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Assay Detail

CHEMBL1033535

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

Binding
Inhibition of equine serum BuChE by Ellman's method
16
Total Activities
16
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, biological evaluation and molecular modeling of oxoisoaporphine and oxoaporphine derivatives as new dual inhibitors of acetylcholinesterase/butyrylcholinesterase.
Tang H, Wei YB, Zhang C, Ning FX, Qiao W, Huang SL, Ma L, Huang ZS, Gu LQ.
Eur J Med Chem (2009) 44 : 2523 -2532
PubMed 19243862 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.16 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL550075 1 6.22
CHEMBL559266 1 5.57
CHEMBL395926 1 5.55
CHEMBL559502 1 5.40
CHEMBL549666 1 5.32
CHEMBL551226 1 5.30
CHEMBL556249 1 5.29
CHEMBL563713 1 5.21
CHEMBL541019 1 5.17
CHEMBL550076 1 5.09
CHEMBL549935 1 5.01
CHEMBL559822 1 4.93
CHEMBL659 GALANTAMINE 4.0 1 4.84
CHEMBL549936 1 4.27
CHEMBL551430 1 4.16
CHEMBL246681 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL550075 IC50 = 600.0 nM 6.22
CHEMBL559266 IC50 = 2710.0 nM 5.57
CHEMBL395926 IC50 = 2820.0 nM 5.55
CHEMBL559502 IC50 = 4010.0 nM 5.40
CHEMBL549666 IC50 = 4750.0 nM 5.32
CHEMBL551226 IC50 = 5030.0 nM 5.30
CHEMBL556249 IC50 = 5190.0 nM 5.29
CHEMBL563713 IC50 = 6240.0 nM 5.21
CHEMBL541019 IC50 = 6760.0 nM 5.17
CHEMBL550076 IC50 = 8140.0 nM 5.09
CHEMBL549935 IC50 = 9720.0 nM 5.01
CHEMBL559822 IC50 = 11690.0 nM 4.93
CHEMBL659 GALANTAMINE IC50 = 14400.0 nM 4.84
CHEMBL549936 IC50 = 53250.0 nM 4.27
CHEMBL551430 IC50 = 68730.0 nM 4.16
CHEMBL246681 IC50 > 100000.0 nM -