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Compound Detail

CHEMBL4636777

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COc1c(O)cc2c3c1C[C@@H](C)C[C@H](OC)[C@H](O3)[C@@H](C)/C=C(\C)[C@H](OC(N)=O)[C@@H](OC)C[C@@H](O)/C=C(\C)C(=O)N2

Basic Information

ChEMBL ID CHEMBL4636777
Phase Preclinical
Structure Type MOL
InChI Key VFUDTWBANAOTEF-YRTOUZEESA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

562.7
MW (Da)
3.46
ALogP
9
HBA
4
HBD
158.8
PSA (Ų)
0.40
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H42N2O9
MW 562.66
Aromatic Rings 1
Heavy Atoms 40
NP-Likeness 2.09

Activity Summary

IC50 1 meas. best 4.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Heat shock protein HSP 90-alpha
CHEMBL3880
IC50 4.02 4.02 96000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Heat shock protein HSP 90-alpha IC50 = 96000.0 nM 4.02 Inhibition of HSP90alpha (unknown origin) 32273216

Literature References

PubMed DOI Target Context # Activities
32273216 10.1016/j.bmcl.2020.127168 Staphylococcus aureus 2
32273216 10.1016/j.bmcl.2020.127168 Bacillus amyloliquefaciens 2
32273216 10.1016/j.bmcl.2020.127168 Shewanella oneidensis 2
32273216 10.1016/j.bmcl.2020.127168 K562 1
32273216 10.1016/j.bmcl.2020.127168 HL-60 1
32273216 10.1016/j.bmcl.2020.127168 A549 1
32273216 10.1016/j.bmcl.2020.127168 MCF7 1
32273216 10.1016/j.bmcl.2020.127168 Heat shock protein HSP 90-alpha 1

Data from ChEMBL 36 via Core Engine