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Assay Detail

CHEMBL4035007

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

Binding
Inhibition of recombinant full length Anopheles gambiae AChE1 G122S mutant expressed in baculovirus-infected Sf9 insect cells using acetylthiocholine iodide as substrate measured over 60 secs by Ellman's method
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Anopheles gambiae
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Acetylcholinesterase (CHEMBL2046266)
Type SINGLE PROTEIN
Organism Anopheles gambiae

Publication

N-Aryl-N'-ethyleneaminothioureas effectively inhibit acetylcholinesterase 1 from disease-transmitting mosquitoes.
Knutsson S, Kindahl T, Engdahl C, Nikjoo D, Forsgren N, Kitur S, Ekström F, Kamau L, Linusson A.
Eur J Med Chem (2017) 134 : 415 -427
PubMed 28433681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 4.39 4.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4075136 1 4.77
CHEMBL4071394 1 4.66
CHEMBL1340607 1 4.62
CHEMBL4079963 1 4.48
CHEMBL4064806 1 4.30
CHEMBL4073401 1 4.18
CHEMBL4092186 1 4.08
CHEMBL4099934 1 4.03
CHEMBL1482486 1 -
CHEMBL4081932 1 -
CHEMBL1543212 1 -
CHEMBL1416246 1 -
CHEMBL4087841 1 -
CHEMBL1301463 1 -
CHEMBL4104206 1 -
CHEMBL4100253 1 -
CHEMBL4095547 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4075136 IC50 = 17000.0 nM 4.77
CHEMBL4071394 IC50 = 22000.0 nM 4.66
CHEMBL1340607 IC50 = 24000.0 nM 4.62
CHEMBL4079963 IC50 = 33000.0 nM 4.48
CHEMBL4064806 IC50 = 50000.0 nM 4.30
CHEMBL4073401 IC50 = 66000.0 nM 4.18
CHEMBL4092186 IC50 = 84000.0 nM 4.08
CHEMBL4099934 IC50 = 94000.0 nM 4.03
CHEMBL1482486 IC50 > 200000.0 nM -
CHEMBL4081932 IC50 > 200000.0 nM -
CHEMBL1543212 IC50 > 200000.0 nM -
CHEMBL1416246 IC50 > 200000.0 nM -
CHEMBL4087841 IC50 > 200000.0 nM -
CHEMBL1301463 IC50 > 200000.0 nM -
CHEMBL4104206 IC50 > 200000.0 nM -
CHEMBL4100253 IC50 > 200000.0 nM -
CHEMBL4095547 IC50 > 200000.0 nM -