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Compound Detail

CHEMBL485202

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CN(C(=O)c1ccccc1)c1ccc2c(c1)nc(NC(=O)c1ccccc1)n2CCC(N)=O

Basic Information

ChEMBL ID CHEMBL485202
Phase Preclinical
Structure Type MOL
InChI Key NWUSHDACDTZXCD-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

441.5
MW (Da)
3.44
ALogP
5
HBA
2
HBD
110.3
PSA (Ų)
0.46
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H23N5O3
MW 441.49
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.59

Activity Summary

IC50 5 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase ITK/TSK
CHEMBL2959
IC50 8.52 6.97 3.0 3
Insulin receptor
CHEMBL1981
IC50 6.92 6.585 120.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19111460 10.1016/j.bmcl.2008.12.028 Tyrosine-protein kinase ITK/TSK 2
18819794 10.1016/j.bmcl.2008.09.017 Tyrosine-protein kinase ITK/TSK 1
18819794 10.1016/j.bmcl.2008.09.017 Insulin receptor 1
19111460 10.1016/j.bmcl.2008.12.028 Insulin receptor 1
19111460 10.1016/j.bmcl.2008.12.028 Unchecked 1

Data from ChEMBL 36 via Core Engine