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Compound Detail

CHEMBL3314273

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CSc1nccc(-c2c(-c3ccc(F)cc3)nc3nc(-c4cn(CC(=O)[O-])nn4)ccn23)n1.[Na+]

Basic Information

ChEMBL ID CHEMBL3314273
Phase Preclinical
Structure Type MOL
InChI Key CWJBAPFHGXBIMX-UHFFFAOYSA-M
Parent Compound CHEMBL3558113
Active Moiety CHEMBL3558113
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

462.5
MW (Da)
3.06
ALogP
10
HBA
1
HBD
124.0
PSA (Ų)
0.30
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H14FN8NaO2S
MW 484.45
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -1.80

Activity Summary

IC50 1 meas. best 6.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.6 6.6 250.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 250.0 nM 6.6 Inhibition of p38alpha MAPK (unknown origin) by radiometric assay 24930833

Literature References

PubMed DOI Target Context # Activities
24930833 10.1016/j.bmcl.2014.05.080 Mitogen-activated protein kinase 14 1
24930833 10.1016/j.bmcl.2014.05.080 Casein kinase I isoform delta 1
24930833 10.1016/j.bmcl.2014.05.080 Tyrosine-protein kinase JAK1 1
24930833 10.1016/j.bmcl.2014.05.080 Tyrosine-protein kinase JAK2 1
24930833 10.1016/j.bmcl.2014.05.080 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine