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Compound Detail

CHEMBL207797

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CCOC(=O)[C@@H]1[C@@H](C(=O)OCC)N1C(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)OC(C)(C)C

Basic Information

ChEMBL ID CHEMBL207797
Phase Preclinical
Structure Type BOTH
InChI Key POOZGSRLIRHTHZ-XSLAGTTESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

497.6
MW (Da)
1.62
ALogP
8
HBA
1
HBD
131.3
PSA (Ų)
0.29
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H39N3O8
MW 497.59
Aromatic Rings 0
Heavy Atoms 35
NP-Likeness -0.47

Activity Summary

Ki 1 meas. best 5.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rhodesain
CHEMBL4188
Ki 5.51 5.51 3100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rhodesain Ki = 3100.0 nM 5.51 Inhibition of Trypanosoma brucei rhodesiense rhodesain 16516467

Literature References

PubMed DOI Target Context # Activities
16516467 10.1016/j.bmcl.2006.02.026 Rhodesain 1
16516467 10.1016/j.bmcl.2006.02.026 Trypanosoma brucei brucei 1
16516467 10.1016/j.bmcl.2006.02.026 J774 1

Data from ChEMBL 36 via Core Engine