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Compound Detail

CHEMBL244501

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COc1ccc(C(=O)Nc2ccc3cc4ccc(NC(C)=O)cc4nc3c2)cc1OC

Basic Information

ChEMBL ID CHEMBL244501
Phase Preclinical
Structure Type MOL
InChI Key VSMJHXOYMJKVPR-UHFFFAOYSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

415.4
MW (Da)
4.62
ALogP
5
HBA
2
HBD
89.5
PSA (Ų)
0.46
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 C24H21N3O4
MW 415.45
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.96

Activity Summary

IC50 3 meas. best 5.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leishmania infantum
CHEMBL612848
IC50 5.89 5.89 1300.0 1
THP-1
CHEMBL614245
IC50 5.68 5.68 2100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Leishmania infantum IC50 = 1300.0 nM 5.89 Antiamastigote activity against Leishmania infantum 17418916
THP-1 IC50 = 2100.0 nM 5.68 Cytotoxicity against human THP1 cells 17418916

Literature References

PubMed DOI Target Context # Activities
17418916 10.1016/j.ejmech.2007.02.010 Leishmania infantum 2
17418916 10.1016/j.ejmech.2007.02.010 Unchecked 2
17418916 10.1016/j.ejmech.2007.02.010 THP-1 1

Data from ChEMBL 36 via Core Engine