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Assay Detail

CHEMBL1101959

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

Binding
Inhibition of mouse brain AChE after 1 hr by modified Ellman's colorimetric method
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL3198)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, synthesis, evaluation and QSAR analysis of N(1)-substituted norcymserine derivatives as selective butyrylcholinesterase inhibitors.
Takahashi J, Hijikuro I, Kihara T, Murugesh MG, Fuse S, Kunimoto R, Tsumura Y, Akaike A, Niidome T, Okuno Y, Takahashi T, Sugimoto H.
Bioorg Med Chem Lett (2010) 20 : 1718 -1720
PubMed 20137934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.59 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94 PHYSOSTIGMINE 3.0 1 7.40
CHEMBL1081275 1 5.46
CHEMBL1080737 1 5.38
CHEMBL129837 4-ISOPROPYLPHENSERINE 1 5.08
CHEMBL1081428 1 4.64
CHEMBL1087663 1 -
CHEMBL1080386 PHENETHYLCYMSERINE 1 -
CHEMBL1087152 1 -
CHEMBL1086635 1 -
CHEMBL1086636 1 -
CHEMBL1087623 1 -
CHEMBL1080541 1 -
CHEMBL1080720 1 -
CHEMBL1080562 1 -
CHEMBL1080730 1 -
CHEMBL1076547 1 -
CHEMBL1076548 1 -
CHEMBL1081427 1 -
CHEMBL1080542 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94 PHYSOSTIGMINE IC50 = 40.0 nM 7.40
CHEMBL1081275 IC50 = 3500.0 nM 5.46
CHEMBL1080737 IC50 = 4200.0 nM 5.38
CHEMBL129837 4-ISOPROPYLPHENSERINE IC50 = 8400.0 nM 5.08
CHEMBL1081428 IC50 = 23000.0 nM 4.64
CHEMBL1087663 IC50 > 100000.0 nM -
CHEMBL1080386 PHENETHYLCYMSERINE IC50 > 100000.0 nM -
CHEMBL1087152 IC50 > 100000.0 nM -
CHEMBL1086635 IC50 > 100000.0 nM -
CHEMBL1086636 IC50 > 100000.0 nM -
CHEMBL1087623 IC50 > 100000.0 nM -
CHEMBL1080541 IC50 > 100000.0 nM -
CHEMBL1080720 IC50 > 100000.0 nM -
CHEMBL1080562 IC50 > 100000.0 nM -
CHEMBL1080730 IC50 > 100000.0 nM -
CHEMBL1076547 IC50 > 100000.0 nM -
CHEMBL1076548 IC50 > 100000.0 nM -
CHEMBL1081427 IC50 > 100000.0 nM -
CHEMBL1080542 IC50 > 100000.0 nM -