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Compound Detail

CHEMBL5420139

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O=C(O)CNC(=O)c1ncc(C2CCN(C(=O)c3ccc(OC(F)(F)F)cc3)CC2)cc1O

Basic Information

ChEMBL ID CHEMBL5420139
Phase Preclinical
Structure Type MOL
InChI Key OFROEPBCNLRELG-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

467.4
MW (Da)
2.52
ALogP
6
HBA
3
HBD
129.1
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H20F3N3O6
MW 467.40
Aromatic Rings 2
Heavy Atoms 33
NP-Likeness -0.93

Activity Summary

IC50 1 meas. best 7.61

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Egl nine homolog 1
CHEMBL5697
IC50 7.61 7.61 24.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Egl nine homolog 1 IC50 = 24.63 nM 7.61 Binding affinity to full length PHD2 (181 to 426 residues) (unknown origin) by f... 37367818

Literature References

PubMed DOI Target Context # Activities
37367818 10.1021/acs.jmedchem.3c00231 Unchecked 5
37367818 10.1021/acs.jmedchem.3c00231 Egl nine homolog 1 1
37367818 10.1021/acs.jmedchem.3c00231 Hep 3B2 1
37367818 10.1021/acs.jmedchem.3c00231 Hypoxia-inducible factor 1-alpha 1
37367818 10.1021/acs.jmedchem.3c00231 Endothelial PAS domain-containing protein 1 1

Data from ChEMBL 36 via Core Engine