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Compound Detail

CHEMBL2448724

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O=C(Nc1ccccc1-n1ccnc1)c1cnc(-c2ccccc2)s1

Basic Information

ChEMBL ID CHEMBL2448724
Phase Preclinical
Structure Type MOL
InChI Key QKAQPMIIFZVJKK-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

346.4
MW (Da)
4.25
ALogP
5
HBA
1
HBD
59.8
PSA (Ų)
0.60
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14N4OS
MW 346.42
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -2.27

Activity Summary

IC50 4 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 8.49 8.4067 3.2 3
Cytochrome P450 3A4
CHEMBL340
IC50 5.7 5.7 2000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 57.0 mL.min-1.g-1 Homo sapiens
T1/2 0.5 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma cruzi IC50 = 3.2 nM 8.49 DNDI: Chagas in Vitro -
Trypanosoma cruzi IC50 = 3.8 nM 8.42 DNDI: Chagas in Vitro -
Trypanosoma cruzi IC50 = 4.9 nM 8.31 DNDI: Chagas in Vitro -
Cytochrome P450 3A4 IC50 = 2000.0 nM 5.7 DNDI: Human CYP3A4 inhibition determined using 6b-hydroxylation of testosterone -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL2448688 Trypanosoma cruzi 5
- 10.6019/CHEMBL2448688 No relevant target 4
- 10.6019/CHEMBL2448688 ADMET 3
- 10.6019/CHEMBL2448688 Cytochrome P450 3A4 3
- 10.6019/CHEMBL2448688 L6 2

Data from ChEMBL 36 via Core Engine