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Compound Detail

CHEMBL3617205

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CNC(=O)c1nc(-c2cccs2)[nH]c(=O)c1O

Basic Information

ChEMBL ID CHEMBL3617205
Phase Preclinical
Structure Type MOL
InChI Key MAOSMWFVKCTXKC-UHFFFAOYSA-N
3
Targets
4
Activities
2
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

251.3
MW (Da)
0.56
ALogP
5
HBA
3
HBD
95.1
PSA (Ų)
0.73
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H9N3O3S
MW 251.27
Aromatic Rings 2
Heavy Atoms 17
NP-Likeness -1.32

Activity Summary

IC50 3 meas. best 6.22
Kd 1 meas. best 5.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
DNA excision repair protein ERCC-1/DNA repair endonuclease XPF
CHEMBL3883316
IC50 6.22 6.22 600.0 1
DNA excision repair protein ERCC-1/DNA repair endonuclease XPF
CHEMBL3883316
Kd 5.4 5.4 4000.0 1
Flap endonuclease 1
CHEMBL5027
IC50 4.92 4.92 12000.0 1
Deoxyribonuclease-1
CHEMBL3351219
IC50 4.17 4.17 67600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 6.667 hr Mus musculus
T1/2 3.017 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26321360 10.1016/j.bmcl.2015.08.024 DNA excision repair protein ERCC-1/DNA repair endonuclease XPF 6
26321360 10.1016/j.bmcl.2015.08.024 No relevant target 2
26321360 10.1016/j.bmcl.2015.08.024 Flap endonuclease 1 1
26321360 10.1016/j.bmcl.2015.08.024 Deoxyribonuclease-1 1
26321360 10.1016/j.bmcl.2015.08.024 A-375 1
26321360 10.1016/j.bmcl.2015.08.024 HepG2 1
26321360 10.1016/j.bmcl.2015.08.024 Liver 1
26321360 10.1016/j.bmcl.2015.08.024 Liver microsome 1

Data from ChEMBL 36 via Core Engine