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Compound Detail

CHEMBL3109278

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CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C.O=C(O)CC(O)C(=O)O

Basic Information

ChEMBL ID CHEMBL3109278
Phase Preclinical
Structure Type MOL
InChI Key LBWFXVZLPYTWQI-HBPAQXCTSA-N
Parent Compound CHEMBL535
Active Moiety CHEMBL535
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

398.5
MW (Da)
3.33
ALogP
3
HBA
3
HBD
77.2
PSA (Ų)
0.63
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33FN4O7
MW 532.57
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -1.21

Activity Summary

IC50 2 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 7.51 7.51 31.2 1
Bile salt export pump
CHEMBL6020
IC50 4.34 4.34 46000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24368209 10.1016/j.ejmech.2013.11.023 Vascular endothelial growth factor receptor 2 1
23956101 10.1093/toxsci/kft176 Bile salt export pump 1
23956101 10.1093/toxsci/kft176 ATP-binding cassette sub-family C member 2 1
23956101 10.1093/toxsci/kft176 ATP-binding cassette sub-family C member 3 1
23956101 10.1093/toxsci/kft176 ATP-binding cassette sub-family C member 4 1

Data from ChEMBL 36 via Core Engine