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Compound Detail

CHEMBL476124

CYCLAPOLIN 9
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NC(=O)c1sc2c([N+](=O)[O-])cc(C(F)(F)F)cc2[n+]1[O-]

Basic Information

ChEMBL ID CHEMBL476124
Name CYCLAPOLIN 9
Phase Preclinical
Structure Type MOL
InChI Key FHFLXKUKCSDMLD-UHFFFAOYSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

307.2
MW (Da)
1.56
ALogP
5
HBA
1
HBD
113.2
PSA (Ų)
0.39
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H4F3N3O4S
MW 307.21
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -1.00

Activity Summary

IC50 5 meas. best 6.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase PLK1
CHEMBL3024
IC50 6.3 5.96 500.0 2
HeLa
CHEMBL399
IC50 5.18 5.18 6600.0 1
HT-29
CHEMBL384
IC50 5.11 5.11 7700.0 1
A549
CHEMBL392
IC50 4.61 4.61 24800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17028581 10.1038/nchembio825 Unchecked 6
34046598 10.1039/d0md00390e Mycobacterium tuberculosis 2
17028581 10.1038/nchembio825 Cyclin-dependent kinase 2/cyclin E1 2
17028581 10.1038/nchembio825 Tyrosine-protein kinase CSK 1
17028581 10.1038/nchembio825 Dual specificity mitogen-activated protein kinase kinase 6 1
17028581 10.1038/nchembio825 Dual specificity mitogen-activated protein kinase kinase 1 1
17028581 10.1038/nchembio825 MAP kinase-activated protein kinase 2 1
17028581 10.1038/nchembio825 Mitogen-activated protein kinase 9 1
17028581 10.1038/nchembio825 Insulin receptor 1
17028581 10.1038/nchembio825 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
17028581 10.1038/nchembio825 Insulin-like growth factor 1 receptor 1
17028581 10.1038/nchembio825 Fibroblast growth factor receptor 3 1
18762425 10.1016/j.bmcl.2008.08.033 Serine/threonine-protein kinase PLK1 1
17028581 10.1038/nchembio825 Serine/threonine-protein kinase Chk2 1
17028581 10.1038/nchembio825 Serine/threonine-protein kinase Chk1 1
17028581 10.1038/nchembio825 RAF proto-oncogene serine/threonine-protein kinase 1
17028581 10.1038/nchembio825 HT-29 1
17028581 10.1038/nchembio825 HeLa 1
17028581 10.1038/nchembio825 A549 1
17028581 10.1038/nchembio825 Serine/threonine-protein kinase PLK1 1

Data from ChEMBL 36 via Core Engine