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Compound Detail

CHEMBL5282048

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CC1(C)O[C@H]2O[C@H](NCCCCCCCNc3c4c(nc5ccccc35)CCCC4)[C@H](O)[C@H]2O1

Basic Information

ChEMBL ID CHEMBL5282048
Phase Preclinical
Structure Type MOL
InChI Key LORDNJPNOIOTPN-FXSWLTOZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

469.6
MW (Da)
4.26
ALogP
7
HBA
3
HBD
84.9
PSA (Ų)
0.45
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H39N3O4
MW 469.63
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness 0.11

Activity Summary

IC50 2 meas. best 8.06

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL3198
IC50 8.06 8.06 8.7 1
Cholinesterase
CHEMBL2528
IC50 7.57 7.57 27.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 8.7 nM 8.06 Inhibition of mouse brain AChE 35028560
Cholinesterase IC50 = 27.0 nM 7.57 Inhibition of mouse serum BuChE 35028560

Literature References

PubMed DOI Target Context # Activities
35028560 10.1039/D1MD00217A Acetylcholinesterase 1
35028560 10.1039/D1MD00217A Cholinesterase 1

Data from ChEMBL 36 via Core Engine