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Compound Detail

CHEMBL410195

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COc1cc2c(cc1O)Nc1cc(-c3ccc([N+](=O)[O-])c(OC)c3)ccc1C(=O)N2

Basic Information

ChEMBL ID CHEMBL410195
Phase Preclinical
Structure Type MOL
InChI Key RWGPRVWPJKEHLU-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

407.4
MW (Da)
4.29
ALogP
7
HBA
3
HBD
123.0
PSA (Ų)
0.33
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 C21H17N3O6
MW 407.38
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.20

Activity Summary

EC50 1 meas. best 7.16
IC50 1 meas. best 9.05

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 9.05 9.05 0.9 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
EC50 7.16 7.16 70.0 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