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Assay Detail

CHEMBL745478

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

Binding
Binding affinity against Muscarinic acetylcholine receptor M2 by displacement of [3H]QNB in rat myocardium
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Myocardium
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL309)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
Rzeszotarski WJ, McPherson DW, Ferkany JW, Kinnier WJ, Noronha-Blob L, Kirkien-Rzeszotarski A.
J Med Chem (1988) 31 : 1463 -1466
PubMed 3385735 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.75 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL558910 1 9.64
CHEMBL549577 1 9.41
CHEMBL517712 ATROPINE 4.0 1 9.15
CHEMBL1788199 1 8.23
CHEMBL2115342 1 8.16
CHEMBL2115341 1 7.43
CHEMBL1788286 1 7.13
CHEMBL9967 PIRENZEPINE 2.0 1 6.42
CHEMBL2114396 1 6.03
CHEMBL2114395 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL558910 Ki = 0.23 nM 9.64
CHEMBL549577 Ki = 0.39 nM 9.41
CHEMBL517712 ATROPINE Ki = 0.7 nM 9.15
CHEMBL1788199 Ki = 5.83 nM 8.23
CHEMBL2115342 Ki = 6.9 nM 8.16
CHEMBL2115341 Ki = 37.0 nM 7.43
CHEMBL1788286 Ki = 74.0 nM 7.13
CHEMBL9967 PIRENZEPINE Ki = 377.0 nM 6.42
CHEMBL2114396 Ki = 934.0 nM 6.03
CHEMBL2114395 Ki = 1372.0 nM 5.86