Assay Detail

CHEMBL4009112

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Binding

Antagonist activity at 5-HT6 receptor (unknown origin)

ChEMBL ↗

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Target

5-hydroxytryptamine receptor 6 (CHEMBL3371) ↗

Open DB target context

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5-hydroxytryptamine receptor 6 (CHEMBL3371) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target 5-hydroxytryptamine receptor 6

CHEMBL3371

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	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery and Development of 1-[(2-Bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole Dimesylate Monohydrate (SUVN-502): A Novel, Potent, Selective and Orally Active Serotonin 6 (5-HT6) Receptor Antagonist for Potential Treatment of Alzheimer's Disease.

Nirogi R, Shinde A, Kambhampati RS, Mohammed AR, Saraf SK, Badange RK, Bandyala TR, Bhatta V, Bojja K, Reballi V, Subramanian R, Benade V, Palacharla RC, Bhyrapuneni G, Jayarajan P, Goyal V, Jasti V.
J Med Chem (2017) 60 : 1843 -1859
PubMed 28212021 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	3	9.20	9.64

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1083390	INTEPIRDINE	3.0	1	9.64
CHEMBL3286580	IDALOPIRDINE	3.0	1	9.08
CHEMBL2103880	CERLAPIRDINE	2.0	1	8.89

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1083390	INTEPIRDINE	Ki	=	0.23	nM	9.64
CHEMBL3286580	IDALOPIRDINE	Ki	=	0.83	nM	9.08
CHEMBL2103880	CERLAPIRDINE	Ki	=	1.3	nM	8.89