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Compound Detail

CHEMBL581128

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COc1ccccc1CNC(=O)c1cc(C2CC2)nc2c1cnn2C(C)C

Basic Information

ChEMBL ID CHEMBL581128
Phase Preclinical
Structure Type MOL
InChI Key WLJYEEIXBTUIEV-UHFFFAOYSA-N
1
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

364.4
MW (Da)
3.83
ALogP
5
HBA
1
HBD
69.0
PSA (Ų)
0.72
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 C21H24N4O2
MW 364.45
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.92

Activity Summary

IC50 3 meas. best 6.03
EC50 1 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 6.17 6.17 680.0 1
Plasmodium falciparum
CHEMBL364
IC50 6.03 5.8467 940.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3832761 Plasmodium falciparum 4
20485427 10.1038/nature09107 Plasmodium falciparum 4
- 10.6019/CHEMBL3832761 HepG2 2
- 10.6019/CHEMBL3987221 Porphobilinogen deaminase 1
39024967 10.1016/j.ejmech.2024.116677 HepG2 1
39024967 10.1016/j.ejmech.2024.116677 Plasmodium falciparum 1
- 10.6019/CHEMBL4513149 Staphylococcus aureus 1
- 10.6019/CHEMBL4513149 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513149 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4513149 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513149 Escherichia coli 1
- 10.6019/CHEMBL4513149 Cryptococcus neoformans 1
- 10.6019/CHEMBL4513149 Candida albicans 1
- 10.6019/CHEMBL4513101 Naegleria gruberi 1
- 10.6019/CHEMBL3987221 Ferrochelatase, mitochondrial 1
- 10.6019/CHEMBL3832761 Plasmodium berghei 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
20485427 10.1038/nature09107 Unchecked 1

Data from ChEMBL 36 via Core Engine