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Compound Detail

CHEMBL388619

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O=C1NCCc2[nH]c(-c3ccnc(-c4cccc(O)c4)c3)cc21

Basic Information

ChEMBL ID CHEMBL388619
Phase Preclinical
Structure Type MOL
InChI Key BEJGBKAIVFARDV-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

305.3
MW (Da)
2.74
ALogP
3
HBA
3
HBD
78.0
PSA (Ų)
0.68
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 C18H15N3O2
MW 305.34
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.23

Activity Summary

IC50 2 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MAP kinase-activated protein kinase 2
CHEMBL2208
IC50 7.6 7.6 25.0 1
U-937
CHEMBL612794
IC50 4.44 4.44 36000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MAP kinase-activated protein kinase 2 IC50 = 25.0 nM 7.6 Inhibition of MK2 17480064
U-937 IC50 = 36000.0 nM 4.44 Inhibition of TNFalpha production in U937 cells 17480064

Literature References

PubMed DOI Target Context # Activities
17480064 10.1021/jm0611004 MAP kinase-activated protein kinase 2 1
17480064 10.1021/jm0611004 U-937 1

Data from ChEMBL 36 via Core Engine