Assay Detail

CHEMBL2394910

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Binding

Binding affinity to human 5-HT transporter by radioligand displacement assay

ChEMBL ↗

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Target

Sodium-dependent serotonin transporter (CHEMBL228) ↗

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Sodium-dependent serotonin transporter (CHEMBL228) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Sodium-dependent serotonin transporter

CHEMBL228

Anchored from Assay target.

Protein identity Sodium-dependent serotonin transporter

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL228) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.

Cappelli A, Manini M, Valenti S, Castriconi F, Giuliani G, Anzini M, Brogi S, Butini S, Gemma S, Campiani G, Giorgi G, Mennuni L, Lanza M, Giordani A, Caselli G, Letari O, Makovec F.
Eur J Med Chem (2013) 63 : 85 -94
PubMed 23466604 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	9.28	9.28
IC50	1	8.96	8.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL11	IMIPRAMINE	4.0	2	9.28

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL11	IMIPRAMINE	Ki	=	0.52	nM	9.28
CHEMBL11	IMIPRAMINE	IC50	=	1.1	nM	8.96