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Compound Detail

CHEMBL530354

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Oc1ccc(Nc2nc(NCc3ccccc3)c3ccccc3n2)cc1

Basic Information

ChEMBL ID CHEMBL530354
Phase Preclinical
Structure Type MOL
InChI Key DOCRZTZPMVOAGN-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

342.4
MW (Da)
4.69
ALogP
5
HBA
3
HBD
70.1
PSA (Ų)
0.46
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H18N4O
MW 342.40
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.06

Activity Summary

IC50 2 meas. best 4.75
EC50 1 meas. best 5.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
EC50 5.23 5.23 5900.0 1
Cruzipain
CHEMBL3563
IC50 4.75 4.75 18000.0 1
Rhodesain
CHEMBL4188
IC50 4.64 4.64 23000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34461718 10.1021/acs.jmedchem.1c01151 Cruzipain 6
20485427 10.1038/nature09107 Plasmodium falciparum 4
34461718 10.1021/acs.jmedchem.1c01151 Rhodesain 2
20485427 10.1038/nature09107 HepG2 1
20485427 10.1038/nature09107 Unchecked 1
- 10.6019/CHEMBL3433997 Hexose transporter 1 1
- 10.6019/CHEMBL3433997 Glucose transporter 1
- 10.6019/CHEMBL3433997 Solute carrier family 2, facilitated glucose transporter member 1 1
34461718 10.1021/acs.jmedchem.1c01151 Trypanosoma cruzi 1
34461718 10.1021/acs.jmedchem.1c01151 C2C12 1
34461718 10.1021/acs.jmedchem.1c01151 ADMET 1
34461718 10.1021/acs.jmedchem.1c01151 Trypanosoma brucei brucei 1

Data from ChEMBL 36 via Core Engine