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Compound Detail

CHEMBL1834071

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CC(C)N1CCN(c2nccc(NC(c3ccccc3)c3ccccc3)n2)CC1

Basic Information

ChEMBL ID CHEMBL1834071
Phase Preclinical
Structure Type MOL
InChI Key LEAAVIRMAKBSFE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

387.5
MW (Da)
4.21
ALogP
5
HBA
1
HBD
44.3
PSA (Ų)
0.69
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H29N5
MW 387.53
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 5.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 5.01 5.01 9700.0 1
Acetylcholinesterase
CHEMBL220
IC50 4.69 4.69 20300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 9700.0 nM 5.01 Inhibition of equine BuChE by Ellman's method 21873056
Acetylcholinesterase IC50 = 20300.0 nM 4.69 Inhibition of human AChE by Ellman's assay 21873056

Literature References

PubMed DOI Target Context # Activities
21873056 10.1016/j.bmcl.2011.07.091 Unchecked 2
21873056 10.1016/j.bmcl.2011.07.091 Acetylcholinesterase 2
21873056 10.1016/j.bmcl.2011.07.091 Cholinesterase 1

Data from ChEMBL 36 via Core Engine