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Compound Detail

CHEMBL490407

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CC(C)(C)c1ccc(Nc2noc3c(C(=O)Nc4cncnc4)c(Cl)ccc23)cc1

Basic Information

ChEMBL ID CHEMBL490407
Phase Preclinical
Structure Type MOL
InChI Key IYVUYLAUPKYTIO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

421.9
MW (Da)
5.56
ALogP
6
HBA
2
HBD
92.9
PSA (Ų)
0.45
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H20ClN5O2
MW 421.89
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.46

Activity Summary

IC50 2 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Mast/stem cell growth factor receptor Kit
CHEMBL1936
IC50 8.1 8.1 8.0 1
Unchecked
CHEMBL612545
IC50 6.72 6.72 190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Mast/stem cell growth factor receptor Kit IC50 = 8.0 nM 8.1 Inhibition of c-kit 18723346
Unchecked IC50 = 190.0 nM 6.72 Inhibition of p38 18723346

Literature References

PubMed DOI Target Context # Activities
18723346 10.1016/j.bmcl.2008.07.111 Unchecked 2
18723346 10.1016/j.bmcl.2008.07.111 Mast/stem cell growth factor receptor Kit 1

Data from ChEMBL 36 via Core Engine