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Assay Detail

CHEMBL3364794

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

Binding
Displacement of [3H]LSD from human 5-HT7 expressed in HEK-293 cells after 120 mins by scintillation spectrometry
9
Total Activities
9
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 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
Ki 9 7.85 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3321794 1 9.15
CHEMBL3321798 1 8.57
CHEMBL445334 1 8.15
CHEMBL3321778 1 7.62
CHEMBL3321777 1 7.55
CHEMBL3321795 1 7.54
CHEMBL3321793 1 7.44
CHEMBL3321796 1 7.39
CHEMBL3321797 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3321794 Ki = 0.7 nM 9.15
CHEMBL3321798 Ki = 2.7 nM 8.57
CHEMBL445334 Ki = 7.0 nM 8.15
CHEMBL3321778 Ki = 24.0 nM 7.62
CHEMBL3321777 Ki = 28.0 nM 7.55
CHEMBL3321795 Ki = 29.0 nM 7.54
CHEMBL3321793 Ki = 36.0 nM 7.44
CHEMBL3321796 Ki = 41.0 nM 7.39
CHEMBL3321797 Ki = 62.0 nM 7.21