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Compound Detail

CHEMBL4743580

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CC/C(=N\Nc1nc(-c2ccc(Cl)cc2)cs1)c1cccc(Br)c1

Basic Information

ChEMBL ID CHEMBL4743580
Phase Preclinical
Structure Type MOL
InChI Key YHHPPPUAURYNPH-CJLVFECKSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

420.8
MW (Da)
6.45
ALogP
4
HBA
1
HBD
37.3
PSA (Ų)
0.38
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H15BrClN3S
MW 420.76
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.99

Activity Summary

IC50 2 meas. best 4.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cruzipain
CHEMBL3563
IC50 4.49 4.49 32700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cruzipain IC50 = 32700.0 nM 4.49 Inhibition of recombinant Trypanosoma cruzi cruzain using Z-FR-AMC as substrate ... 27295485

Literature References

PubMed DOI Target Context # Activities
27295485 10.1016/j.ejmech.2016.05.050 Cruzipain 2
27295485 10.1016/j.ejmech.2016.05.050 Trypanosoma cruzi 1
27295485 10.1016/j.ejmech.2016.05.050 Splenocyte 1
27295485 10.1016/j.ejmech.2016.05.050 Unchecked 1

Data from ChEMBL 36 via Core Engine