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Compound Detail

CHEMBL524015

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CSc1nc(-c2cccc(C(F)(F)F)c2)c(-c2ccnc(F)c2)[nH]1

Basic Information

ChEMBL ID CHEMBL524015
Phase Preclinical
Structure Type MOL
InChI Key KLOOFNADZQKJDI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

353.3
MW (Da)
5.02
ALogP
3
HBA
1
HBD
41.6
PSA (Ų)
0.41
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H11F4N3S
MW 353.34
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.69

Activity Summary

IC50 2 meas. best 5.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 5.96 5.96 1090.0 1
Blood
CHEMBL613416
IC50 4.36 4.36 44200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 1090.0 nM 5.96 Inhibition of p38alpha 18578517
Blood IC50 = 44200.0 nM 4.36 Inhibition of TNFalpha release in human whole blood 18578517

Literature References

PubMed DOI Target Context # Activities
18578517 10.1021/jm701529q Blood 2
18578517 10.1021/jm701529q Mitogen-activated protein kinase 14 1

Data from ChEMBL 36 via Core Engine