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Compound Detail

CHEMBL5556303

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O=C(Nc1cnc2ccccc2c1N1CCN(Cc2ccccc2)CC1)c1ccc([N+](=O)[O-])c([N+](=O)[O-])c1

Basic Information

ChEMBL ID CHEMBL5556303
Phase Preclinical
Structure Type MOL
InChI Key JAUXJCQUVHIPEY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

512.5
MW (Da)
4.63
ALogP
8
HBA
1
HBD
134.8
PSA (Ų)
0.28
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H24N6O5
MW 512.53
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 5.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 5.04 5.04 9040.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cholinesterase IC50 = 9040.0 nM 5.04 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