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Compound Detail

CHEMBL5093590

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C[C@@]1(COc2ccc(C(F)(F)F)cn2)CCn2cc([N+](=O)[O-])nc2O1

Basic Information

ChEMBL ID CHEMBL5093590
Phase Preclinical
Structure Type MOL
InChI Key IPSCEEDMLVAPAA-ZDUSSCGKSA-N
2
Targets
2
Activities
1
Assay Types
7
PK Parameters
6
Publications
0
Known Names

Molecular Properties

358.3
MW (Da)
2.83
ALogP
7
HBA
0
HBD
92.3
PSA (Ų)
0.62
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H13F3N4O4
MW 358.28
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.92

Activity Summary

IC50 2 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Leishmania infantum
CHEMBL612848
IC50 6.12 6.12 750.0 1
Trypanosoma cruzi
CHEMBL368
IC50 6.01 6.01 980.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 183000.0 ng.hr.mL-1 Mus musculus
AUC 924.0 ng.hr.mL-1 Cricetulus griseus
Cmax 92106.73 nM Mus musculus
Cmax 865.25 nM Cricetulus griseus
T1/2 1.5 hr Mus musculus
Tmax 2.0 hr Mus musculus
Tmax 4.3 hr Cricetulus griseus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33268145 10.1016/j.ejmech.2020.112914 ADMET 11
33268145 10.1016/j.ejmech.2020.112914 Leishmania infantum 4
33268145 10.1016/j.ejmech.2020.112914 Trypanosoma cruzi 1
33268145 10.1016/j.ejmech.2020.112914 MRC5 1
33268145 10.1016/j.ejmech.2020.112914 No relevant target 1
33268145 10.1016/j.ejmech.2020.112914 Leishmania donovani 1

Data from ChEMBL 36 via Core Engine