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Compound Detail

CHEMBL2023963

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Nc1ncnc2c1ccn2[C@@H]1O[C@H](CO)C[C@H]1O

Basic Information

ChEMBL ID CHEMBL2023963
Phase Preclinical
Structure Type MOL
InChI Key GAKDEQRUZQIUER-FMTFEUNWSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

250.3
MW (Da)
-0.35
ALogP
7
HBA
3
HBD
106.4
PSA (Ų)
0.67
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H14N4O3
MW 250.26
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness 1.14

Activity Summary

EC50 2 meas. best 9.28
IC50 1 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
EC50 9.28 9.28 0.5 2
Unchecked
CHEMBL612545
IC50 7.1 7.1 80.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22516671 10.1016/j.bmc.2012.03.049 Unchecked 1
33784107 10.1021/acs.jmedchem.1c00135 Trypanosoma brucei rhodesiense 1
33667845 10.1016/j.ejmech.2021.113290 Trypanosoma brucei rhodesiense 1
35144125 10.1016/j.ejmech.2022.114165 MRC5 1
35144125 10.1016/j.ejmech.2022.114165 Trypanosoma cruzi 1
35144125 10.1016/j.ejmech.2022.114165 Leishmania infantum 1
35144125 10.1016/j.ejmech.2022.114165 Macrophage 1

Data from ChEMBL 36 via Core Engine