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Compound Detail

CHEMBL4458889

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CNCc1ccc(-c2nc3cncc4c3n2CCNC4=O)cc1

Basic Information

ChEMBL ID CHEMBL4458889
Phase Preclinical
Structure Type MOL
InChI Key WFZXKJNCDQJJDD-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

307.4
MW (Da)
1.56
ALogP
5
HBA
2
HBD
71.8
PSA (Ų)
0.77
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H17N5O
MW 307.36
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.53

Activity Summary

IC50 3 meas. best 8.14
EC50 2 meas. best 4.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 2
CHEMBL5366
IC50 8.14 8.14 7.2 1
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 7.89 7.89 13.0 2
MDA-MB-468
CHEMBL614335
EC50 4.09 4.09 81400.0 1
SW-620
CHEMBL612262
EC50 4.05 4.05 89000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27561983 10.1016/j.bmc.2016.08.016 Poly [ADP-ribose] polymerase 1 4
27561983 10.1016/j.bmc.2016.08.016 SW-620 2
27561983 10.1016/j.bmc.2016.08.016 MDA-MB-468 2
27561983 10.1016/j.bmc.2016.08.016 Poly [ADP-ribose] polymerase 2 1
36989813 10.1016/j.ejmech.2023.115300 Poly [ADP-ribose] polymerase 1 1

Data from ChEMBL 36 via Core Engine