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Compound Detail

CHEMBL3797456

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Cn1cc(NC(=O)c2cc(NC(=O)c3ccc(/C=C/c4ccc5nsnc5c4)cc3)cn2C)cc1C(=O)NCCN1CCOCC1

Basic Information

ChEMBL ID CHEMBL3797456
Phase Preclinical
Structure Type MOL
InChI Key KZUQRLRBWCMFPO-ONEGZZNKSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

638.8
MW (Da)
4.11
ALogP
10
HBA
3
HBD
135.4
PSA (Ų)
0.20
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C33H34N8O4S
MW 638.75
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.24

Activity Summary

IC50 3 meas. best 8.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
IC50 8.14 8.14 7.3 1
Plasmodium falciparum
CHEMBL364
IC50 5.29 5.255 5144.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27212070 10.1016/j.bmcl.2016.05.039 Plasmodium falciparum 2
27060763 10.1016/j.ejmech.2016.03.064 HEK293 1
27060763 10.1016/j.ejmech.2016.03.064 Trypanosoma brucei brucei 1
27060763 10.1016/j.ejmech.2016.03.064 Unchecked 1
27212070 10.1016/j.bmcl.2016.05.039 HEK293 1
27349332 10.1016/j.bmcl.2016.06.040 NON-PROTEIN TARGET 1

Data from ChEMBL 36 via Core Engine