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Compound Detail

CHEMBL570142

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COc1cc2c(c(OC)c1OC)-c1ccc(SC)c(=O)cc1[C@@H](NC(=O)CCCSSCCCC(=O)N[C@H]1CCc3cc(OC)c(OC)c(OC)c3-c3ccc(SC)c(=O)cc31)CC2

Basic Information

ChEMBL ID CHEMBL570142
Phase Preclinical
Structure Type MOL
InChI Key RXXRGSGBOSQLHA-HEVIKAOCSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

949.2
MW (Da)
9.09
ALogP
14
HBA
2
HBD
147.7
PSA (Ų)
0.05
QED
3
Ro5 Violations
19
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H56N2O10S4
MW 949.25
Aromatic Rings 4
Heavy Atoms 64
NP-Likeness 0.18

Activity Summary

IC50 1 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
IGROV-1
CHEMBL613984
IC50 7.3 7.3 50.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
IGROV-1 IC50 = 50.0 nM 7.3 Antiproliferative activity against human IGROV1 cells assessed as growth inhibit... 19833515

Literature References

PubMed DOI Target Context # Activities
19833515 10.1016/j.bmcl.2009.09.075 IGROV-1 1
19833515 10.1016/j.bmcl.2009.09.075 Histone deacetylase 1 1
19833515 10.1016/j.bmcl.2009.09.075 Histone deacetylase 6 1

Data from ChEMBL 36 via Core Engine