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Compound Detail

CHEMBL1165777

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COc1cc2c(cc1OC)C(=O)N1C=C(c3ccc4ncccc4c3)C[C@H]1C=N2

Basic Information

ChEMBL ID CHEMBL1165777
Phase Preclinical
Structure Type MOL
InChI Key IWVNYWQNPQXEPO-KRWDZBQOSA-N
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

385.4
MW (Da)
4.22
ALogP
5
HBA
0
HBD
64.0
PSA (Ų)
0.68
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H19N3O3
MW 385.42
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness 0.19

Activity Summary

IC50 3 meas. best 9.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NCI-H460
CHEMBL396
IC50 9.27 9.19 0.5 2
K562
CHEMBL385
IC50 8.85 8.85 1.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20218628 10.1021/jm901722v NON-PROTEIN TARGET 3
20218628 10.1021/jm901722v Calf thymus DNA 2
29079474 10.1016/j.bmcl.2017.10.023 NCI-H460 2
20218628 10.1021/jm901722v K562 1
20218628 10.1021/jm901722v HCT-116 1
20218628 10.1021/jm901722v Mus musculus 1
29079474 10.1016/j.bmcl.2017.10.023 No relevant target 1
29079474 10.1016/j.bmcl.2017.10.023 Unchecked 1

Data from ChEMBL 36 via Core Engine