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Compound Detail

CHEMBL520734

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NC(=O)Nc1sc(-c2ccsc2)cc1C(=O)N[C@H]1CCCNC1

Basic Information

ChEMBL ID CHEMBL520734
Phase Preclinical
Structure Type MOL
InChI Key PBCBIZJDVCDFNU-JTQLQIEISA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

350.5
MW (Da)
2.45
ALogP
5
HBA
4
HBD
96.2
PSA (Ų)
0.68
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H18N4O2S2
MW 350.47
Aromatic Rings 2
Heavy Atoms 23
NP-Likeness -1.73

Activity Summary

IC50 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 8.22 8.22 6.0 1
Cyclin-dependent kinase 2-associated protein 1
CHEMBL5578
IC50 5.28 5.28 5300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 IC50 = 6.0 nM 8.22 Inhibition of Chk1 18547806
Cyclin-dependent kinase 2-associated protein 1 IC50 = 5300.0 nM 5.28 Inhibition of Cdk1 18547806

Literature References

PubMed DOI Target Context # Activities
18547806 10.1016/j.bmcl.2008.05.016 HT-29 1
18547806 10.1016/j.bmcl.2008.05.016 Serine/threonine-protein kinase Chk1 1
18547806 10.1016/j.bmcl.2008.05.016 Cyclin-dependent kinase 2-associated protein 1 1
18547806 10.1016/j.bmcl.2008.05.016 Unchecked 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine