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Compound Detail

CHEMBL3974431

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CNC(=O)NCCNC(=O)c1c2cc[n+](C)cc2c(C)c2c1[nH]c1ccc(OC)cc12.[Cl-]

Basic Information

ChEMBL ID CHEMBL3974431
Phase Preclinical
Structure Type MOL
InChI Key JRCMLRZEHUVRAA-UHFFFAOYSA-N
Parent Compound CHEMBL3990415
Active Moiety CHEMBL3990415
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

420.5
MW (Da)
2.27
ALogP
3
HBA
4
HBD
99.1
PSA (Ų)
0.29
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26ClN5O3
MW 455.95
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.17

Activity Summary

IC50 1 meas. best 4.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 4.5 4.5 32000.0 1

Pharmacokinetic Data

Parameter Value Units Species
Ka 2.04 10'5/M -
Ka 3.62 10'5/M -
Ka 3.74 10'5/M -
Ka 2.55 10'5/M -
Ka 3.62 10'5/M -
Ka 1.46 10'5/M -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
NON-PROTEIN TARGET IC50 = 32000.0 nM 4.5 Cytotoxicity against human HeLaS3 cells assessed as reduction in cell viability ... 28063783

Literature References

PubMed DOI Target Context # Activities
28063783 10.1016/j.bmc.2016.12.031 Unchecked 9
28063783 10.1016/j.bmc.2016.12.031 NON-PROTEIN TARGET 2
28063783 10.1016/j.bmc.2016.12.031 Mus musculus 1

Data from ChEMBL 36 via Core Engine