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Assay Detail

CHEMBL4254547

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

Binding
Displacement of [3H]LSD from recombinant human 5-HT7 receptor expressed in CHO cell membranes after 120 mins by TopCount scintillation counting method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and antidepressant-like activity of novel aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.
Gu ZS, Zhou AN, Xiao Y, Zhang QW, Li JQ.
Eur J Med Chem (2018) 144 : 701 -715
PubMed 29291438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.71 9.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4291322 1 9.59
CHEMBL4277476 1 9.26
CHEMBL4285796 1 9.10
CHEMBL4286174 1 8.96
CHEMBL4278933 1 8.96
CHEMBL4294077 1 8.64
CHEMBL4288120 1 8.59
CHEMBL4289783 1 8.48
CHEMBL4289605 1 7.92
CHEMBL2104993 VORTIOXETINE 4.0 1 7.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4291322 Ki = 0.26 nM 9.59
CHEMBL4277476 Ki = 0.55 nM 9.26
CHEMBL4285796 Ki = 0.79 nM 9.10
CHEMBL4286174 Ki = 1.1 nM 8.96
CHEMBL4278933 Ki = 1.1 nM 8.96
CHEMBL4294077 Ki = 2.3 nM 8.64
CHEMBL4288120 Ki = 2.6 nM 8.59
CHEMBL4289783 Ki = 3.3 nM 8.48
CHEMBL4289605 Ki = 12.0 nM 7.92
CHEMBL2104993 VORTIOXETINE Ki = 26.0 nM 7.58