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Compound Detail

CHEMBL5517904

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O=C(Nc1cnc2ccccc2c1N1CCN(Cc2ccccc2)CC1)c1ccc([N+](=O)[O-])cc1

Basic Information

ChEMBL ID CHEMBL5517904
Phase Preclinical
Structure Type MOL
InChI Key NFSUOMQYKJCBRI-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

467.5
MW (Da)
4.72
ALogP
6
HBA
1
HBD
91.6
PSA (Ų)
0.33
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25N5O3
MW 467.53
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.54

Activity Summary

IC50 1 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 700.0 nM 6.16 Inhibition of equine serum BChE using BTC as substrate incubated for 2 mins by E... 38704944

Literature References

PubMed DOI Target Context # Activities
38704944 10.1016/j.ejmech.2024.116463 Cholinesterase 2
38704944 10.1016/j.ejmech.2024.116463 Unchecked 1
38704944 10.1016/j.ejmech.2024.116463 Acetylcholinesterase 1

Data from ChEMBL 36 via Core Engine