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Assay Detail

CHEMBL2185665

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

Binding
Displacement of [3H]GR113808 from 5HT4 receptor in monkey striatal membrane after 30 mins by liquid scintillation counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Macaca mulatta
Tissue Striatum
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of multiple 5-HT₄ partial agonist clinical candidates for the treatment of Alzheimer's disease.
Brodney MA, Johnson DE, Sawant-Basak A, Coffman KJ, Drummond EM, Hudson EL, Fisher KE, Noguchi H, Waizumi N, McDowell LL, Papanikolaou A, Pettersen BA, Schmidt AW, Tseng E, Stutzman-Engwall K, Rubitski DM, Vanase-Frawley MA, Grimwood S.
J Med Chem (2012) 55 : 9240 -9254
PubMed 22974325 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.78 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152922 PF-04995274 1.0 1 9.57
CHEMBL2179583 1 8.72
CHEMBL2179582 PF-03382792 1.0 1 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152922 PF-04995274 Ki = 0.27 nM 9.57
CHEMBL2179583 Ki = 1.9 nM 8.72
CHEMBL2179582 PF-03382792 Ki = 8.9 nM 8.05