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Compound Detail

CHEMBL5288285

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CC1(C)O[C@H]2O[C@H](CNCCCCCCCCCCCNc3c4c(nc5ccccc35)CCCC4)[C@H](O)[C@H]2O1

Basic Information

ChEMBL ID CHEMBL5288285
Phase Preclinical
Structure Type MOL
InChI Key OYIWCOZWLUTAQH-GEIIOTBESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

539.8
MW (Da)
5.86
ALogP
7
HBA
3
HBD
84.9
PSA (Ų)
0.24
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H49N3O4
MW 539.76
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness 0.20

Activity Summary

IC50 2 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Acetylcholinesterase
CHEMBL3198
IC50 8.66 8.66 2.2 1
Cholinesterase
CHEMBL2528
IC50 8.31 8.31 4.9 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Acetylcholinesterase IC50 = 2.2 nM 8.66 Inhibition of mouse brain AChE 35028560
Cholinesterase IC50 = 4.9 nM 8.31 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