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Assay Detail

CHEMBL747482

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

Binding
Binding affinity against human cloned Muscarinic acetylcholine receptor M2.
17
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

Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.
Kozlowski JA, Zhou G, Tagat JR, Lin SI, McCombie SW, Ruperto VB, Duffy RA, McQuade RA, Crosby G, Taylor LA, Billard W, Binch H, Lachowicz JE.
Bioorg Med Chem Lett (2002) 12 : 791 -794
PubMed 11859004 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 9.38 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL349497 1 10.52
CHEMBL164705 1 10.52
CHEMBL350956 1 10.40
CHEMBL164762 1 9.85
CHEMBL424530 1 9.82
CHEMBL435849 1 9.70
CHEMBL165375 1 9.70
CHEMBL165439 1 9.52
CHEMBL163777 1 9.52
CHEMBL310912 1 9.22
CHEMBL163714 1 9.15
CHEMBL163658 1 9.10
CHEMBL349720 1 9.05
CHEMBL165337 1 8.89
CHEMBL163887 1 8.60
CHEMBL164397 1 8.05
CHEMBL352607 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL349497 Ki = 0.03 nM 10.52
CHEMBL164705 Ki = 0.03 nM 10.52
CHEMBL350956 Ki = 0.04 nM 10.40
CHEMBL164762 Ki = 0.14 nM 9.85
CHEMBL424530 Ki = 0.15 nM 9.82
CHEMBL435849 Ki = 0.2 nM 9.70
CHEMBL165375 Ki = 0.2 nM 9.70
CHEMBL165439 Ki = 0.3 nM 9.52
CHEMBL163777 Ki = 0.3 nM 9.52
CHEMBL310912 Ki = 0.6 nM 9.22
CHEMBL163714 Ki = 0.7 nM 9.15
CHEMBL163658 Ki = 0.8 nM 9.10
CHEMBL349720 Ki = 0.9 nM 9.05
CHEMBL165337 Ki = 1.3 nM 8.89
CHEMBL163887 Ki = 2.5 nM 8.60
CHEMBL164397 Ki = 9.0 nM 8.05
CHEMBL352607 Ki = 16.0 nM 7.80