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Assay Detail

CHEMBL1100207

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

Binding
Inhibition of rat plasma BChE by Ellman's method
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Plasma
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Butyrylcholinesterase (CHEMBL3403)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of physostigmine analogues and evaluation of their anticholinesterase activities.
Zhan ZJ, Bian HL, Wang JW, Shan WG.
Bioorg Med Chem Lett (2010) 20 : 1532 -1534
PubMed 20144867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.06 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL74950 1 8.24
CHEMBL94 PHYSOSTIGMINE 3.0 1 8.12
CHEMBL1082185 1 8.07
CHEMBL1080691 1 7.85
CHEMBL1076615 1 7.83
CHEMBL1080317 1 7.40
CHEMBL1080937 1 7.21
CHEMBL1081473 1 7.05
CHEMBL74926 PHENSERINE 1 6.98
CHEMBL1081300 1 6.98
CHEMBL1080319 1 6.95
CHEMBL1080318 1 6.29
CHEMBL1080515 1 6.08
CHEMBL1082186 1 6.03
CHEMBL1081464 1 5.99
CHEMBL1080692 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL74950 IC50 = 5.8 nM 8.24
CHEMBL94 PHYSOSTIGMINE IC50 = 7.6 nM 8.12
CHEMBL1082185 IC50 = 8.5 nM 8.07
CHEMBL1080691 IC50 = 14.1 nM 7.85
CHEMBL1076615 IC50 = 14.9 nM 7.83
CHEMBL1080317 IC50 = 39.6 nM 7.40
CHEMBL1080937 IC50 = 61.3 nM 7.21
CHEMBL1081473 IC50 = 88.7 nM 7.05
CHEMBL74926 PHENSERINE IC50 = 103.7 nM 6.98
CHEMBL1081300 IC50 = 105.4 nM 6.98
CHEMBL1080319 IC50 = 113.5 nM 6.95
CHEMBL1080318 IC50 = 516.8 nM 6.29
CHEMBL1080515 IC50 = 829.9 nM 6.08
CHEMBL1082186 IC50 = 935.3 nM 6.03
CHEMBL1081464 IC50 = 1021.6 nM 5.99
CHEMBL1080692 IC50 = 1397.5 nM 5.86