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Assay Detail

CHEMBL4390414

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

Binding
Displacement of [3H]5-CT from human 5HT7 receptor expressed in in COS7 cells incubated for 30 mins by liquid scintillation counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants.
Zaręba P, Jaśkowska J, Czekaj I, Satała G.
Bioorg Med Chem (2019) 27 : 3396 -3407
PubMed 31253535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.76 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL428494 1 8.70
CHEMBL12702 1 8.30
CHEMBL307101 1 7.92
CHEMBL71390 1 7.70
CHEMBL69388 1 7.13
CHEMBL302723 1 6.83

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL428494 Ki = 2.0 nM 8.70
CHEMBL12702 Ki = 5.0 nM 8.30
CHEMBL307101 Ki = 12.0 nM 7.92
CHEMBL71390 Ki = 20.0 nM 7.70
CHEMBL69388 Ki = 74.0 nM 7.13
CHEMBL302723 Ki = 147.0 nM 6.83