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Compound Detail

CHEMBL596639

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COc1cc2ncnc(NC3CCN(Cc4ccccc4)CC3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL596639
Phase Preclinical
Structure Type MOL
InChI Key QGLMINHDDNFQAQ-UHFFFAOYSA-N
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

378.5
MW (Da)
3.72
ALogP
6
HBA
1
HBD
59.5
PSA (Ų)
0.71
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 C22H26N4O2
MW 378.48
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.06

Activity Summary

IC50 4 meas. best 6.21
EC50 2 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 6.4 6.355 400.0 2
Plasmodium falciparum
CHEMBL364
IC50 6.21 6.01 620.0 3
Histone-lysine N-methyltransferase NSD2
CHEMBL3108645
IC50 5.84 5.84 1449.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3832761 Plasmodium falciparum 4
18579783 10.1073/pnas.0802982105 Plasmodium falciparum 2
39230932 10.1021/acs.jmedchem.4c00639 Histone-lysine N-methyltransferase EHMT2 2
- 10.6019/CHEMBL4513149 Candida albicans 1
39230932 10.1021/acs.jmedchem.4c00639 Histone-lysine N-methyltransferase NSD2 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
18579783 10.1073/pnas.0802982105 Unchecked 1
- 10.6019/CHEMBL4513101 Naegleria gruberi 1
- 10.6019/CHEMBL3987221 Porphobilinogen deaminase 1
- 10.6019/CHEMBL3987221 Ferrochelatase, mitochondrial 1
- 10.6019/CHEMBL3832761 HepG2 1
- 10.6019/CHEMBL3832761 Plasmodium berghei 1
18579783 10.1073/pnas.0802982105 Huh-7 1

Data from ChEMBL 36 via Core Engine