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Compound Detail

CHEMBL454986

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CO[C@]12C=C(c3c4[nH]c5ccccc5c4cc[n+]3C)C3CCN(CCCC/C=C\CC1)C[C@@]31C[C@@H]3/C=C\CCCCN3[C@H]12.O=S(=O)([O-])C(F)(F)F

Basic Information

ChEMBL ID CHEMBL454986
Phase Preclinical
Structure Type MOL
InChI Key DVCVOOFKOUGDFE-FRNSZEQHSA-N
Parent Compound CHEMBL1186229
Active Moiety CHEMBL1186229
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

577.8
MW (Da)
6.94
ALogP
3
HBA
1
HBD
35.4
PSA (Ų)
0.26
QED
2
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H49F3N4O4S
MW 726.91
Aromatic Rings 3
Heavy Atoms 43
NP-Likeness 1.90

Activity Summary

IC50 1 meas. best 4.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cryptococcus neoformans
CHEMBL365
IC50 4.28 4.28 52000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cryptococcus neoformans IC50 = 52000.0 nM 4.28 Antimicrobial activity against Cryptococcus neoformans ATCC 90113 18595720

Literature References

PubMed DOI Target Context # Activities
18595720 10.1016/j.bmc.2008.05.079 Cryptococcus neoformans 3
18595720 10.1016/j.bmc.2008.05.079 Plasmodium falciparum 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 Staphylococcus aureus 1
18595720 10.1016/j.bmc.2008.05.079 Mycobacterium intracellulare 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