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Compound Detail

CHEMBL402629

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COc1ccc2ncc(-c3cccc(NC4CCNCC4)n3)n2c1

Basic Information

ChEMBL ID CHEMBL402629
Phase Preclinical
Structure Type MOL
InChI Key QTFQLQSPZXWTOC-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

323.4
MW (Da)
2.57
ALogP
6
HBA
2
HBD
63.5
PSA (Ų)
0.77
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 C18H21N5O
MW 323.40
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.21

Activity Summary

IC50 2 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
IC50 8.22 8.22 6.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 19.5 mL.min-1.g-1 Homo sapiens
CL 5.3 mL.min-1.g-1 Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Interleukin-1 receptor-associated kinase 4 IC50 = 6.0 nM 8.22 Inhibition of IRAK4 18501603

Literature References

PubMed DOI Target Context # Activities
18501603 10.1016/j.bmcl.2008.04.042 ADMET 2
18501603 10.1016/j.bmcl.2008.04.042 Interleukin-1 receptor-associated kinase 4 1
18501603 10.1016/j.bmcl.2008.04.042 Interleukin-1 receptor-associated kinase 1 1
18501603 10.1016/j.bmcl.2008.04.042 PBMC 1
18501603 10.1016/j.bmcl.2008.04.042 Cytochrome P450 3A4 1
18501603 10.1016/j.bmcl.2008.04.042 Cytochrome P450 2D6 1

Data from ChEMBL 36 via Core Engine