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Compound Detail

CHEMBL2022560

APRATOXIN F
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CC[C@H](C)[C@H]1C(=O)N(C)[C@@H](C)C(=O)O[C@H](C(C)(C)C)C[C@@H](C)C[C@H](O)[C@H](C)C2=N[C@@H](/C=C(\C)C(=O)N[C@@H](Cc3ccc(OC)cc3)C(=O)N(C)[C@@H](C)C(=O)N1C)CS2

Basic Information

ChEMBL ID CHEMBL2022560
Name APRATOXIN F
Phase Preclinical
Structure Type MOL
InChI Key BAYCKSGCVUIVNR-FQASXUTMSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

828.1
MW (Da)
5.13
ALogP
10
HBA
2
HBD
158.2
PSA (Ų)
0.38
QED
2
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C44H69N5O8S
MW 828.13
Aromatic Rings 1
Heavy Atoms 58
NP-Likeness 1.20

Activity Summary

IC50 2 meas. best 9.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 9.34 8.825 0.5 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
HCT-116 IC50 = 0.461 nM 9.34 Inhibition of VEGF-A secretion in human HCT116 cells after 12 hrs 22081789
HCT-116 IC50 = 4.92 nM 8.31 Cytotoxicity against human HCT116 cells after 48 hrs 22081789

Literature References

PubMed DOI Target Context # Activities
22081789 10.1021/ml200176m HCT-116 2
22081789 10.1021/ml200176m Hepatocyte growth factor receptor 1

Data from ChEMBL 36 via Core Engine