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Compound Detail

CHEMBL3104374

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CS(=O)(=O)c1ccc(N2CCN(C(=O)C(c3ccc(C#N)cc3)c3cccnc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL3104374
Phase Preclinical
Structure Type MOL
InChI Key DOTQGOWEPGZREI-UHFFFAOYSA-N
1
Targets
4
Activities
1
Assay Types
6
PK Parameters
12
Publications
0
Known Names

Molecular Properties

460.6
MW (Da)
2.84
ALogP
6
HBA
0
HBD
94.4
PSA (Ų)
0.58
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N4O3S
MW 460.56
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.78

Activity Summary

IC50 4 meas. best 7.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 7.75 7.5625 18.0 4

Pharmacokinetic Data

Parameter Value Units Species
CL 15.0 mL.min-1.g-1 Homo sapiens
CL 10.0 mL.min-1.g-1 Homo sapiens
CL 7.0 mL.min-1.g-1 Homo sapiens
T1/2 1.883 hr Homo sapiens
T1/2 2.817 hr Homo sapiens
T1/2 4.167 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3137386 No relevant target 12
- 10.6019/CHEMBL3137386 ADMET 9
- 10.6019/CHEMBL3137386 Trypanosoma cruzi 8
- 10.6019/CHEMBL3137386 L6 4
24304150 10.1021/jm401610c No relevant target 3
- 10.6019/CHEMBL3137386 Trypanosoma brucei rhodesiense 3
- 10.6019/CHEMBL3137386 Cytochrome P450 3A4 3
24304150 10.1021/jm401610c Plasma 2
24304150 10.1021/jm401610c Mus musculus 1
24304150 10.1021/jm401610c Cytochrome P450 3A4 1
24304150 10.1021/jm401610c L6 1
24304150 10.1021/jm401610c Trypanosoma cruzi 1

Data from ChEMBL 36 via Core Engine