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Compound Detail

CHEMBL5175270

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COC1=CC(=O)N(C(=O)/C=C/[C@H](CCc2ccccc2)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)C2CCN(C)CC2)C1Cc1ccc(-c2ccc(C#N)cc2)cc1

Basic Information

ChEMBL ID CHEMBL5175270
Phase Preclinical
Structure Type MOL
InChI Key PSYGZORLNLCMLD-WYUYGYAUSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

843.1
MW (Da)
6.11
ALogP
8
HBA
3
HBD
160.9
PSA (Ų)
0.12
QED
2
Ro5 Violations
19
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C50H62N6O6
MW 843.08
Aromatic Rings 3
Heavy Atoms 62
NP-Likeness -0.06

Activity Summary

EC50 1 meas. best 6.37
IC50 1 meas. best 9.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cruzipain
CHEMBL3563
IC50 9.89 9.89 0.1 1
Trypanosoma cruzi
CHEMBL368
EC50 6.37 6.37 423.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35188371 10.1021/acs.jmedchem.1c02063 Cruzipain 1
35188371 10.1021/acs.jmedchem.1c02063 Trypanosoma cruzi 1
35188371 10.1021/acs.jmedchem.1c02063 C2C12 1

Data from ChEMBL 36 via Core Engine