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Compound Detail

CHEMBL223862

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O=C(COc1ccc(C23CC4CC(CC(C4)C2)C3)cc1)Nc1cc(C(=O)O)ccc1O

Basic Information

ChEMBL ID CHEMBL223862
Phase Preclinical
Structure Type MOL
InChI Key LTJZINXKULUVGF-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

421.5
MW (Da)
4.58
ALogP
4
HBA
3
HBD
95.9
PSA (Ų)
0.59
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27NO5
MW 421.49
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.72

Activity Summary

IC50 3 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
AGS
CHEMBL613860
IC50 6.46 6.46 350.0 1
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha
CHEMBL2221345
IC50 6.4 6.4 400.0 1
Hypoxia-inducible factor 1-alpha
CHEMBL4261
IC50 5.51 5.51 3100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17328532 10.1021/jm0610292 Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha 1
17328532 10.1021/jm0610292 AGS 1
17328532 10.1021/jm0610292 Hypoxia-inducible factor 1-alpha 1
20083404 10.1016/j.bmcl.2009.12.037 Hypoxia-inducible factor 1-alpha 1
20083404 10.1016/j.bmcl.2009.12.037 HeLa 1

Data from ChEMBL 36 via Core Engine