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Compound Detail

CHEMBL271372

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Cc1ccc(NC(=O)c2cccc(C(F)(F)F)c2)cc1C(=O)Nc1cnc(NC2CCN(C)CC2)nc1

Basic Information

ChEMBL ID CHEMBL271372
Phase Preclinical
Structure Type MOL
InChI Key RCPGEVOBRRSEJB-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

512.5
MW (Da)
4.81
ALogP
6
HBA
3
HBD
99.2
PSA (Ų)
0.44
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H27F3N6O2
MW 512.54
Aromatic Rings 3
Heavy Atoms 37
NP-Likeness -1.70

Activity Summary

IC50 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mitogen-activated protein kinase 14
CHEMBL260
IC50 8.3 8.3 5.0 1
Tyrosine-protein kinase Lck
CHEMBL258
IC50 5.88 5.88 1310.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mitogen-activated protein kinase 14 IC50 = 5.0 nM 8.3 Inhibition of p38alpha by HTRF assay 18321037
Tyrosine-protein kinase Lck IC50 = 1310.0 nM 5.88 Inhibition of Lck by HTRF assay 18321037

Literature References

PubMed DOI Target Context # Activities
18321037 10.1021/jm7010996 Tyrosine-protein kinase Lck 1
18321037 10.1021/jm7010996 Angiopoietin-1 receptor 1
18321037 10.1021/jm7010996 Vascular endothelial growth factor receptor 2 1
18321037 10.1021/jm7010996 Mitogen-activated protein kinase 14 1
18321037 10.1021/jm7010996 Tyrosine-protein kinase JAK3 1

Data from ChEMBL 36 via Core Engine