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Assay Detail

CHEMBL5337119

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

Binding
Binding affinity to 5-HT6 receptor (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
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

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 5 8.99 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1083390 INTEPIRDINE 3.0 1 9.77
CHEMBL362628 1 9.24
CHEMBL1210710 SB-399885 1 9.10
CHEMBL431298 1 8.90
CHEMBL5219240 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1083390 INTEPIRDINE Ki = 0.17 nM 9.77
CHEMBL362628 Ki = 0.58 nM 9.24
CHEMBL1210710 SB-399885 Ki = 0.79 nM 9.10
CHEMBL431298 Ki = 1.26 nM 8.90
CHEMBL5219240 Ki = 11.0 nM 7.96