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Assay Detail

CHEMBL2166103

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

Functional
Antagonist activity at human 5HT7A receptor expressed in human HeLa cells assessed as inhibition of 5-HT-induced cAMP accumulation by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Investigations on the 1-(2-biphenyl)piperazine motif: identification of new potent and selective ligands for the serotonin(7) (5-HT(7)) receptor with agonist or antagonist action in vitro or ex vivo.
Lacivita E, Patarnello D, Stroth N, Caroli A, Niso M, Contino M, De Giorgio P, Di Pilato P, Colabufo NA, Berardi F, Perrone R, Svenningsson P, Hedlund PB, Leopoldo M.
J Med Chem (2012) 55 : 6375 -6380
PubMed 22738316 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.32 6.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164336 1 6.36
CHEMBL494675 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164336 IC50 = 438.0 nM 6.36
CHEMBL494675 IC50 = 531.0 nM 6.28