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Compound Detail

CHEMBL2178399

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O=C(/C=C/Oc1ccc(C23CC4CC(CC(C4)C2)C3)cc1)Nc1cccc(C(=O)OCCN2CCOCC2)c1

Basic Information

ChEMBL ID CHEMBL2178399
Phase Preclinical
Structure Type MOL
InChI Key KNKKZWPDCMPLGC-XYOKQWHBSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

530.7
MW (Da)
5.17
ALogP
6
HBA
1
HBD
77.1
PSA (Ų)
0.27
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H38N2O5
MW 530.67
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness -0.81

Activity Summary

IC50 1 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hypoxia-inducible factor 1-alpha
CHEMBL4261
IC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23153200 10.1021/jm301419d Hypoxia-inducible factor 1-alpha 8
23153200 10.1021/jm301419d HCT-116 5
23153200 10.1021/jm301419d No relevant target 3
23153200 10.1021/jm301419d HUVEC 2
23153200 10.1021/jm301419d PC-3 1
23153200 10.1021/jm301419d HeLa 1
23153200 10.1021/jm301419d A549 1
23153200 10.1021/jm301419d LoVo 1

Data from ChEMBL 36 via Core Engine