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Compound Detail

CHEMBL4281179

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Cc1cc(Oc2nc(O[C@@H](C(=O)O)C(C)(C)C)c(F)cc2F)cc(-c2cccc(CN)c2)c1

Basic Information

ChEMBL ID CHEMBL4281179
Phase Preclinical
Structure Type MOL
InChI Key IBHLYVDUKHZEBW-NRFANRHFSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

456.5
MW (Da)
5.46
ALogP
5
HBA
2
HBD
94.7
PSA (Ų)
0.49
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26F2N2O4
MW 456.49
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.50

Activity Summary

IC50 3 meas. best 7.29

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL3286
IC50 7.29 7.29 51.0 1
Tissue-type plasminogen activator
CHEMBL1873
IC50 6.33 6.33 470.0 1
Plasminogen
CHEMBL1801
IC50 5.72 5.72 1900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Urokinase-type plasminogen activator IC50 = 51.0 nM 7.29 Inhibition of human uPA 30201291
Tissue-type plasminogen activator IC50 = 470.0 nM 6.33 Inhibition of human tPA 30201291
Plasminogen IC50 = 1900.0 nM 5.72 Inhibition of human plasmin 30201291

Literature References

PubMed DOI Target Context # Activities
30201291 10.1016/j.bmcl.2018.09.001 Urokinase-type plasminogen activator 1
30201291 10.1016/j.bmcl.2018.09.001 Tissue-type plasminogen activator 1
30201291 10.1016/j.bmcl.2018.09.001 Plasminogen 1

Data from ChEMBL 36 via Core Engine