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Assay Detail

CHEMBL900178

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

Binding
Inhibition of human butyrylcholinesterase
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.
Elsinghorst PW, Cieslik JS, Mohr K, Tränkle C, Gütschow M.
J Med Chem (2007) 50 : 5685 -5695
PubMed 17944454 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 8.16 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1203986 1 8.85
CHEMBL1203985 1 8.82
CHEMBL1203984 2 8.62
CHEMBL540131 1 8.07
CHEMBL95 TACRINE 4.0 1 7.99
CHEMBL540132 1 7.78
CHEMBL555247 1 7.58
CHEMBL1677 TACRINE HYDROCHLORIDE 4.0 1 7.54
CHEMBL360055 GALLAMINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1203986 IC50 = 1.42 nM 8.85
CHEMBL1203985 IC50 = 1.5 nM 8.82
CHEMBL1203984 IC50 = 2.4 nM 8.62
CHEMBL540131 IC50 = 8.55 nM 8.07
CHEMBL95 TACRINE IC50 = 10.2 nM 7.99
CHEMBL540132 IC50 = 16.7 nM 7.78
CHEMBL555247 IC50 = 26.5 nM 7.58
CHEMBL1677 TACRINE HYDROCHLORIDE IC50 = 28.9 nM 7.54
CHEMBL360055 GALLAMINE IC50 = 2390000.0 nM -
CHEMBL1203984 IC50 = 235000.0 nM -