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Assay Detail

CHEMBL4479286

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

Binding
Inhibition of equine serum BuChE preincubated for 6 mins followed by addition of S-butyrylthiocholine iodide by Ellman's method
30
Total Activities
30
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

Synthesis and evaluation of novel 1,2,3-triazole-based acetylcholinesterase inhibitors with neuroprotective activity.
Li JC, Zhang J, Rodrigues MC, Ding DJ, Longo JP, Azevedo RB, Muehlmann LA, Jiang CS.
Bioorg Med Chem Lett (2016) 26 : 3881 -3885
PubMed 27426301 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 4.24 4.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL659 GALANTAMINE 4.0 1 4.79
CHEMBL4541730 1 4.46
CHEMBL4536296 1 4.46
CHEMBL4531267 1 4.44
CHEMBL4524162 1 4.39
CHEMBL4578074 1 4.36
CHEMBL4584351 1 4.34
CHEMBL4522818 1 4.34
CHEMBL4581887 1 4.34
CHEMBL4571408 1 4.33
CHEMBL4545234 1 4.29
CHEMBL4547644 1 4.25
CHEMBL4521556 1 4.22
CHEMBL4516485 1 4.22
CHEMBL4561751 1 4.22
CHEMBL4572737 1 4.21
CHEMBL4539017 1 4.17
CHEMBL4534953 1 4.17
CHEMBL4525497 1 4.16
CHEMBL4576458 1 4.15
CHEMBL4549496 1 4.14
CHEMBL4530986 1 4.11
CHEMBL4515828 1 4.08
CHEMBL4513605 1 4.05
CHEMBL4589486 1 4.04
CHEMBL4581664 1 4.04
CHEMBL4551175 1 4.03
CHEMBL4525580 1 4.02
CHEMBL4540499 1 -
CHEMBL4513836 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL659 GALANTAMINE IC50 = 16320.0 nM 4.79
CHEMBL4541730 IC50 = 34450.0 nM 4.46
CHEMBL4536296 IC50 = 34780.0 nM 4.46
CHEMBL4531267 IC50 = 36250.0 nM 4.44
CHEMBL4524162 IC50 = 40340.0 nM 4.39
CHEMBL4578074 IC50 = 43660.0 nM 4.36
CHEMBL4584351 IC50 = 45150.0 nM 4.34
CHEMBL4522818 IC50 = 45520.0 nM 4.34
CHEMBL4581887 IC50 = 45560.0 nM 4.34
CHEMBL4571408 IC50 = 47230.0 nM 4.33
CHEMBL4545234 IC50 = 50760.0 nM 4.29
CHEMBL4547644 IC50 = 56230.0 nM 4.25
CHEMBL4521556 IC50 = 60230.0 nM 4.22
CHEMBL4516485 IC50 = 60780.0 nM 4.22
CHEMBL4561751 IC50 = 60460.0 nM 4.22
CHEMBL4572737 IC50 = 60960.0 nM 4.21
CHEMBL4539017 IC50 = 67770.0 nM 4.17
CHEMBL4534953 IC50 = 68120.0 nM 4.17
CHEMBL4525497 IC50 = 68950.0 nM 4.16
CHEMBL4576458 IC50 = 70760.0 nM 4.15
CHEMBL4549496 IC50 = 72850.0 nM 4.14
CHEMBL4530986 IC50 = 78560.0 nM 4.11
CHEMBL4515828 IC50 = 83120.0 nM 4.08
CHEMBL4513605 IC50 = 89560.0 nM 4.05
CHEMBL4589486 IC50 = 90860.0 nM 4.04
CHEMBL4581664 IC50 = 90760.0 nM 4.04
CHEMBL4551175 IC50 = 92830.0 nM 4.03
CHEMBL4525580 IC50 = 95450.0 nM 4.02
CHEMBL4540499 IC50 - -
CHEMBL4513836 IC50 - -