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Assay Detail

CHEMBL3875273

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

Binding
Inhibition of equine serum BuChE preincubated for 5 mins followed by butyrylthiocholine iodide substrate addition measured after 5 mins by Ellman's method
20
Total Activities
20
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

Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT6 receptor antagonists. Design, synthesis and biological evaluation.
Więckowska A, Kołaczkowski M, Bucki A, Godyń J, Marcinkowska M, Więckowski K, Zaręba P, Siwek A, Kazek G, Głuch-Lutwin M, Mierzejewski P, Bienkowski P, Sienkiewicz-Jarosz H, Knez D, Wichur T, Gobec S, Malawska B.
Eur J Med Chem (2016) 124 : 63 -81
PubMed 27560283 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.45 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.70
CHEMBL3885186 1 8.09
CHEMBL3884690 1 8.00
CHEMBL3883432 1 7.91
CHEMBL3884618 1 7.85
CHEMBL3884988 1 7.78
CHEMBL3884858 1 7.67
CHEMBL3884154 1 6.22
CHEMBL3885452 1 5.88
CHEMBL3884704 1 5.78
CHEMBL502 DONEPEZIL 4.0 1 5.74
CHEMBL3883443 1 5.71
CHEMBL3884254 1 5.67
CHEMBL3884312 1 5.66
CHEMBL3884227 1 5.62
CHEMBL3884709 1 5.51
CHEMBL3884195 1 5.49
CHEMBL3885238 1 5.47
CHEMBL3883921 1 5.21
CHEMBL3883620 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 2.0 nM 8.70
CHEMBL3885186 IC50 = 8.2 nM 8.09
CHEMBL3884690 IC50 = 10.0 nM 8.00
CHEMBL3883432 IC50 = 12.4 nM 7.91
CHEMBL3884618 IC50 = 14.2 nM 7.85
CHEMBL3884988 IC50 = 16.8 nM 7.78
CHEMBL3884858 IC50 = 21.3 nM 7.67
CHEMBL3884154 IC50 = 607.9 nM 6.22
CHEMBL3885452 IC50 = 1307.0 nM 5.88
CHEMBL3884704 IC50 = 1673.0 nM 5.78
CHEMBL502 DONEPEZIL IC50 = 1830.0 nM 5.74
CHEMBL3883443 IC50 = 1951.0 nM 5.71
CHEMBL3884254 IC50 = 2163.0 nM 5.67
CHEMBL3884312 IC50 = 2211.0 nM 5.66
CHEMBL3884227 IC50 = 2384.0 nM 5.62
CHEMBL3884709 IC50 = 3071.0 nM 5.51
CHEMBL3884195 IC50 = 3217.0 nM 5.49
CHEMBL3885238 IC50 = 3394.0 nM 5.47
CHEMBL3883921 IC50 = 6221.0 nM 5.21
CHEMBL3883620 IC50 = 10550.0 nM 4.98