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Compound Detail

CHEMBL2448739

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Cc1ccc(-n2ccnc2)c(NC(=O)c2cnc(-c3ccccc3)s2)c1

Basic Information

ChEMBL ID CHEMBL2448739
Phase Preclinical
Structure Type MOL
InChI Key IRDKASZLBXOERK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

360.4
MW (Da)
4.56
ALogP
5
HBA
1
HBD
59.8
PSA (Ų)
0.58
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 C20H16N4OS
MW 360.44
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -2.38

Activity Summary

IC50 2 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 8.7 8.7 2.0 1
L6
CHEMBL614793
IC50 4.06 4.06 86640.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 109.0 mL.min-1.g-1 Homo sapiens
T1/2 0.2667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma cruzi IC50 = 1.975 nM 8.7 DNDI: Chagas in Vitro -
L6 IC50 = 86640.0 nM 4.06 DNDI: Cytotoxicity in vitro, against rat skeletal myoblast (L-6) cells -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL2448688 No relevant target 4
- 10.6019/CHEMBL2448688 ADMET 3
- 10.6019/CHEMBL2448688 Cytochrome P450 3A4 3
- 10.6019/CHEMBL2448688 Trypanosoma cruzi 2
- 10.6019/CHEMBL2448688 L6 1

Data from ChEMBL 36 via Core Engine