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Compound Detail

CHEMBL524771

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COc1ccc2nc3cc(Cl)ccc3c(NCCCCN)c2c1.Cl

Basic Information

ChEMBL ID CHEMBL524771
Phase Preclinical
Structure Type MOL
InChI Key HSKXYPJPZDVIBE-UHFFFAOYSA-N
Parent Compound CHEMBL528155
Active Moiety CHEMBL528155
3
Targets
7
Activities
2
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

329.8
MW (Da)
4.20
ALogP
4
HBA
2
HBD
60.2
PSA (Ų)
0.53
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21Cl2N3O
MW 366.29
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.70

Activity Summary

IC50 6 meas. best 7.17
Kd 1 meas. best 5.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 7.17 6.7225 67.0 4
KB
CHEMBL398
IC50 6.22 6.22 600.0 1
Unchecked
CHEMBL612545
Kd 5.09 5.09 8100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19879150 10.1016/j.bmc.2009.10.005 Unchecked 6
20485427 10.1038/nature09107 Plasmodium falciparum 4
19879150 10.1016/j.bmc.2009.10.005 Plasmodium falciparum 4
20485427 10.1038/nature09107 Unchecked 1
20485427 10.1038/nature09107 HepG2 1
19879150 10.1016/j.bmc.2009.10.005 No relevant target 1
19879150 10.1016/j.bmc.2009.10.005 KB 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1

Data from ChEMBL 36 via Core Engine