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Compound Detail

CHEMBL4086748

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COC(=O)CNC(=O)c1cnc2c(SSc3cccc4cc(C(=O)NCC(=O)OC)cnc34)cccc2c1

Basic Information

ChEMBL ID CHEMBL4086748
Phase Preclinical
Structure Type MOL
InChI Key KWDAVAFOLMHSLD-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

550.6
MW (Da)
3.39
ALogP
10
HBA
2
HBD
136.6
PSA (Ų)
0.24
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H22N4O6S2
MW 550.62
Aromatic Rings 4
Heavy Atoms 38
NP-Likeness -0.62

Activity Summary

IC50 1 meas. best 5.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
STAM-binding protein
CHEMBL4105848
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
STAM-binding protein IC50 = 2200.0 nM 5.66 Inhibition of AMSH (unknown origin) using DiUbK63TAMRA as substrate by fluoresce... 28191850

Literature References

PubMed DOI Target Context # Activities
28191850 10.1021/acs.jmedchem.6b01379 26S proteasome non-ATPase regulatory subunit 14 2
28191850 10.1021/acs.jmedchem.6b01379 COP9 signalosome complex subunit 5 1
28191850 10.1021/acs.jmedchem.6b01379 STAM-binding protein 1

Data from ChEMBL 36 via Core Engine