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Assay Detail

CHEMBL2185684

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Functional
Agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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
EC50 11 8.92 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2179580 1 9.40
CHEMBL2179584 1 9.10
CHEMBL2179583 1 9.05
CHEMBL2179582 PF-03382792 1.0 1 9.05
CHEMBL2179589 1 9.01
CHEMBL2179586 1 8.96
CHEMBL2179587 1 8.92
CHEMBL2179585 1 8.92
CHEMBL2179590 1 8.77
CHEMBL2179581 1 8.72
CHEMBL2179588 1 8.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2179580 EC50 = 0.4 nM 9.40
CHEMBL2179584 EC50 = 0.8 nM 9.10
CHEMBL2179583 EC50 = 0.9 nM 9.05
CHEMBL2179582 PF-03382792 EC50 = 0.9 nM 9.05
CHEMBL2179589 EC50 = 0.98 nM 9.01
CHEMBL2179586 EC50 = 1.1 nM 8.96
CHEMBL2179587 EC50 = 1.2 nM 8.92
CHEMBL2179585 EC50 = 1.2 nM 8.92
CHEMBL2179590 EC50 = 1.7 nM 8.77
CHEMBL2179581 EC50 = 1.9 nM 8.72
CHEMBL2179588 EC50 = 6.3 nM 8.20