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Assay Detail

CHEMBL4409664

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

Binding
Inhibition of rat synaptosomes 5HT transporter assessed as reduction in [3H]serotonin reuptake incubated for 15 mins by scintillation counting method
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Synaptosomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
IC50 13 8.41 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439849 VILAZODONE 4.0 1 9.30
CHEMBL4457939 1 9.04
CHEMBL4476294 1 8.96
CHEMBL4544153 1 8.89
CHEMBL4438415 1 8.57
CHEMBL2104993 VORTIOXETINE 4.0 1 8.54
CHEMBL4543789 1 8.52
CHEMBL4471208 1 8.40
CHEMBL4441488 1 8.15
CHEMBL4434876 1 7.85
CHEMBL4539622 1 7.85
CHEMBL4459410 1 7.68
CHEMBL4574299 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439849 VILAZODONE IC50 = 0.5 nM 9.30
CHEMBL4457939 IC50 = 0.92 nM 9.04
CHEMBL4476294 IC50 = 1.1 nM 8.96
CHEMBL4544153 IC50 = 1.3 nM 8.89
CHEMBL4438415 IC50 = 2.7 nM 8.57
CHEMBL2104993 VORTIOXETINE IC50 = 2.9 nM 8.54
CHEMBL4543789 IC50 = 3.0 nM 8.52
CHEMBL4471208 IC50 = 4.0 nM 8.40
CHEMBL4441488 IC50 = 7.08 nM 8.15
CHEMBL4434876 IC50 = 14.0 nM 7.85
CHEMBL4539622 IC50 = 14.0 nM 7.85
CHEMBL4459410 IC50 = 21.0 nM 7.68
CHEMBL4574299 IC50 = 23.0 nM 7.64