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Compound Detail

CHEMBL443420

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C[n+]1ccc2c([nH]c3ccccc32)c1C1=C[C@@]2(O)CC/C=C\CCCCN3CCC1[C@]1(C[C@@H]4/C=C\CCCCN4[C@H]12)C3.O=S(=O)([O-])C(F)(F)F

Basic Information

ChEMBL ID CHEMBL443420
Phase Preclinical
Structure Type MOL
InChI Key JKGIEXAJEDKIJT-GTWBRYFRSA-N
Parent Compound CHEMBL1185968
Active Moiety CHEMBL1185968
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

563.8
MW (Da)
6.29
ALogP
3
HBA
2
HBD
46.4
PSA (Ų)
0.27
QED
2
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H47F3N4O4S
MW 712.88
Aromatic Rings 3
Heavy Atoms 42
NP-Likeness 2.14

Activity Summary

IC50 5 meas. best 6.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.13 6.065 736.0 2
Mycobacterium intracellulare
CHEMBL612640
IC50 4.75 4.75 17800.0 1
Staphylococcus aureus
CHEMBL352
IC50 4.35 4.35 44500.0 1
Cryptococcus neoformans
CHEMBL365
IC50 4.15 4.15 71100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18595720 10.1016/j.bmc.2008.05.079 Staphylococcus aureus 3
18595720 10.1016/j.bmc.2008.05.079 Mycobacterium intracellulare 3
18595720 10.1016/j.bmc.2008.05.079 Plasmodium falciparum 2
18595720 10.1016/j.bmc.2008.05.079 Unchecked 2
18595720 10.1016/j.bmc.2008.05.079 Cryptococcus neoformans 2
18595720 10.1016/j.bmc.2008.05.079 Hepatitis C virus 2
18595720 10.1016/j.bmc.2008.05.079 Vero 1
18595720 10.1016/j.bmc.2008.05.079 Candida albicans 1
18595720 10.1016/j.bmc.2008.05.079 Escherichia coli 1
18595720 10.1016/j.bmc.2008.05.079 Pseudomonas aeruginosa 1
18595720 10.1016/j.bmc.2008.05.079 Aspergillus fumigatus 1

Data from ChEMBL 36 via Core Engine