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Compound Detail

CHEMBL207987

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NC(=O)c1nc(-c2ccccc2)oc1N

Basic Information

ChEMBL ID CHEMBL207987
Phase Preclinical
Structure Type MOL
InChI Key UPWLRKVVLBSIPK-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
1
PK Parameters
12
Publications
0
Known Names

Molecular Properties

203.2
MW (Da)
1.02
ALogP
4
HBA
2
HBD
95.1
PSA (Ų)
0.76
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 C10H9N3O2
MW 203.20
Aromatic Rings 2
Heavy Atoms 15
NP-Likeness -1.05

Activity Summary

IC50 2 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 4.96 4.96 11000.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.133 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16686533 10.1021/jm0510979 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
16686533 10.1021/jm0510979 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
16686533 10.1021/jm0510979 No relevant target 1
16686533 10.1021/jm0510979 Caco-2 1
16686533 10.1021/jm0510979 Liver microsomes 1
16686533 10.1021/jm0510979 Cytochrome P450 1A2 1
16686533 10.1021/jm0510979 Cytochrome P450 2C9 1
16686533 10.1021/jm0510979 Cytochrome P450 2C19 1
16686533 10.1021/jm0510979 Cytochrome P450 2D6 1
16686533 10.1021/jm0510979 Cytochrome P450 3A4 1
16686533 10.1021/jm0510979 HeLa 1
21708416 10.1016/j.ejmech.2011.05.066 Inhibitor of nuclear factor kappa-B kinase subunit beta 1

Data from ChEMBL 36 via Core Engine