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Compound Detail

CHEMBL583256

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O=[N+]([O-])c1cn2c(n1)OC[C@@H](OCc1ccc(-c3ccc(C(F)(F)F)cc3Cl)cc1)C2

Basic Information

ChEMBL ID CHEMBL583256
Phase Preclinical
Structure Type MOL
InChI Key UYAFPHSEADQNSM-HNNXBMFYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
10
Publications
0
Known Names

Molecular Properties

453.8
MW (Da)
5.11
ALogP
6
HBA
0
HBD
79.4
PSA (Ų)
0.40
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15ClF3N3O4
MW 453.80
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.81

Activity Summary

IC50 2 meas. best 5.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 5.43 5.43 3700.0 1
L6
CHEMBL614793
IC50 4.47 4.47 34000.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 4.167 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19928920 10.1021/jm901207n Mycobacterium tuberculosis 4
33007723 10.1016/j.ejmech.2020.112849 Trypanosoma cruzi 3
33007723 10.1016/j.ejmech.2020.112849 ADMET 2
19928920 10.1021/jm901207n Liver microsomes 1
19928920 10.1021/jm901207n ADMET 1
19928920 10.1021/jm901207n Vero 1
33007723 10.1016/j.ejmech.2020.112849 L6 1
33007723 10.1016/j.ejmech.2020.112849 Unchecked 1
33007723 10.1016/j.ejmech.2020.112849 No relevant target 1
33007723 10.1016/j.ejmech.2020.112849 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine