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Compound Detail

CHEMBL1086435

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CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)/C=C/C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(N)=O)C(C)C

Basic Information

ChEMBL ID CHEMBL1086435
Phase Preclinical
Structure Type MOL
InChI Key PBNMBULNRARQKS-ACHRGXQGSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

772.9
MW (Da)
-1.22
ALogP
9
HBA
9
HBD
284.1
PSA (Ų)
0.06
QED
2
Ro5 Violations
23
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H56N8O10
MW 772.90
Aromatic Rings 1
Heavy Atoms 55
NP-Likeness -0.26

Activity Summary

Ki 2 meas. best 6.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rhodesain
CHEMBL4188
Ki 6.0 6.0 1000.0 1
Procathepsin L
CHEMBL2113
Ki 4.51 4.51 30700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Rhodesain Ki = 1000.0 nM 6.0 Inhibition of Trypanosoma brucei rhodesiense recombinant rhodesain 19715342
Procathepsin L Ki = 30700.0 nM 4.51 Inhibition of bovine spleen cathepsin L 19715342

Literature References

PubMed DOI Target Context # Activities
19715342 10.1021/jm900629w Unchecked 3
19715342 10.1021/jm900629w Rhodesain 3
19715342 10.1021/jm900629w Cathepsin B 2
19715342 10.1021/jm900629w Trypanosoma brucei brucei 1
19715342 10.1021/jm900629w Procathepsin L 1
19715342 10.1021/jm900629w Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine