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Assay Detail

CHEMBL3364796

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Functional
Agonist activity at human 5-HT7 expressed in HEK-293 cells assessed as increase in cAMP level after 45 mins by HTRF assay
3
Total Activities
3
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 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The extracellular entrance provides selectivity to serotonin 5-HT7 receptor antagonists with antidepressant-like behavior in vivo.
Medina RA, Vázquez-Villa H, Gómez-Tamayo JC, Benhamú B, Martín-Fontecha M, de la Fuente T, Caltabiano G, Hedlund PB, Pardo L, López-Rodríguez ML.
J Med Chem (2014) 57 : 6879 -6884
PubMed 25073094 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.21 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39 SEROTONIN 3.0 1 7.77
CHEMBL3321798 1 7.22
CHEMBL3321794 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39 SEROTONIN EC50 = 17.0 nM 7.77
CHEMBL3321798 EC50 = 60.0 nM 7.22
CHEMBL3321794 EC50 = 230.0 nM 6.64