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Compound Detail

CHEMBL4281574

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CC(C)(C)[C@@H](Oc1nc(Oc2cccc(-c3cccc(CN)c3)c2)c(F)cc1F)C(=O)O

Basic Information

ChEMBL ID CHEMBL4281574
Phase Preclinical
Structure Type MOL
InChI Key OCHYOADZYHAHDM-FQEVSTJZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

442.5
MW (Da)
5.16
ALogP
5
HBA
2
HBD
94.7
PSA (Ų)
0.53
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 C24H24F2N2O4
MW 442.46
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.44

Activity Summary

IC50 3 meas. best 7.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Urokinase-type plasminogen activator
CHEMBL3286
IC50 7.08 7.08 84.0 1
Tissue-type plasminogen activator
CHEMBL1873
IC50 5.84 5.84 1450.0 1
Plasminogen
CHEMBL1801
IC50 5.26 5.26 5450.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Urokinase-type plasminogen activator IC50 = 84.0 nM 7.08 Inhibition of human uPA 30201291
Tissue-type plasminogen activator IC50 = 1450.0 nM 5.84 Inhibition of human tPA 30201291
Plasminogen IC50 = 5450.0 nM 5.26 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