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Compound Detail

CHEMBL458806

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COc1cc(Nc2nc(NCC(C)(C)N)n3cc(-c4ccccc4)nc3c2C(N)=O)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL458806
Phase Preclinical
Structure Type MOL
InChI Key VTOIZTHVLKSUOX-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

475.6
MW (Da)
3.41
ALogP
9
HBA
4
HBD
141.8
PSA (Ų)
0.29
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H29N7O3
MW 475.55
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.80

Activity Summary

IC50 2 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 6.8 6.8 160.0 1
Tyrosine-protein kinase SYK
CHEMBL2599
IC50 6.08 6.08 840.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18823784 10.1016/j.bmc.2008.09.015 Tyrosine-protein kinase SYK 1
18823784 10.1016/j.bmc.2008.09.015 Tyrosine-protein kinase ZAP-70 1

Data from ChEMBL 36 via Core Engine