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Compound Detail

CHEMBL3585466

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C[C@@]12C[C@@H]3C(=CC[C@@H]4C(=O)NC(=O)[C@@H]43)[C@H](c3ccc(C(F)(F)F)cc3)[C@]1(C)C(=O)c1ccccc1C2=O

Basic Information

ChEMBL ID CHEMBL3585466
Phase Preclinical
Structure Type MOL
InChI Key DRAKQVLBCKFKNR-INUIQVKHSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

507.5
MW (Da)
5.12
ALogP
4
HBA
1
HBD
80.3
PSA (Ų)
0.43
QED
2
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H24F3NO4
MW 507.51
Aromatic Rings 2
Heavy Atoms 37
NP-Likeness 0.52

Activity Summary

EC50 1 meas. best 5.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hypoxia-inducible factor 1-alpha
CHEMBL4261
EC50 5.11 5.11 7800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hypoxia-inducible factor 1-alpha EC50 = 7800.0 nM 5.11 Inhibition of human HIF1alpha-mediated transcription expressed in human U251 cel... -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00111G Unchecked 1
- 10.1039/C4MD00111G U-251 1
- 10.1039/C4MD00111G Hypoxia-inducible factor 1-alpha 1

Data from ChEMBL 36 via Core Engine