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Compound Detail

CHEMBL518484

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NC(=O)c1cccc2[nH]c(C3CCN(S(=O)(=O)c4ccccc4)CC3)nc12

Basic Information

ChEMBL ID CHEMBL518484
Phase Preclinical
Structure Type MOL
InChI Key LWYGAYYSBCIGHJ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

384.5
MW (Da)
2.23
ALogP
4
HBA
2
HBD
109.2
PSA (Ų)
0.72
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 C19H20N4O3S
MW 384.46
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -1.52

Activity Summary

Ki 2 meas. best 7.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 2
CHEMBL5366
Ki 7.62 7.62 24.0 1
Poly [ADP-ribose] polymerase 1
CHEMBL3105
Ki 7.57 7.57 27.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 2 Ki = 24.0 nM 7.62 Inhibition of PARP2 18541433
Poly [ADP-ribose] polymerase 1 Ki = 27.0 nM 7.57 Inhibition of PARP1 18541433

Literature References

PubMed DOI Target Context # Activities
18541433 10.1016/j.bmc.2008.05.044 Poly [ADP-ribose] polymerase 1 2
18541433 10.1016/j.bmc.2008.05.044 Poly [ADP-ribose] polymerase 2 1

Data from ChEMBL 36 via Core Engine