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Assay Detail

CHEMBL5611214

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

Binding
Displacement of [3H]-LSD from human 5-HT6 receptor extracted from CHO-K1 cell membrane assessed as inhibition constant incubated for 1 hr by Microbeta plate reader analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Contilisant+Tubastatin A Hybrids: Polyfunctionalized Indole Derivatives as New HDAC Inhibitor-Based Multitarget Small Molecules with <i>In Vitro</i> and <i>In Vivo</i> Activity in Neurodegenerative Diseases.
Toledano-Pinedo M, Porro-Pérez A, Schäker-Hübner L, Romero F, Dong M, Samadi A, Almendros P, Iriepa I, Bautista-Aguilera ÒM, Rodríguez-Fernández MM, Solana-Manrique C, Sanchis I, Mora-Morell A, Rodrìguez AC, Sànchez-Pérez AM, Knez D, Gobec S, Bellver-Sanchis A, Pérez B, Dobrydnev AV, Artetxe-Zurutuza A, Matheu A, Siwek A, Wolak M, Satała G, Bojarski AJ, Doroz-Płonka A, Handzlik J, Godyń J, Więckowska A, Paricio N, Griñán-Ferré C, Hansen FK, Marco-Contelles J.
J Med Chem (2024) 67 : 16533 -16555
PubMed 39256214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.16 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5612392 1 5.47
CHEMBL5612956 1 5.37
CHEMBL5614364 1 5.24
CHEMBL5612289 1 5.20
CHEMBL5613964 1 4.51
CHEMBL268229 1 -
CHEMBL95 TACRINE 4.0 1 -
CHEMBL396778 SAFINAMIDE 4.0 1 -
CHEMBL887 RASAGILINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5612392 Ki = 3392.0 nM 5.47
CHEMBL5612956 Ki = 4307.0 nM 5.37
CHEMBL5614364 Ki = 5820.0 nM 5.24
CHEMBL5612289 Ki = 6376.0 nM 5.20
CHEMBL5613964 Ki = 30650.0 nM 4.51
CHEMBL268229 Ki - -
CHEMBL95 TACRINE Ki - -
CHEMBL396778 SAFINAMIDE Ki - -
CHEMBL887 RASAGILINE Ki - -