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Assay Detail

CHEMBL748901

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

Binding
Binding affinity against Muscarinic acetylcholine receptor M2 stably expressed in CHO-K1 cells.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M2 (CHEMBL211)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of piperidinyl piperidine analogues as potent and selective M2 muscarinic receptor antagonists.
Wang Y, Chackalamannil S, Hu Z, Clader JW, Greenlee W, Billard W, Binch H, Crosby G, Ruperto V, Duffy RA, McQuade R, Lachowicz JE.
Bioorg Med Chem Lett (2000) 10 : 2247 -2250
PubMed 11055330 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 9.28 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL308566 1 9.96
CHEMBL73893 1 9.80
CHEMBL71147 1 9.77
CHEMBL74117 1 9.59
CHEMBL421113 1 9.54
CHEMBL440491 1 9.52
CHEMBL72408 1 9.46
CHEMBL72494 1 9.44
CHEMBL72551 1 9.42
CHEMBL72363 1 9.42
CHEMBL72957 1 9.39
CHEMBL70860 1 9.35
CHEMBL73245 1 9.34
CHEMBL74352 1 9.23
CHEMBL307234 1 9.00
CHEMBL420008 1 8.94
CHEMBL422770 1 8.84
CHEMBL70848 1 8.66
CHEMBL72787 1 8.52
CHEMBL305607 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL308566 Ki = 0.11 nM 9.96
CHEMBL73893 Ki = 0.16 nM 9.80
CHEMBL71147 Ki = 0.17 nM 9.77
CHEMBL74117 Ki = 0.26 nM 9.59
CHEMBL421113 Ki = 0.29 nM 9.54
CHEMBL440491 Ki = 0.3 nM 9.52
CHEMBL72408 Ki = 0.35 nM 9.46
CHEMBL72494 Ki = 0.36 nM 9.44
CHEMBL72551 Ki = 0.38 nM 9.42
CHEMBL72363 Ki = 0.38 nM 9.42
CHEMBL72957 Ki = 0.41 nM 9.39
CHEMBL70860 Ki = 0.45 nM 9.35
CHEMBL73245 Ki = 0.46 nM 9.34
CHEMBL74352 Ki = 0.59 nM 9.23
CHEMBL307234 Ki = 0.99 nM 9.00
CHEMBL420008 Ki = 1.14 nM 8.94
CHEMBL422770 Ki = 1.45 nM 8.84
CHEMBL70848 Ki = 2.2 nM 8.66
CHEMBL72787 Ki = 2.99 nM 8.52
CHEMBL305607 Ki = 3.8 nM 8.42