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Assay Detail

CHEMBL5337118

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

Binding
Displacement of [3H]-LSD from human 5-HT6 receptor expressed in human HeLa cells assessed as inhibition constant incubated for 120 mins by Topcount scintillation counting analysis
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First-in-Class Selenium-Containing Potent Serotonin Receptor 5-HT<sub>6</sub> Agents with a Beneficial Neuroprotective Profile against Alzheimer's Disease.
Pyka P, Haberek W, Więcek M, Szymanska E, Ali W, Cios A, Jastrzębska-Więsek M, Satała G, Podlewska S, Di Giacomo S, Di Sotto A, Garbo S, Karcz T, Lambona C, Marocco F, Latacz G, Sudoł-Tałaj S, Mordyl B, Głuch-Lutwin M, Siwek A, Czarnota-Łydka K, Gogola D, Olejarz-Maciej A, Wilczyńska-Zawal N, Honkisz-Orzechowska E, Starek M, Dąbrowska M, Kucwaj-Brysz K, Fioravanti R, Nasim MJ, Hittinger M, Partyka A, Wesołowska A, Battistelli C, Zwergel C, Handzlik J.
J Med Chem (2024) 67 : 1580 -1610
PubMed 38190615 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.49 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL392760 1 8.66
CHEMBL571858 1 8.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL392760 Ki = 2.2 nM 8.66
CHEMBL571858 Ki = 4.8 nM 8.32