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Compound Detail

CHEMBL2012855

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CN(C)CCC(=O)Nc1cc2n[nH]c(=O)n2c2cc(-c3ccsc3)ccc12

Basic Information

ChEMBL ID CHEMBL2012855
Phase Preclinical
Structure Type MOL
InChI Key RISGDPZHROSWOU-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

381.5
MW (Da)
2.79
ALogP
6
HBA
2
HBD
82.5
PSA (Ų)
0.56
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 C19H19N5O2S
MW 381.46
Aromatic Rings 4
Heavy Atoms 27
NP-Likeness -1.86

Activity Summary

EC50 1 meas. best 5.89
IC50 1 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.4 7.4 40.0 1
HT-29
CHEMBL384
EC50 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22342147 10.1016/j.bmcl.2012.01.043 Serine/threonine-protein kinase Chk1 1
22342147 10.1016/j.bmcl.2012.01.043 HT-29 1
22342147 10.1016/j.bmcl.2012.01.043 No relevant target 1

Data from ChEMBL 36 via Core Engine