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Compound Detail

CHEMBL4172435

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Fc1cccc(COc2ccc(Nc3ncnc4ccc(-n5nncc5CN5CCOCC5)cc34)cc2Cl)c1

Basic Information

ChEMBL ID CHEMBL4172435
Phase Preclinical
Structure Type MOL
InChI Key IBSHTZPVQHNLTI-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

546.0
MW (Da)
5.16
ALogP
9
HBA
1
HBD
90.2
PSA (Ų)
0.29
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25ClFN7O2
MW 546.01
Aromatic Rings 5
Heavy Atoms 39
NP-Likeness -2.02

Activity Summary

EC50 6 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei brucei
CHEMBL612851
EC50 6.21 6.21 610.0 1
Leishmania major
CHEMBL612879
EC50 5.79 5.495 1630.0 2
Plasmodium falciparum
CHEMBL364
EC50 5.22 5.04 6050.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29049963 10.1016/j.ejmech.2017.10.007 Plasmodium falciparum 3
29049963 10.1016/j.ejmech.2017.10.007 Trypanosoma brucei brucei 2
29049963 10.1016/j.ejmech.2017.10.007 Trypanosoma cruzi 2
29049963 10.1016/j.ejmech.2017.10.007 Leishmania major 2
29049963 10.1016/j.ejmech.2017.10.007 No relevant target 1
29049963 10.1016/j.ejmech.2017.10.007 HepG2 1
29049963 10.1016/j.ejmech.2017.10.007 NIH3T3 1

Data from ChEMBL 36 via Core Engine