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Compound Detail

CHEMBL404189

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COc1cc2c(cc1OC)Nc1cc(-c3ccc([N+](=O)[O-])c(OC)c3)ccc1C(=O)N2

Basic Information

ChEMBL ID CHEMBL404189
Phase Preclinical
Structure Type MOL
InChI Key RAENNXQWJIKCTR-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

421.4
MW (Da)
4.60
ALogP
7
HBA
2
HBD
112.0
PSA (Ų)
0.46
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 C22H19N3O6
MW 421.41
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.43

Activity Summary

EC50 1 meas. best 6.55
IC50 1 meas. best 9.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 9.22 9.22 0.6 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
EC50 6.55 6.55 280.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18358720 10.1016/j.bmcl.2008.02.080 Serine/threonine-protein kinase Chk1 2
18358720 10.1016/j.bmcl.2008.02.080 HeLa 1
18358720 10.1016/j.bmcl.2008.02.080 Molecular identity unknown 1

Data from ChEMBL 36 via Core Engine