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Assay Detail

CHEMBL5611212

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

Binding
Inhibition of equine serum BuChE using butyrylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by DNTB reagent based Ellman's method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Equus caballus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL5763)
Type SINGLE PROTEIN
Organism Equus caballus

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
IC50 6 6.50 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.52
CHEMBL5612956 1 5.93
CHEMBL5613964 1 5.05
CHEMBL268229 1 -
CHEMBL396778 SAFINAMIDE 4.0 1 -
CHEMBL887 RASAGILINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 3.0 nM 8.52
CHEMBL5612956 IC50 = 1180.0 nM 5.93
CHEMBL5613964 IC50 = 8806.0 nM 5.05
CHEMBL268229 IC50 - -
CHEMBL396778 SAFINAMIDE IC50 - -
CHEMBL887 RASAGILINE IC50 - -