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Compound Detail

CHEMBL510733

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Nc1ncnc2c1ncn2[C@@H]1O[C@H](COC(=O)N2CCN(CC(=O)Nc3cccc4c3CNC4=O)CC2)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL510733
Phase Preclinical
Structure Type MOL
InChI Key XOPDCDNHUYDKRE-UFRIGAJXSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

567.6
MW (Da)
-1.34
ALogP
13
HBA
5
HBD
210.3
PSA (Ų)
0.23
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N9O7
MW 567.56
Aromatic Rings 3
Heavy Atoms 41
NP-Likeness -0.23

Activity Summary

IC50 1 meas. best 7.35

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 7.35 7.35 45.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 1 IC50 = 45.0 nM 7.35 Inhibition of human recombinant PARP1 19125579

Literature References

PubMed DOI Target Context # Activities
19125579 10.1021/jm800902t Poly [ADP-ribose] polymerase 1 1

Data from ChEMBL 36 via Core Engine