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Compound Detail

CHEMBL509890

MAKALUVAMINE F
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O=C1C(NC2Cc3cc(Br)c(O)cc3S2)=CC2=NCCc3c[nH]c1c32

Basic Information

ChEMBL ID CHEMBL509890
Name MAKALUVAMINE F
Phase Preclinical
Structure Type MOL
InChI Key ZEIRCDSUNJVVPP-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

416.3
MW (Da)
3.17
ALogP
5
HBA
3
HBD
77.5
PSA (Ų)
0.70
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C18H14BrN3O2S
MW 416.30
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 1.82

Activity Summary

IC50 5 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
XRS6
CHEMBL614060
IC50 7.1 7.1 80.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.14 5.14 7200.0 1
Hypoxia-inducible factor 1-alpha
CHEMBL4261
IC50 5.08 5.08 8300.0 1
K562
CHEMBL385
IC50 5.05 5.05 8900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27140429 10.1021/acs.jnatprod.5b00846 Hypoxia-inducible factor 1-alpha 6
27140429 10.1021/acs.jnatprod.5b00846 NON-PROTEIN TARGET 3
8691207 10.1021/np50126a008 HCT-116 1
8691207 10.1021/np50126a008 DNA topoisomerase 2-alpha 1
20055495 10.1021/np9005629 K562 1
20055495 10.1021/np9005629 Salmonella enterica 1
20055495 10.1021/np9005629 Proteus vulgaris 1
20055495 10.1021/np9005629 Escherichia coli 1
20055495 10.1021/np9005629 Staphylococcus aureus 1
20055495 10.1021/np9005629 Micrococcus luteus 1
20055495 10.1021/np9005629 Bacillus subtilis 1
20055495 10.1021/np9005629 Sortase A 1
22686608 10.1021/jm3002795 DNA topoisomerase 2-alpha 1
22686608 10.1021/jm3002795 HCT-116 1
22686608 10.1021/jm3002795 XRS6 1

Data from ChEMBL 36 via Core Engine