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Compound Detail

CHEMBL3338019

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COc1nc(Nc2ccc(C#N)cc2)nc(Nc2c(C)cc(C)cc2Br)n1

Basic Information

ChEMBL ID CHEMBL3338019
Phase Preclinical
Structure Type MOL
InChI Key OZMDMKBWNGONNJ-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

425.3
MW (Da)
4.62
ALogP
7
HBA
2
HBD
95.8
PSA (Ų)
0.62
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 C19H17BrN6O
MW 425.29
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.58

Activity Summary

IC50 3 meas. best 4.94
EC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
EC50 8.7 8.7 2.0 1
Plasmodium falciparum
CHEMBL364
IC50 4.94 4.94 11470.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 4.94 4.94 11600.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 4.92 4.92 11970.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
25199582 10.1016/j.bmc.2014.08.005 ADMET 2
25199582 10.1016/j.bmc.2014.08.005 Trypanosoma brucei brucei 1
25199582 10.1016/j.bmc.2014.08.005 Trypanosoma brucei rhodesiense 1
25199582 10.1016/j.bmc.2014.08.005 Human immunodeficiency virus 1 1
25199582 10.1016/j.bmc.2014.08.005 Trypanosoma cruzi 1
25199582 10.1016/j.bmc.2014.08.005 Leishmania infantum 1
25199582 10.1016/j.bmc.2014.08.005 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine