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Assay Detail

CHEMBL644626

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

Binding
Inhibition of human acetylcholinesterase from erythrocytes (RBC)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.
Yu QS, Pei XF, Holloway HW, Greig NH, Brossi A.
J Med Chem (1997) 40 : 2895 -2901
PubMed 9288171 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.26 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54727 1 7.62
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.55
CHEMBL418917 1 7.39
CHEMBL431784 1 7.25
CHEMBL80221 1 6.79
CHEMBL319541 1 6.61
CHEMBL99581 1 6.41
CHEMBL100366 1 6.11
CHEMBL99414 1 5.66
CHEMBL317162 1 5.55
CHEMBL75919 1 5.46
CHEMBL99284 1 5.25
CHEMBL76640 (+)-PHYSOSTIGMINE 1 5.00
CHEMBL99655 1 4.95

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54727 IC50 = 24.0 nM 7.62
CHEMBL94 PHYSOSTIGMINE IC50 = 27.9 nM 7.55
CHEMBL418917 IC50 = 40.8 nM 7.39
CHEMBL431784 IC50 = 56.7 nM 7.25
CHEMBL80221 IC50 = 160.8 nM 6.79
CHEMBL319541 IC50 = 245.3 nM 6.61
CHEMBL99581 IC50 = 387.5 nM 6.41
CHEMBL100366 IC50 = 780.4 nM 6.11
CHEMBL99414 IC50 = 2193.5 nM 5.66
CHEMBL317162 IC50 = 2847.5 nM 5.55
CHEMBL75919 IC50 = 3500.5 nM 5.46
CHEMBL99284 IC50 = 5654.5 nM 5.25
CHEMBL76640 (+)-PHYSOSTIGMINE IC50 = 9887.0 nM 5.00
CHEMBL99655 IC50 = 11223.0 nM 4.95