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Compound Detail

CHEMBL411632

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

Basic Information

ChEMBL ID CHEMBL411632
Phase Preclinical
Structure Type MOL
InChI Key HZYVHWDHIRWTNY-UHFFFAOYSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

415.4
MW (Da)
3.89
ALogP
5
HBA
3
HBD
110.0
PSA (Ų)
0.60
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16F3N5O2
MW 415.38
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.72

Activity Summary

IC50 7 meas. best 7.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase Lck
CHEMBL258
IC50 7.85 7.34 14.0 2
Mitogen-activated protein kinase 14
CHEMBL260
IC50 7.85 7.85 14.0 1
Lymphocyte
CHEMBL612599
IC50 6.97 6.97 107.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
IC50 6.9 6.9 125.0 1
Blood
CHEMBL613416
IC50 5.9 5.9 1270.0 1
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 5.47 5.47 3423.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18321037 10.1021/jm7010996 Blood 2
18321037 10.1021/jm7010996 Tyrosine-protein kinase Lck 1
18321037 10.1021/jm7010996 Angiopoietin-1 receptor 1
18321037 10.1021/jm7010996 Mitogen-activated protein kinase 14 1
18321037 10.1021/jm7010996 Tyrosine-protein kinase JAK3 1
18321037 10.1021/jm7010996 Lymphocyte 1
18321037 10.1021/jm7010996 Vascular endothelial growth factor receptor 2 1
24915291 10.1021/jm4017762 Tyrosine-protein kinase BTK 1
24915291 10.1021/jm4017762 Tyrosine-protein kinase Lck 1
24915291 10.1021/jm4017762 Unchecked 1

Data from ChEMBL 36 via Core Engine