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Compound Detail

CHEMBL532994

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COc1cc2nc(N3CCC(C(N)=O)CC3)nc(NCc3ccccc3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL532994
Phase Preclinical
Structure Type MOL
InChI Key MJPXJPVGOCGDCV-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
2.96
ALogP
7
HBA
2
HBD
102.6
PSA (Ų)
0.60
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H27N5O3
MW 421.50
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.21

Activity Summary

IC50 2 meas. best 6.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.75 6.75 180.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum IC50 = 180.0 nM 6.75 Antimalarial activity against Plasmodium falciparum NF54 assessed as inhibition ... 33524940

Literature References

PubMed DOI Target Context # Activities
20485427 10.1038/nature09107 Plasmodium falciparum 4
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 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
33524940 10.1016/j.bmc.2021.116018 Plasmodium falciparum 1
33524940 10.1016/j.bmc.2021.116018 L6 1
33524940 10.1016/j.bmc.2021.116018 Unchecked 1

Data from ChEMBL 36 via Core Engine