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Compound Detail

CHEMBL4074432

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N#C/C=C/[C@H](CCc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)OCc1ccc([N+](=O)[O-])cc1

Basic Information

ChEMBL ID CHEMBL4074432
Phase Preclinical
Structure Type MOL
InChI Key NBEKUGPYIHFGOY-PWLQFARKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

512.6
MW (Da)
4.63
ALogP
6
HBA
2
HBD
134.4
PSA (Ų)
0.21
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28N4O5
MW 512.57
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.28

Activity Summary

Ki 1 meas. best 5.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rhodesain
CHEMBL4188
Ki 5.76 5.76 1743.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rhodesain Ki = 1743.0 nM 5.76 Inhibition of recombinant Trypanosoma brucei rhodesiense rhodesain expressed in ... 28763614

Literature References

PubMed DOI Target Context # Activities
28763614 10.1021/acs.jmedchem.7b00405 Rhodesain 3
28763614 10.1021/acs.jmedchem.7b00405 Procathepsin L 3
28763614 10.1021/acs.jmedchem.7b00405 Plasmodium falciparum 1
28763614 10.1021/acs.jmedchem.7b00405 Falcipain 2 1

Data from ChEMBL 36 via Core Engine