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Compound Detail

CHEMBL2448717

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CO/N=C(\C)c1ccc(-n2ccnc2)c(NC(=O)c2ccc(-c3cccs3)nc2)c1

Basic Information

ChEMBL ID CHEMBL2448717
Phase Preclinical
Structure Type MOL
InChI Key VSTCTLPTEFNPSS-CVKSISIWSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
5
Publications
0
Known Names

Molecular Properties

417.5
MW (Da)
4.62
ALogP
7
HBA
1
HBD
81.4
PSA (Ų)
0.37
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19N5O2S
MW 417.49
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -2.24

Activity Summary

IC50 2 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 8.57 8.57 2.7 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.85 5.85 1400.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 102.0 mL.min-1.g-1 Homo sapiens
T1/2 0.2833 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma cruzi IC50 = 2.7 nM 8.57 DNDI: Chagas in Vitro -
Cytochrome P450 3A4 IC50 = 1400.0 nM 5.85 DNDI: Human CYP3A4 inhibition determined using 6b-hydroxylation of testosterone -

Literature References

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

Data from ChEMBL 36 via Core Engine