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Compound Detail

CHEMBL4483477

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Cn1c(N2CCOCC2)nc2cc(N3CCC(CO)CC3)c(NC(=O)c3cnn4cccnc34)cc21

Basic Information

ChEMBL ID CHEMBL4483477
Phase Preclinical
Structure Type MOL
InChI Key LVDMRCKBQDTUEU-UHFFFAOYSA-N
1
Targets
2
Activities
2
Assay Types
4
PK Parameters
3
Publications
0
Known Names

Molecular Properties

490.6
MW (Da)
1.91
ALogP
10
HBA
2
HBD
113.0
PSA (Ų)
0.44
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H30N8O3
MW 490.57
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -1.96

Activity Summary

IC50 1 meas. best 7.01
Ki 1 meas. best 8.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
Ki 8.74 8.74 1.8 1
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
IC50 7.01 7.01 97.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 245.28 ng.hr.mL-1 Mus musculus
CL 23.0 mL.min-1.kg-1 Mus musculus
Cmax 200.0 nM Mus musculus
F 3.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31082230 10.1021/acs.jmedchem.9b00439 ADMET 8
31082230 10.1021/acs.jmedchem.9b00439 Interleukin-1 receptor-associated kinase 4 2
31082230 10.1021/acs.jmedchem.9b00439 Interleukin-1 receptor-associated kinase 1 1

Data from ChEMBL 36 via Core Engine