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Compound Detail

CHEMBL488230

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NC(=O)Nc1sc(-c2cccnc2)cc1C(=O)N[C@H]1CCCNC1

Basic Information

ChEMBL ID CHEMBL488230
Phase Preclinical
Structure Type MOL
InChI Key GCSKSASBAPPULE-NSHDSACASA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

345.4
MW (Da)
1.78
ALogP
5
HBA
4
HBD
109.1
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 C16H19N5O2S
MW 345.43
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.36

Activity Summary

IC50 2 meas. best 8.22
EC50 1 meas. best 6.52

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
HT-29
CHEMBL384
EC50 6.52 6.52 300.0 1
Cyclin-dependent kinase 2-associated protein 1
CHEMBL5578
IC50 5.48 5.48 3300.0 1

Activity Data Samples

Top measurements by pChEMBL value

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

Data from ChEMBL 36 via Core Engine