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Assay Detail

CHEMBL4182005

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 measured after 60 mins by scintillation counting method
4
Total Activities
4
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 activity of a series of arylalkanol and aralkyl piperazine derivatives targeting SSRI/5-HT1A/5-HT7.
Gu ZS, Xiao Y, Zhang QW, Li JQ.
Bioorg Med Chem Lett (2017) 27 : 5420 -5423
PubMed 29138029 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.48 9.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209430 1 9.08
CHEMBL4203932 1 8.62
CHEMBL4215605 1 8.20
CHEMBL2104993 VORTIOXETINE 4.0 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209430 Ki = 0.84 nM 9.08
CHEMBL4203932 Ki = 2.4 nM 8.62
CHEMBL4215605 Ki = 6.3 nM 8.20
CHEMBL2104993 VORTIOXETINE Ki = 9.5 nM 8.02