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Assay Detail

CHEMBL744775

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

Binding
Binding affinity against Muscarinic acetylcholine receptor M1 expressed in CHO-K1 cells
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Muscarinic acetylcholine receptor M1 (CHEMBL216)
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 5 7.95 8.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71147 1 8.55
CHEMBL308566 1 8.19
CHEMBL420008 1 8.04
CHEMBL421113 1 7.59
CHEMBL72551 1 7.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71147 Ki = 2.8 nM 8.55
CHEMBL308566 Ki = 6.5 nM 8.19
CHEMBL420008 Ki = 9.1 nM 8.04
CHEMBL421113 Ki = 25.7 nM 7.59
CHEMBL72551 Ki = 42.0 nM 7.38