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Compound Detail

CHEMBL4852264

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C#CC(=O)N1CCC(c2cnn3c(C(N)=O)c(-c4ccc(Oc5ccc(F)cc5)cc4)[nH]c23)C1

Basic Information

ChEMBL ID CHEMBL4852264
Phase Preclinical
Structure Type MOL
InChI Key DIDJYPFYHDBXHU-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

457.5
MW (Da)
3.31
ALogP
5
HBA
2
HBD
105.7
PSA (Ų)
0.45
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20FN5O3
MW 457.47
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.10

Activity Summary

IC50 4 meas. best 7.41

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.41 7.41 38.6 1
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 6.99 6.99 103.0 1
Cytoplasmic tyrosine-protein kinase BMX
CHEMBL3834
IC50 6.92 6.92 121.0 1
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 6.42 6.42 385.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34391034 10.1016/j.ejmech.2021.113724 Unchecked 3
34391034 10.1016/j.ejmech.2021.113724 Tyrosine-protein kinase BTK 1
34391034 10.1016/j.ejmech.2021.113724 Epidermal growth factor receptor 1
34391034 10.1016/j.ejmech.2021.113724 Cytoplasmic tyrosine-protein kinase BMX 1
34391034 10.1016/j.ejmech.2021.113724 Tyrosine-protein kinase ITK/TSK 1

Data from ChEMBL 36 via Core Engine