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Compound Detail

CHEMBL4065318

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O=C(Nc1ncco1)c1cnc2c(SSc3cccc4cc(C(=O)Nc5ncco5)cnc34)cccc2c1

Basic Information

ChEMBL ID CHEMBL4065318
Phase Preclinical
Structure Type MOL
InChI Key XABQDVKTPWAYAO-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

540.6
MW (Da)
6.06
ALogP
10
HBA
2
HBD
136.0
PSA (Ų)
0.23
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H16N6O4S2
MW 540.59
Aromatic Rings 6
Heavy Atoms 38
NP-Likeness -0.67

Activity Summary

IC50 3 meas. best 5.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
26S proteasome non-ATPase regulatory subunit 14
CHEMBL2007629
IC50 5.58 5.58 2600.0 1
STAM-binding protein
CHEMBL4105848
IC50 5.3 5.3 5000.0 1
COP9 signalosome complex subunit 5
CHEMBL4105809
IC50 4.82 4.82 15000.0 1

Activity Data Samples

Top measurements by pChEMBL value

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
28191850 10.1021/acs.jmedchem.6b01379 No relevant target 1

Data from ChEMBL 36 via Core Engine