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Assay Detail

CHEMBL997710

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

Binding
Inhibition of human recombinant AChE
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL220)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.
Butini S, Guarino E, Campiani G, Brindisi M, Coccone SS, Fiorini I, Novellino E, Belinskaya T, Saxena A, Gemma S.
Bioorg Med Chem Lett (2008) 18 : 5213 -5216
PubMed 18786825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.31 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL397271 1 8.21
CHEMBL451304 1 8.17
CHEMBL504571 1 7.81
CHEMBL129108 1 7.55
CHEMBL95 TACRINE 4.0 1 7.44
CHEMBL502244 1 6.89
CHEMBL525917 1 6.55
CHEMBL495711 1 5.72
CHEMBL495712 1 5.66
CHEMBL496126 1 5.48
CHEMBL521874 1 5.38
CHEMBL522073 1 5.20
CHEMBL508778 1 5.10
CHEMBL496946 1 4.95
CHEMBL496127 1 4.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL397271 Ki = 6.21 nM 8.21
CHEMBL451304 Ki = 6.75 nM 8.17
CHEMBL504571 Ki = 15.4 nM 7.81
CHEMBL129108 Ki = 27.9 nM 7.55
CHEMBL95 TACRINE Ki = 36.0 nM 7.44
CHEMBL502244 Ki = 130.0 nM 6.89
CHEMBL525917 Ki = 280.0 nM 6.55
CHEMBL495711 Ki = 1908.0 nM 5.72
CHEMBL495712 Ki = 2214.0 nM 5.66
CHEMBL496126 Ki = 3330.0 nM 5.48
CHEMBL521874 Ki = 4130.0 nM 5.38
CHEMBL522073 Ki = 6320.0 nM 5.20
CHEMBL508778 Ki = 7970.0 nM 5.10
CHEMBL496946 Ki = 11190.0 nM 4.95
CHEMBL496127 Ki = 34030.0 nM 4.47