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Compound Detail

CHEMBL4591985

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CC(C)C[C@H](N[C@H](c1ccc(-c2ccccc2)cc1)C(F)(F)F)C(=O)N[C@H](C#N)Cc1ccccc1

Basic Information

ChEMBL ID CHEMBL4591985
Phase Preclinical
Structure Type MOL
InChI Key VCYHSLAYQYYGHC-GMQQYTKMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

493.6
MW (Da)
6.21
ALogP
3
HBA
2
HBD
64.9
PSA (Ų)
0.35
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H30F3N3O
MW 493.57
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.48

Activity Summary

Ki 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cruzipain
CHEMBL3563
Ki 6.6 6.6 251.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cruzipain Ki = 251.19 nM 6.6 Inhibition of Trypanosoma cruzi cruzain using Z-Phe-Arg-7-amido-4-methylcoumarin... 31561938

Literature References

PubMed DOI Target Context # Activities
31561938 10.1016/j.bmc.2019.115083 Cruzipain 1
31561938 10.1016/j.bmc.2019.115083 No relevant target 1
31561938 10.1016/j.bmc.2019.115083 Trypanosoma cruzi 1

Data from ChEMBL 36 via Core Engine