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Assay Detail

CHEMBL641387

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

Binding
Inhibition of acetylcholinesterase activity in rat cerebral cortex homogenate, in the presence of a specific butyrylcholinesterase (BChE) inhibitor; ethopropazine
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.
Carlier PR, Chow ES, Han Y, Liu J, El Yazal J, Pang YP.
J Med Chem (1999) 42 : 4225 -4231
PubMed 10514292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.15 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555320 1 8.82
CHEMBL557225 1 8.11
CHEMBL542236 1 8.06
CHEMBL545539 1 8.00
CHEMBL542234 1 7.89
CHEMBL543906 1 7.87
CHEMBL544369 1 7.41
CHEMBL539811 1 7.35
CHEMBL541853 1 7.33
CHEMBL542732 1 7.28
CHEMBL542477 1 7.15
CHEMBL543667 1 7.08
CHEMBL544605 1 7.05
CHEMBL545774 1 6.88
CHEMBL540837 1 6.83
CHEMBL544143 1 6.75
CHEMBL544603 1 6.75
CHEMBL1677 TACRINE HYDROCHLORIDE 4.0 1 6.65
CHEMBL542482 1 6.58
CHEMBL538533 1 6.58
CHEMBL540830 1 6.50
CHEMBL58146 QUINOLIN-4-AMINE 1 4.29
CHEMBL284348 DALFAMPRIDINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555320 IC50 = 1.5 nM 8.82
CHEMBL557225 IC50 = 7.8 nM 8.11
CHEMBL542236 IC50 = 8.8 nM 8.06
CHEMBL545539 IC50 = 10.1 nM 8.00
CHEMBL542234 IC50 = 12.8 nM 7.89
CHEMBL543906 IC50 = 13.6 nM 7.87
CHEMBL544369 IC50 = 38.7 nM 7.41
CHEMBL539811 IC50 = 45.0 nM 7.35
CHEMBL541853 IC50 = 47.0 nM 7.33
CHEMBL542732 IC50 = 52.0 nM 7.28
CHEMBL542477 IC50 = 71.0 nM 7.15
CHEMBL543667 IC50 = 83.6 nM 7.08
CHEMBL544605 IC50 = 89.4 nM 7.05
CHEMBL545774 IC50 = 131.0 nM 6.88
CHEMBL540837 IC50 = 147.0 nM 6.83
CHEMBL544143 IC50 = 176.0 nM 6.75
CHEMBL544603 IC50 = 180.0 nM 6.75
CHEMBL1677 TACRINE HYDROCHLORIDE IC50 = 223.0 nM 6.65
CHEMBL542482 IC50 = 261.0 nM 6.58
CHEMBL538533 IC50 = 264.0 nM 6.58
CHEMBL540830 IC50 = 319.0 nM 6.50
CHEMBL58146 QUINOLIN-4-AMINE IC50 = 50700.0 nM 4.29
CHEMBL284348 DALFAMPRIDINE IC50 > 500000.0 nM -