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Compound Detail

CHEMBL475882

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COc1cc(Nc2nc(N[C@H]3CCCC[C@H]3N)n3nc(-c4cccc(OC)c4)nc3c2C(N)=O)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL475882
Phase Preclinical
Structure Type MOL
InChI Key QQVFMNGYKNAGOD-RTWAWAEBSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

532.6
MW (Da)
3.34
ALogP
11
HBA
4
HBD
163.9
PSA (Ų)
0.25
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N8O4
MW 532.61
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -1.00

Activity Summary

IC50 2 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ZAP-70
CHEMBL2803
IC50 6.92 6.92 120.0 1
Lysine--tRNA ligase
CHEMBL5575
IC50 6.92 6.92 120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lysine--tRNA ligase IC50 = 120.0 nM 6.92 Inhibition of human Syk 18585046
Tyrosine-protein kinase ZAP-70 IC50 = 120.0 nM 6.92 Inhibition of human ZAP70 18585046

Literature References

PubMed DOI Target Context # Activities
18585046 10.1016/j.bmc.2008.06.017 Lysine--tRNA ligase 1
18585046 10.1016/j.bmc.2008.06.017 Tyrosine-protein kinase ZAP-70 1

Data from ChEMBL 36 via Core Engine