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Assay Detail

CHEMBL4035002

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Binding
Inhibition of recombinant full length Aedes aegypti AChE1 expressed in baculovirus-infected Sf9 insect cells using acetylthiocholine iodide as substrate measured over 60 secs by Ellman's method
23
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Aedes aegypti
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 20 5.01 7.05
Inhibition 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4092186 1 7.05
CHEMBL1340607 2 6.20
CHEMBL4079963 2 5.26
CHEMBL4064806 2 5.22
CHEMBL1543212 1 4.96
CHEMBL4100253 1 4.85
CHEMBL4075136 1 4.80
CHEMBL4073401 1 4.66
CHEMBL4099934 1 4.55
CHEMBL1416246 1 4.28
CHEMBL179218 1 4.25
CHEMBL1301463 1 4.08
CHEMBL4087841 1 -
CHEMBL1311140 1 -
CHEMBL4092142 1 -
CHEMBL4104206 1 -
CHEMBL4095547 1 -
CHEMBL4071394 1 -
CHEMBL4081932 1 -
CHEMBL1482486 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4092186 IC50 = 90.0 nM 7.05
CHEMBL1340607 IC50 = 630.0 nM 6.20
CHEMBL4079963 IC50 = 5500.0 nM 5.26
CHEMBL4064806 IC50 = 6000.0 nM 5.22
CHEMBL1543212 IC50 = 11000.0 nM 4.96
CHEMBL4100253 IC50 = 14000.0 nM 4.85
CHEMBL4075136 IC50 = 16000.0 nM 4.80
CHEMBL4073401 IC50 = 22000.0 nM 4.66
CHEMBL4099934 IC50 = 28000.0 nM 4.55
CHEMBL1416246 IC50 = 53000.0 nM 4.28
CHEMBL179218 IC50 = 56000.0 nM 4.25
CHEMBL1301463 IC50 = 83000.0 nM 4.08
CHEMBL4087841 IC50 > 200000.0 nM -
CHEMBL1311140 IC50 > 200000.0 nM -
CHEMBL4064806 Inhibition - % -
CHEMBL4092142 IC50 > 200000.0 nM -
CHEMBL4104206 IC50 > 200000.0 nM -
CHEMBL4079963 Inhibition - % -
CHEMBL4095547 IC50 > 200000.0 nM -
CHEMBL4071394 IC50 = 120000.0 nM -
CHEMBL4081932 IC50 > 200000.0 nM -
CHEMBL1482486 IC50 > 200000.0 nM -
CHEMBL1340607 Inhibition - % -