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Compound Detail

CHEMBL221560

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O=C(COc1ccc(C23CC4CC(CC(C4)C2)C3)cc1)Nc1cccc(C(=O)Nc2ccc(Cl)cc2)c1

Basic Information

ChEMBL ID CHEMBL221560
Phase Preclinical
Structure Type MOL
InChI Key INFZJTTXUMJLDY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

515.0
MW (Da)
7.08
ALogP
3
HBA
2
HBD
67.4
PSA (Ų)
0.35
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H31ClN2O3
MW 515.05
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.32

Activity Summary

IC50 1 meas. best 5.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
AGS
CHEMBL613860
IC50 5.02 5.02 9500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
AGS IC50 = 9500.0 nM 5.02 Inhibition of hypoxia induced HIF1 transcriptional activity in human AGS cells b... 17328532

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

Data from ChEMBL 36 via Core Engine