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Compound Detail

CHEMBL500157

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Nc1nccc(Oc2ccc(NC(=O)NC(=O)Cc3ccc(F)cc3)cc2F)c1C#CCO

Basic Information

ChEMBL ID CHEMBL500157
Phase Preclinical
Structure Type MOL
InChI Key HGHDKUIVPHCCKQ-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

452.4
MW (Da)
2.97
ALogP
6
HBA
4
HBD
126.6
PSA (Ų)
0.44
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H18F2N4O4
MW 452.42
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.29

Activity Summary

IC50 4 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
IC50 8.52 8.52 3.0 2
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.52 7.52 30.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 6.16 6.16 700.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18479916 10.1016/j.bmcl.2008.04.047 Hepatocyte growth factor receptor 1
18479916 10.1016/j.bmcl.2008.04.047 NON-PROTEIN TARGET 1
18479916 10.1016/j.bmcl.2008.04.047 Cytochrome P450 3A4 1
21641696 10.1016/j.ejmech.2011.05.031 Hepatocyte growth factor receptor 1

Data from ChEMBL 36 via Core Engine