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Assay Detail

CHEMBL2072352

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

Binding
Inhibition of human AChE pre-incubated for 10 mins before acetylthiocholine iodide substrate addition
11
Total Activities
11
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

Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
Ohlendorf B, Schulz D, Erhard A, Nagel K, Imhoff JF.
J Nat Prod (2012) 75 : 1400 -1404
PubMed 22775474 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.11 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395280 HUPERZINE A 2.0 1 7.92
CHEMBL659 GALANTAMINE 4.0 1 6.00
CHEMBL2071425 DIACETYLGERANYLPHENAZINEDIOL 1 5.70
CHEMBL2071424 GERANYLPHENAZINEDIOL 1 5.58
CHEMBL2071426 1 5.34
CHEMBL2071427 1 -
CHEMBL463686 PHENAZINE-1-CARBOXYLIC ACID 1 -
CHEMBL2071428 ENDOPHENAZINE A 1 -
CHEMBL1952289 ENDOPHENAZINE B 1 -
CHEMBL130 CHLORAMPHENICOL 4.0 1 -
CHEMBL83 TAMOXIFEN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395280 HUPERZINE A IC50 = 12.0 nM 7.92
CHEMBL659 GALANTAMINE IC50 = 1000.0 nM 6.00
CHEMBL2071425 DIACETYLGERANYLPHENAZINEDIOL IC50 = 2010.0 nM 5.70
CHEMBL2071424 GERANYLPHENAZINEDIOL IC50 = 2620.0 nM 5.58
CHEMBL2071426 IC50 = 4520.0 nM 5.34
CHEMBL2071427 IC50 > 50000.0 nM -
CHEMBL463686 PHENAZINE-1-CARBOXYLIC ACID IC50 > 50000.0 nM -
CHEMBL2071428 ENDOPHENAZINE A IC50 > 50000.0 nM -
CHEMBL1952289 ENDOPHENAZINE B IC50 > 50000.0 nM -
CHEMBL130 CHLORAMPHENICOL IC50 - -
CHEMBL83 TAMOXIFEN IC50 - -