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Assay Detail

CHEMBL2185685

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

Binding
Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 4 (CHEMBL1875)
Type SINGLE PROTEIN
Organism Homo sapiens

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 12 9.02 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2152922 PF-04995274 1.0 1 9.82
CHEMBL2179584 1 9.57
CHEMBL2179587 1 9.54
CHEMBL2179589 1 9.44
CHEMBL2179580 1 9.30
CHEMBL2179585 1 9.13
CHEMBL2179586 1 9.01
CHEMBL2179583 1 8.77
CHEMBL2179582 PF-03382792 1.0 1 8.57
CHEMBL2179590 1 8.44
CHEMBL2179581 1 8.35
CHEMBL2179588 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2152922 PF-04995274 Ki = 0.15 nM 9.82
CHEMBL2179584 Ki = 0.27 nM 9.57
CHEMBL2179587 Ki = 0.29 nM 9.54
CHEMBL2179589 Ki = 0.36 nM 9.44
CHEMBL2179580 Ki = 0.5 nM 9.30
CHEMBL2179585 Ki = 0.74 nM 9.13
CHEMBL2179586 Ki = 0.97 nM 9.01
CHEMBL2179583 Ki = 1.7 nM 8.77
CHEMBL2179582 PF-03382792 Ki = 2.7 nM 8.57
CHEMBL2179590 Ki = 3.6 nM 8.44
CHEMBL2179581 Ki = 4.5 nM 8.35
CHEMBL2179588 Ki = 5.2 nM 8.28