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Assay Detail

CHEMBL4371162

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

Binding
inhibition of rat cerebral 5HT transporter assessed as reduction in [3H]5HT reuptake after 4 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design.
Meanwell NA.
J Med Chem (2018) 61 : 5822 -5880
PubMed 29400967 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.89 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360390 1 9.52
CHEMBL189709 1 9.40
CHEMBL439849 VILAZODONE 4.0 1 9.30
CHEMBL188799 1 9.22
CHEMBL186655 1 9.00
CHEMBL188798 1 9.00
CHEMBL364610 1 8.00
CHEMBL360407 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360390 IC50 = 0.3 nM 9.52
CHEMBL189709 IC50 = 0.4 nM 9.40
CHEMBL439849 VILAZODONE IC50 = 0.5 nM 9.30
CHEMBL188799 IC50 = 0.6 nM 9.22
CHEMBL186655 IC50 = 1.0 nM 9.00
CHEMBL188798 IC50 = 1.0 nM 9.00
CHEMBL364610 IC50 = 10.0 nM 8.00
CHEMBL360407 IC50 = 20.0 nM 7.70