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Assay Detail

CHEMBL855418

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

Binding
Inhibition of [3H](R)-QNB binding to human M1/M5(o2o3) chimeric receptor expressed in A9 L cells
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type A9L
Confidence 7 — Homologous single protein target
Curated By Expert

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
Ki 4 5.90 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL335542 1 7.00
CHEMBL216927 1 6.50
CHEMBL21536 XANOMELINE 4.0 1 5.90
CHEMBL14 CARBACHOL 4.0 1 4.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL335542 Ki = 100.0 nM 7.00
CHEMBL216927 Ki = 316.23 nM 6.50
CHEMBL21536 XANOMELINE Ki = 1258.93 nM 5.90
CHEMBL14 CARBACHOL Ki = 63095.73 nM 4.20