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Assay Detail

CHEMBL4409660

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

Binding
Displacement of [3H]-8-OH-DPAT from 5HT1A receptor (unknown origin) expressed in HEK293 cells membranes incubated for 60 mins by scintillation counting method
8
Total Activities
8
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 effect of novel aralkyl piperazine and piperidine derivatives targeting SSRI/5-HT1A/5-HT7.
Gu ZS, Wang WT, Qian H, Zhou AN, Sun HB, Zhang QW, Li JQ.
Bioorg Med Chem Lett (2019) 29 : 126703 -126703
PubMed 31627993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.36 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.70
CHEMBL4574299 1 8.80
CHEMBL4476294 1 8.80
CHEMBL4544153 1 8.20
CHEMBL4471208 1 8.08
CHEMBL2104993 VORTIOXETINE 4.0 1 8.02
CHEMBL4543789 1 7.82
CHEMBL4459410 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE Ki = 0.2 nM 9.70
CHEMBL4574299 Ki = 1.6 nM 8.80
CHEMBL4476294 Ki = 1.6 nM 8.80
CHEMBL4544153 Ki = 6.3 nM 8.20
CHEMBL4471208 Ki = 8.4 nM 8.08
CHEMBL2104993 VORTIOXETINE Ki = 9.5 nM 8.02
CHEMBL4543789 Ki = 15.0 nM 7.82
CHEMBL4459410 Ki = 38.0 nM 7.42