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Compound Detail

CHEMBL460260

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CN(C)S(=O)(=O)N1CCC(c2nc3c(C(N)=O)cccc3[nH]2)CC1

Basic Information

ChEMBL ID CHEMBL460260
Phase Preclinical
Structure Type MOL
InChI Key YKVNCVKRDCRGHE-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
0.65
ALogP
4
HBA
2
HBD
112.4
PSA (Ų)
0.84
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 C15H21N5O3S
MW 351.43
Aromatic Rings 2
Heavy Atoms 24
NP-Likeness -1.45

Activity Summary

EC50 1 meas. best 6.77
Ki 1 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 1
CHEMBL3105
Ki 7.55 7.55 28.0 1
Poly [ADP-ribose] polymerase 1
CHEMBL3105
EC50 6.77 6.77 170.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 1 Ki = 28.0 nM 7.55 Inhibition of PARP1 18541433
Poly [ADP-ribose] polymerase 1 EC50 = 170.0 nM 6.77 Inhibition of PARP1 in human C41 cells 18541433

Literature References

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

Data from ChEMBL 36 via Core Engine