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Compound Detail

CHEMBL2040568

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COC(=O)c1nc(-c2cnccn2)[nH]c(=O)c1O

Basic Information

ChEMBL ID CHEMBL2040568
Phase Preclinical
Structure Type MOL
InChI Key SMBXFQJIADQFFG-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

248.2
MW (Da)
-0.28
ALogP
7
HBA
2
HBD
118.1
PSA (Ų)
0.70
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 C10H8N4O4
MW 248.20
Aromatic Rings 2
Heavy Atoms 18
NP-Likeness -0.74

Activity Summary

EC50 1 meas. best 4.59
Ki 1 meas. best 5.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Polymerase acidic protein
CHEMBL1169598
Ki 5.1 5.1 8000.0 1
Polymerase acidic protein
CHEMBL1169598
EC50 4.59 4.59 25460.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Polymerase acidic protein Ki = 8000.0 nM 5.1 Binding affinity to PA N-terminal domain (Competitive) 22211528
Polymerase acidic protein EC50 = 25460.0 nM 4.59 Plaque growth inhibition 22211528

Literature References

PubMed DOI Target Context # Activities
22211528 10.1021/cb200439z Polymerase acidic protein 2

Data from ChEMBL 36 via Core Engine