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Compound Detail

CHEMBL5285357

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CC#CC(=O)N1CC[C@H](N2CN(c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1

Basic Information

ChEMBL ID CHEMBL5285357
Phase Preclinical
Structure Type MOL
InChI Key ATTKNMWCPOFQHD-IBGZPJMESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

440.5
MW (Da)
3.39
ALogP
7
HBA
1
HBD
87.8
PSA (Ų)
0.62
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H24N6O2
MW 440.51
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.80

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

Literature References

PubMed DOI Target Context # Activities
34479103 10.1016/j.bmc.2021.116358 Tyrosine-protein kinase BTK 1
34479103 10.1016/j.bmc.2021.116358 Tyrosine-protein kinase Tec 1
34479103 10.1016/j.bmc.2021.116358 Tyrosine-protein kinase Lck 1
34479103 10.1016/j.bmc.2021.116358 Tyrosine-protein kinase Lyn 1
34479103 10.1016/j.bmc.2021.116358 Tyrosine-protein kinase Fyn 1

Data from ChEMBL 36 via Core Engine