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Compound Detail

CHEMBL3975003

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C=CC(=O)Nc1cccc(-n2cnc3cnc(Nc4ccc(N5CCN(C)CC5)cc4)nc32)c1

Basic Information

ChEMBL ID CHEMBL3975003
Phase Preclinical
Structure Type MOL
InChI Key RLLHYPPCOXFSDP-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

454.5
MW (Da)
3.44
ALogP
8
HBA
2
HBD
91.2
PSA (Ų)
0.43
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26N8O
MW 454.54
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.49

Activity Summary

IC50 4 meas. best 7.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase BTK
CHEMBL5251
IC50 7.99 7.99 10.2 1
Tyrosine-protein kinase JAK3
CHEMBL2148
IC50 7.17 7.17 67.1 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.12 5.1 7550.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27994736 10.1021/acsmedchemlett.6b00235 NON-PROTEIN TARGET 2
27994736 10.1021/acsmedchemlett.6b00235 Tyrosine-protein kinase JAK3 1
27994736 10.1021/acsmedchemlett.6b00235 Tyrosine-protein kinase BTK 1

Data from ChEMBL 36 via Core Engine