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Compound Detail

CHEMBL431151

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COc1cc2c(c(OC)c1OC)-c1ccc(SC)c(=O)cc1[C@@H](COC(=O)c1cccc(F)c1)C2

Basic Information

ChEMBL ID CHEMBL431151
Phase Preclinical
Structure Type MOL
InChI Key WXBUOQLKAHEQNX-QGZVFWFLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

496.6
MW (Da)
5.10
ALogP
7
HBA
0
HBD
71.1
PSA (Ų)
0.33
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H25FO6S
MW 496.56
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness 0.32

Activity Summary

IC50 1 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tubulin alpha chain
CHEMBL3658
IC50 5.47 5.47 3388.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tubulin alpha chain IC50 = 3388.44 nM 5.47 Inhibition of tubulin polymerization interacting at the colchicine binding site. 10649972

Literature References

PubMed DOI Target Context # Activities
8496935 10.1021/jm00057a004 Tubulin 2
10649972 10.1021/jm990333a Tubulin alpha chain 1
8496935 10.1021/jm00057a004 KB 1
8496935 10.1021/jm00057a004 A549 1
8496935 10.1021/jm00057a004 HCT-8 1
8496935 10.1021/jm00057a004 P388 1
8496935 10.1021/jm00057a004 RPMI-7951 1
8496935 10.1021/jm00057a004 TE-671 1
8496935 10.1021/jm00057a004 Tubulin beta chain 1

Data from ChEMBL 36 via Core Engine