Assay Detail

CHEMBL4426397

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Binding

Displacement of [3H]Lu AE60157 from rat brain 5-HT6 receptor

ChEMBL ↗

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Target

5-hydroxytryptamine receptor 6 (CHEMBL3372) ↗

Open DB target context

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5-hydroxytryptamine receptor 6 (CHEMBL3372) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target 5-hydroxytryptamine receptor 6

CHEMBL3372

Anchored from Assay target.

Protein identity 5-hydroxytryptamine receptor 6

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	Rattus norvegicus
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3372) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

N1-Azinylsulfonyl-1H-indoles: 5-HT6 Receptor Antagonists with Procognitive and Antidepressant-Like Properties.

Zajdel P, Marciniec K, Satała G, Canale V, Kos T, Partyka A, Jastrzębska-Więsek M, Wesołowska A, Basińska-Ziobroń A, Wójcikowski J, Daniel WA, Bojarski AJ, Popik P, Popik P.
ACS Med Chem Lett (2016) 7 : 618 -622
PubMed 27326337 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	2	9.36	9.63

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1083390	INTEPIRDINE	3.0	1	9.63
CHEMBL3286580	IDALOPIRDINE	3.0	1	9.08

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1083390	INTEPIRDINE	Ki	=	0.234	nM	9.63
CHEMBL3286580	IDALOPIRDINE	Ki	=	0.83	nM	9.08