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Assay Detail

CHEMBL4254545

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

Binding
Displacement of [3H]8-OH-DPAT from recombinant human 5-HT1A receptor expressed in HEK293 cell membranes after 60 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 HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
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 7.95 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4291322 1 9.28
CHEMBL4285796 1 8.25
CHEMBL4278933 1 8.09
CHEMBL2104993 VORTIOXETINE 4.0 1 8.02
CHEMBL4286174 1 7.89
CHEMBL4288120 1 7.82
CHEMBL4277476 1 7.75
CHEMBL4294077 1 7.60
CHEMBL4289783 1 7.55
CHEMBL4289605 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4291322 Ki = 0.53 nM 9.28
CHEMBL4285796 Ki = 5.6 nM 8.25
CHEMBL4278933 Ki = 8.1 nM 8.09
CHEMBL2104993 VORTIOXETINE Ki = 9.5 nM 8.02
CHEMBL4286174 Ki = 13.0 nM 7.89
CHEMBL4288120 Ki = 15.0 nM 7.82
CHEMBL4277476 Ki = 18.0 nM 7.75
CHEMBL4294077 Ki = 25.0 nM 7.60
CHEMBL4289783 Ki = 28.0 nM 7.55
CHEMBL4289605 Ki = 62.0 nM 7.21