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Compound Detail

CHEMBL4174815

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Cl.O=C(O)CNC(=O)c1c(O)ccn2ncnc12

Basic Information

ChEMBL ID CHEMBL4174815
Phase Preclinical
Structure Type MOL
InChI Key PUHKYYMZSXZVPU-UHFFFAOYSA-N
Parent Compound CHEMBL4302712
Active Moiety CHEMBL4302712
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

236.2
MW (Da)
-0.75
ALogP
6
HBA
3
HBD
116.8
PSA (Ų)
0.65
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C9H9ClN4O4
MW 272.65
Aromatic Rings 2
Heavy Atoms 17
NP-Likeness -1.15

Activity Summary

IC50 1 meas. best 6.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Egl nine homolog 1
CHEMBL5697
IC50 6.09 6.09 820.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Egl nine homolog 1 IC50 = 820.0 nM 6.09 Inhibition of human HIF-PHD2 assessed as reduction in HIF1-alpha binding to VBC ... 29259755

Literature References

PubMed DOI Target Context # Activities
29259755 10.1021/acsmedchemlett.7b00404 Egl nine homolog 1 2
29259755 10.1021/acsmedchemlett.7b00404 ADMET 1

Data from ChEMBL 36 via Core Engine