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Assay Detail

CHEMBL855414

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

Binding
Antagonist activity at human M3 receptor assessed as inhibition of carbachol binding
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Muscarinic acetylcholine receptor M3 (CHEMBL245)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of novel derivatives of the muscarinic agonist tetra(ethylene glycol)(3-methoxy-1,2,5-thiadiazol-4-yl) [3-(1-methyl-1,2,5,6-tetrahydropyrid-3-yl)-1,2,5-thiadiazol-4-yl] ether (CDD-0304): effects of structural modifications on the binding and activity at muscarinic receptor subtypes and chimeras.
Tejada FR, Nagy PI, Xu M, Wu C, Katz T, Dorsey J, Rieman M, Lawlor E, Warrier M, Messer WS.
J Med Chem (2006) 49 : 7518 -7531
PubMed 17149881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 3 6.93 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386983 1 7.20
CHEMBL216927 1 6.80
CHEMBL216928 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386983 Kd = 63.1 nM 7.20
CHEMBL216927 Kd = 158.49 nM 6.80
CHEMBL216928 Kd = 158.49 nM 6.80