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Compound Detail

CHEMBL4175428

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CC#CC(=O)N1CCC[C@@H](n2c(=O)n(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1

Basic Information

ChEMBL ID CHEMBL4175428
Phase Preclinical
Structure Type MOL
InChI Key BYZCNAKZYXERPN-LJQANCHMSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

468.5
MW (Da)
3.14
ALogP
8
HBA
1
HBD
108.3
PSA (Ų)
0.46
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 C26H24N6O3
MW 468.52
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.64

Activity Summary

IC50 2 meas. best 8.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 8.66 8.66 2.2 1
Tyrosine-protein kinase Tec
CHEMBL4246
IC50 8.28 8.28 5.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase BTK IC50 = 2.2 nM 8.66 Inhibition of BTK (unknown origin) 29631132
Tyrosine-protein kinase Tec IC50 = 5.3 nM 8.28 Inhibition of TEC (unknown origin) 29631132

Literature References

PubMed DOI Target Context # Activities
29631132 10.1016/j.ejmech.2018.03.062 Tyrosine-protein kinase Tec 1
29631132 10.1016/j.ejmech.2018.03.062 Tyrosine-protein kinase BTK 1

Data from ChEMBL 36 via Core Engine