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Compound Detail

CHEMBL4456233

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COc1ccc(C[C@H](N[C@H](c2ccccc2)C(F)(F)F)C(=O)N[C@H](C#N)Cc2ccccc2)cc1

Basic Information

ChEMBL ID CHEMBL4456233
Phase Preclinical
Structure Type MOL
InChI Key LAXRPVSMHNUJNR-ZKMPZPQNSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

481.5
MW (Da)
4.75
ALogP
4
HBA
2
HBD
74.2
PSA (Ų)
0.44
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H26F3N3O2
MW 481.52
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.52

Activity Summary

Ki 2 meas. best 5.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Procathepsin L
CHEMBL3837
Ki 5.8 5.8 1584.9 1
Cruzipain
CHEMBL3563
Ki 5.4 5.4 3981.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31561938 10.1016/j.bmc.2019.115083 Cruzipain 1
31561938 10.1016/j.bmc.2019.115083 Procathepsin L 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