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Compound Detail

CHEMBL4085114

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CC(=O)Nc1nc(NCCc2ccccc2)c2ccccc2n1

Basic Information

ChEMBL ID CHEMBL4085114
Phase Preclinical
Structure Type MOL
InChI Key VQKVYAIAPBPQEF-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

306.4
MW (Da)
3.24
ALogP
4
HBA
2
HBD
66.9
PSA (Ų)
0.76
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H18N4O
MW 306.37
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.21

Activity Summary

IC50 1 meas. best 5.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL220
IC50 5.16 5.16 7000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 7000.0 nM 5.16 Inhibition of human AChE using acetylthiocholine iodide as substrate preincubate... 27951490

Literature References

PubMed DOI Target Context # Activities
27951490 10.1016/j.ejmech.2016.12.005 Acetylcholinesterase 1
27951490 10.1016/j.ejmech.2016.12.005 Cholinesterase 1

Data from ChEMBL 36 via Core Engine