Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL869256

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

Binding
Inhibition of rat brain AChE
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Acetylcholinesterase (CHEMBL3199)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge.
Rydberg EH, Brumshtein B, Greenblatt HM, Wong DM, Shaya D, Williams LD, Carlier PR, Pang YP, Silman I, Sussman JL.
J Med Chem (2006) 49 : 5491 -5500
PubMed 16942022 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.40 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL32823 1 8.82
CHEMBL73800 1 8.42
CHEMBL75274 1 8.11
CHEMBL179732 1 7.55
CHEMBL424707 1 7.51
CHEMBL386423 1 7.40
CHEMBL211313 1 6.80
CHEMBL95 TACRINE 4.0 1 6.65
CHEMBL378006 1 6.59
CHEMBL213377 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL32823 IC50 = 1.5 nM 8.82
CHEMBL73800 IC50 = 3.8 nM 8.42
CHEMBL75274 IC50 = 7.8 nM 8.11
CHEMBL179732 IC50 = 28.0 nM 7.55
CHEMBL424707 IC50 = 31.0 nM 7.51
CHEMBL386423 IC50 = 40.0 nM 7.40
CHEMBL211313 IC50 = 157.0 nM 6.80
CHEMBL95 TACRINE IC50 = 223.0 nM 6.65
CHEMBL378006 IC50 = 254.0 nM 6.59
CHEMBL213377 IC50 = 711.0 nM 6.15