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Compound Detail

CHEMBL4080163

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Cc1cccc2c(=O)[nH]c(CCC(=O)O)nc12

Basic Information

ChEMBL ID CHEMBL4080163
Phase Preclinical
Structure Type MOL
InChI Key OOIMOZIUYZYXLA-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
12
Publications
0
Known Names

Molecular Properties

232.2
MW (Da)
1.25
ALogP
3
HBA
2
HBD
83.0
PSA (Ų)
0.83
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 C12H12N2O3
MW 232.24
Aromatic Rings 2
Heavy Atoms 17
NP-Likeness -1.03

Activity Summary

IC50 4 meas. best 6.84

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 2
CHEMBL5366
IC50 6.84 6.84 144.5 2
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 6.0 5.59 1000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27983846 10.1021/acs.jmedchem.6b01574 Poly [ADP-ribose] polymerase 2 2
27983846 10.1021/acs.jmedchem.6b01574 Poly [ADP-ribose] polymerase 1 2
27983846 10.1021/acs.jmedchem.6b01574 Unchecked 2
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP16 1
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP15 1
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP14 1
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP12 1
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP10 1
27983846 10.1021/acs.jmedchem.6b01574 Poly [ADP-ribose] polymerase tankyrase-2 1
27983846 10.1021/acs.jmedchem.6b01574 Poly [ADP-ribose] polymerase tankyrase-1 1
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP4 1
27983846 10.1021/acs.jmedchem.6b01574 Protein mono-ADP-ribosyltransferase PARP3 1

Data from ChEMBL 36 via Core Engine