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Compound Detail

CHEMBL108431

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CS(=O)(=O)O.Oc1nc2ccc(N3CCN(CC4CC4)CC3)nc2c2ccccc12

Basic Information

ChEMBL ID CHEMBL108431
Phase Preclinical
Structure Type MOL
InChI Key DMUNWNITOHNAFN-UHFFFAOYSA-N
Parent Compound CHEMBL1179983
Active Moiety CHEMBL1179983
2
Targets
2
Activities
2
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

334.4
MW (Da)
3.02
ALogP
5
HBA
1
HBD
52.5
PSA (Ų)
0.75
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 C21H26N4O4S
MW 430.53
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.40

Activity Summary

EC50 1 meas. best 6.84
IC50 1 meas. best 7.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 7.15 7.15 71.0 1
P388
CHEMBL389
EC50 6.84 6.84 145.0 1

Pharmacokinetic Data

Parameter Value Units Species
Cmax 5830.99 nM Rattus norvegicus
Cmax 7.48 ug g-1 Rattus norvegicus
Cmax 8.85 ug g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12825952 10.1021/jm030109s Rattus norvegicus 4
12825952 10.1021/jm030109s Poly [ADP-ribose] polymerase 1 1
12825952 10.1021/jm030109s P388 1

Data from ChEMBL 36 via Core Engine