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Compound Detail

CHEMBL373396

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COC(=O)c1cccc(NC(=O)COc2ccc(C34CC5CC(CC(C5)C3)C4)cc2)c1

Basic Information

ChEMBL ID CHEMBL373396
Phase Preclinical
Structure Type MOL
InChI Key WOELYKNPIBVROK-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

419.5
MW (Da)
4.96
ALogP
4
HBA
1
HBD
64.6
PSA (Ų)
0.67
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 C26H29NO4
MW 419.52
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.00

Activity Summary

IC50 5 meas. best 6.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hypoxia-inducible factor 1-alpha
CHEMBL4261
IC50 6.16 5.68 700.0 3
AGS
CHEMBL613860
IC50 5.13 5.13 7400.0 1
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha
CHEMBL2221345
IC50 5.0 5.0 9900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17884495 10.1016/j.bmcl.2007.09.005 Hypoxia-inducible factor 1-alpha 2
17328532 10.1021/jm0610292 Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha 1
17328532 10.1021/jm0610292 AGS 1
23153200 10.1021/jm301419d HCT-116 1
23153200 10.1021/jm301419d Hypoxia-inducible factor 1-alpha 1

Data from ChEMBL 36 via Core Engine