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Assay Detail

CHEMBL3608118

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

Binding
Inhibition of BChE in equine serum using butyrylthiocholine iodide substrate by Ellman assay
25
Total Activities
25
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

Evaluation of Homobivalent Carbolines as Designed Multiple Ligands for the Treatment of Neurodegenerative Disorders.
Otto R, Penzis R, Gaube F, Adolph O, Föhr KJ, Warncke P, Robaa D, Appenroth D, Fleck C, Enzensperger C, Lehmann J, Winckler T.
J Med Chem (2015) 58 : 6710 -6715
PubMed 26278660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 7.51 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL95 TACRINE 4.0 1 8.36
CHEMBL1198953 1 8.28
CHEMBL3605357 1 8.19
CHEMBL3605355 1 7.88
CHEMBL3605356 1 7.88
CHEMBL3605361 1 7.80
CHEMBL3605354 1 7.79
CHEMBL1087459 1 7.63
CHEMBL3605360 1 7.50
CHEMBL3605363 1 7.49
CHEMBL3605367 1 7.42
CHEMBL3605368 1 7.37
CHEMBL3605370 1 7.36
CHEMBL3605359 1 7.33
CHEMBL3605362 1 7.32
CHEMBL3605353 1 7.30
CHEMBL3605369 1 7.28
CHEMBL3605365 1 7.25
CHEMBL3605366 1 7.10
CHEMBL3605364 1 7.07
CHEMBL3605358 1 7.03
CHEMBL1098471 1 6.54
CHEMBL807 MEMANTINE 4.0 1 -
CHEMBL8706 CLORGILINE 2.0 1 -
CHEMBL972 SELEGILINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL95 TACRINE IC50 = 4.4 nM 8.36
CHEMBL1198953 IC50 = 5.3 nM 8.28
CHEMBL3605357 IC50 = 6.5 nM 8.19
CHEMBL3605355 IC50 = 13.2 nM 7.88
CHEMBL3605356 IC50 = 13.1 nM 7.88
CHEMBL3605361 IC50 = 15.7 nM 7.80
CHEMBL3605354 IC50 = 16.2 nM 7.79
CHEMBL1087459 IC50 = 23.6 nM 7.63
CHEMBL3605360 IC50 = 31.4 nM 7.50
CHEMBL3605363 IC50 = 32.5 nM 7.49
CHEMBL3605367 IC50 = 37.9 nM 7.42
CHEMBL3605368 IC50 = 42.5 nM 7.37
CHEMBL3605370 IC50 = 43.5 nM 7.36
CHEMBL3605359 IC50 = 46.9 nM 7.33
CHEMBL3605362 IC50 = 47.8 nM 7.32
CHEMBL3605353 IC50 = 50.2 nM 7.30
CHEMBL3605369 IC50 = 52.4 nM 7.28
CHEMBL3605365 IC50 = 55.8 nM 7.25
CHEMBL3605366 IC50 = 80.1 nM 7.10
CHEMBL3605364 IC50 = 85.4 nM 7.07
CHEMBL3605358 IC50 = 93.5 nM 7.03
CHEMBL1098471 IC50 = 288.6 nM 6.54
CHEMBL807 MEMANTINE IC50 - -
CHEMBL8706 CLORGILINE IC50 - -
CHEMBL972 SELEGILINE IC50 - -