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Compound Detail

CHEMBL5079571

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COc1ccccc1C[C@@H](C=O)NC(=O)[C@H](Cc1ccccc1)NCC(=O)OCc1ccccc1

Basic Information

ChEMBL ID CHEMBL5079571
Phase Preclinical
Structure Type MOL
InChI Key ZRCIXVITURBMMP-DQEYMECFSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

474.6
MW (Da)
2.87
ALogP
6
HBA
2
HBD
93.7
PSA (Ų)
0.29
QED
0
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H30N2O5
MW 474.56
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.04

Activity Summary

Ki 1 meas. best 7.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cruzipain
CHEMBL3563
Ki 7.66 7.66 22.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cruzipain Ki = 22.0 nM 7.66 Time dependent inhibition of Trypanosoma cruzi cruzain using Cbz-Phe-Arg-AMC as ... 34288674

Literature References

PubMed DOI Target Context # Activities
34288674 10.1021/acs.jmedchem.1c00628 Cruzipain 1

Data from ChEMBL 36 via Core Engine