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Compound Detail

CHEMBL488835

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NC(=O)Nc1sc(-c2ccc(C(=O)N3CCOCC3)cc2)cc1C(=O)N[C@H]1CCCNC1

Basic Information

ChEMBL ID CHEMBL488835
Phase Preclinical
Structure Type MOL
InChI Key VNGCBJHJMMHMOG-INIZCTEOSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

457.6
MW (Da)
1.86
ALogP
6
HBA
4
HBD
125.8
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H27N5O4S
MW 457.56
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -1.47

Activity Summary

EC50 1 meas. best 6.21
IC50 1 meas. best 8.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 8.0 8.0 10.0 1
HT-29
CHEMBL384
EC50 6.21 6.21 610.0 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

Data from ChEMBL 36 via Core Engine