20.0 nM 7.70
CHEMBL70531 Ki = 26.0 nM 7.58
CHEMBL73661 Ki = 33.0 nM 7.48
CHEMBL73410 Ki = 34.0 nM 7.47
CHEMBL72956 Ki = 36.0 nM 7.44
CHEMBL71088 Ki = 37.0 nM 7.43
CHEMBL431787 Ki = 40.0 nM 7.40
CHEMBL73145 Ki = 135.0 nM 6.87
CHEMBL303443 Ki = 4600.0 nM 5.34