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Compound Detail

CHEMBL487437

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

Basic Information

ChEMBL ID CHEMBL487437
Phase Preclinical
Structure Type MOL
InChI Key SJWFXKQCFFKYPP-LBPRGKRZSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

359.5
MW (Da)
1.97
ALogP
5
HBA
5
HBD
122.3
PSA (Ų)
0.54
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 C17H21N5O2S
MW 359.46
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.03

Activity Summary

EC50 1 meas. best 6.04
IC50 1 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.89 7.89 13.0 1
HT-29
CHEMBL384
EC50 6.04 6.04 920.0 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