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Compound Detail

CHEMBL3814528

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CN(C)CCCn1cnc(NC(=O)c2cc(NC(=O)c3cc(NC(=O)c4cc5ccccc5cn4)cn3C)cn2C)c1.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL3814528
Phase Preclinical
Structure Type MOL
InChI Key CZAHTKMXGGUINR-UHFFFAOYSA-N
Parent Compound CHEMBL235085
Active Moiety CHEMBL235085
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

567.6
MW (Da)
3.82
ALogP
9
HBA
3
HBD
131.1
PSA (Ų)
0.24
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 C32H34F3N9O5
MW 681.68
Aromatic Rings 5
Heavy Atoms 42
NP-Likeness -0.98

Activity Summary

IC50 2 meas. best 5.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 5.35 5.305 4479.0 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
27212070 10.1016/j.bmcl.2016.05.039 HEK293 1
- 10.6019/CHEMBL4513139 Candida albicans 1
- 10.6019/CHEMBL4513139 Cryptococcus neoformans 1
- 10.6019/CHEMBL4513139 Escherichia coli 1
- 10.6019/CHEMBL4513139 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513139 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4513139 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513139 Staphylococcus aureus 1
- 10.6019/CHEMBL4513139 HEK293 1

Data from ChEMBL 36 via Core Engine