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Compound Detail

CHEMBL3288914

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CC(C)Oc1cc(NC(=N)c2cnccn2)ccc1-c1ccc(-c2ccc(NC(=N)c3cnccn3)cc2OC(C)C)o1.Cl

Basic Information

ChEMBL ID CHEMBL3288914
Phase Preclinical
Structure Type MOL
InChI Key BNTOPBPKAKUGQM-UHFFFAOYSA-N
Parent Compound CHEMBL1814117
Active Moiety CHEMBL1814117
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

576.7
MW (Da)
6.64
ALogP
9
HBA
4
HBD
154.9
PSA (Ų)
0.11
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H33ClN8O3
MW 613.12
Aromatic Rings 5
Heavy Atoms 43
NP-Likeness -0.60

Activity Summary

IC50 4 meas. best 6.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.26 6.26 552.0 1
Leishmania amazonensis
CHEMBL612877
IC50 5.43 5.43 3700.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 5.09 5.09 8077.0 1
Trypanosoma cruzi
CHEMBL368
IC50 4.8 4.8 16000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24956553 10.1016/j.ejmech.2014.06.022 Unchecked 4
24956553 10.1016/j.ejmech.2014.06.022 L6 1
24956553 10.1016/j.ejmech.2014.06.022 Trypanosoma cruzi 1
24956553 10.1016/j.ejmech.2014.06.022 Leishmania amazonensis 1
24956553 10.1016/j.ejmech.2014.06.022 Trypanosoma brucei rhodesiense 1
24956553 10.1016/j.ejmech.2014.06.022 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine