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Assay Detail

CHEMBL3280463

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

Binding
Reversible mixed-type inhibition of electric eel acetylcholinesterase using acetylcholine bromide as substrate assessed as free enzyme-inhibitor complex by Lineweaver-Burk plot analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Electrophorus electricus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL4078)
Type SINGLE PROTEIN
Organism Electrophorus electricus

Publication

Potent reversible anticholinesterase agents. Bis- and mono-N-substituted benzoquinolinium halides.
Chen WS, Cocolas GH, Cavallito CJ, Chai KJ.
J Med Chem (1977) 20 : 1617 -1623
PubMed 592327 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 5.95 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3276408 1 8.68
CHEMBL3276410 1 8.18
CHEMBL3276411 1 8.00
CHEMBL3276412 1 6.75
CHEMBL338975 PHYSOSTIGMINE SALICYLATE -1.0 1 6.68
CHEMBL3276417 1 6.60
CHEMBL3276418 1 6.55
CHEMBL3276429 1 6.30
CHEMBL3276416 1 6.28
CHEMBL1200933 HEXAFLUORENIUM BROMIDE 4.0 1 5.89
CHEMBL3276424 1 5.75
CHEMBL3276430 1 5.54
CHEMBL3276414 1 5.50
CHEMBL3276413 1 5.25
CHEMBL3276422 1 5.05
CHEMBL3276423 1 5.03
CHEMBL3276420 1 4.92
CHEMBL3276427 1 4.75
CHEMBL3276415 1 4.66
CHEMBL3276419 1 4.51
CHEMBL3276425 1 4.08
CHEMBL3276428 1 -
CHEMBL3276432 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3276408 Ki = 2.1 nM 8.68
CHEMBL3276410 Ki = 6.6 nM 8.18
CHEMBL3276411 Ki = 10.0 nM 8.00
CHEMBL3276412 Ki = 180.0 nM 6.75
CHEMBL338975 PHYSOSTIGMINE SALICYLATE Ki = 210.0 nM 6.68
CHEMBL3276417 Ki = 250.0 nM 6.60
CHEMBL3276418 Ki = 280.0 nM 6.55
CHEMBL3276429 Ki = 500.0 nM 6.30
CHEMBL3276416 Ki = 530.0 nM 6.28
CHEMBL1200933 HEXAFLUORENIUM BROMIDE Ki = 1300.0 nM 5.89
CHEMBL3276424 Ki = 1800.0 nM 5.75
CHEMBL3276430 Ki = 2900.0 nM 5.54
CHEMBL3276414 Ki = 3200.0 nM 5.50
CHEMBL3276413 Ki = 5600.0 nM 5.25
CHEMBL3276422 Ki = 8900.0 nM 5.05
CHEMBL3276423 Ki = 9300.0 nM 5.03
CHEMBL3276420 Ki = 12000.0 nM 4.92
CHEMBL3276427 Ki = 18000.0 nM 4.75
CHEMBL3276415 Ki = 22000.0 nM 4.66
CHEMBL3276419 Ki = 31000.0 nM 4.51
CHEMBL3276425 Ki = 83000.0 nM 4.08
CHEMBL3276428 Ki = 150000.0 nM -
CHEMBL3276432 Ki = 320000.0 nM -