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Compound Detail

CHEMBL522733

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COc1ccc(C(c2cc3c(cc2O)OCO3)n2ccnc2)cc1

Basic Information

ChEMBL ID CHEMBL522733
Phase Preclinical
Structure Type MOL
InChI Key SLZWZNUKPMKGCR-UHFFFAOYSA-N
2
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

324.3
MW (Da)
2.96
ALogP
6
HBA
1
HBD
65.7
PSA (Ų)
0.80
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H16N2O4
MW 324.34
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.25

Activity Summary

IC50 2 meas. best 7.26
Ki 1 meas. best 7.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Aromatase
CHEMBL1978
Ki 7.88 7.88 13.1 1
Aromatase
CHEMBL1978
IC50 7.26 7.26 55.0 1
Protein disulfide-isomerase
CHEMBL5422
IC50 6.21 6.21 620.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19072235 10.1021/jm800945c Aromatase 2
32830969 10.1021/acs.jmedchem.0c00728 Protein disulfide-isomerase 1
32830969 10.1021/acs.jmedchem.0c00728 U-87 MG 1

Data from ChEMBL 36 via Core Engine