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Compound Detail

CHEMBL4648197

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CCOC(=O)Cn1nnc(-c2cc(C(C)C)c(O)cc2O)c1-c1ccc(S(C)(=O)=O)cc1

Basic Information

ChEMBL ID CHEMBL4648197
Phase Preclinical
Structure Type MOL
InChI Key HWEPYGBSGLNFBC-UHFFFAOYSA-N
5
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

459.5
MW (Da)
3.11
ALogP
9
HBA
2
HBD
131.6
PSA (Ų)
0.52
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N3O6S
MW 459.52
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.80

Activity Summary

IC50 5 meas. best 7.38

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heat shock protein HSP 90-alpha
CHEMBL3880
IC50 7.38 7.38 41.8 1
Endoplasmin
CHEMBL1075323
IC50 7.0 7.0 100.5 1
PC-3
CHEMBL390
IC50 6.49 6.49 323.7 1
HeLa
CHEMBL399
IC50 6.4 6.4 402.0 1
Heat shock protein 75 kDa, mitochondrial
CHEMBL1075132
IC50 4.8 4.8 16014.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31839539 10.1016/j.bmcl.2019.126809 Heat shock protein HSP90 6
31839539 10.1016/j.bmcl.2019.126809 Unchecked 2
31839539 10.1016/j.bmcl.2019.126809 Heat shock protein HSP 90-alpha 1
31839539 10.1016/j.bmcl.2019.126809 Heat shock protein 75 kDa, mitochondrial 1
31839539 10.1016/j.bmcl.2019.126809 Endoplasmin 1
31839539 10.1016/j.bmcl.2019.126809 HeLa 1
31839539 10.1016/j.bmcl.2019.126809 PC-3 1

Data from ChEMBL 36 via Core Engine