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Compound Detail

CHEMBL183569

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COc1cc2c(c(OC)c1OC(=O)CN(C)C)-c1ccc(OC)c(=O)cc1[C@@H](NC(C)=O)CC2

Basic Information

ChEMBL ID CHEMBL183569
Phase Preclinical
Structure Type MOL
InChI Key VGXCCIPNOCCGGN-SFHVURJKSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

470.5
MW (Da)
2.33
ALogP
8
HBA
1
HBD
103.4
PSA (Ų)
0.49
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30N2O7
MW 470.52
Aromatic Rings 2
Heavy Atoms 34
NP-Likeness 0.57

Activity Summary

IC50 1 meas. best 4.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin beta-1 chain
CHEMBL1915
IC50 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tubulin beta-1 chain IC50 = 15000.0 nM 4.82 Inhibitory concentration against tubulin assembly 15582446

Literature References

PubMed DOI Target Context # Activities
15582446 10.1016/j.bmcl.2004.07.098 ADMET 2
15582446 10.1016/j.bmcl.2004.07.098 KB 1
15582446 10.1016/j.bmcl.2004.07.098 KB 3-1 1
15582446 10.1016/j.bmcl.2004.07.098 Tubulin beta-1 chain 1

Data from ChEMBL 36 via Core Engine