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Compound Detail

CHEMBL1836806

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Cc1cn2c(-c3cn[nH]c3)cnc2c(Nc2ccc(C(=O)N3CCNC(=O)C3)c(Cl)c2)n1

Basic Information

ChEMBL ID CHEMBL1836806
Phase Preclinical
Structure Type MOL
InChI Key SOSOLYMLXUWXON-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

450.9
MW (Da)
2.40
ALogP
7
HBA
3
HBD
120.3
PSA (Ų)
0.44
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 C21H19ClN8O2
MW 450.89
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.98

Activity Summary

IC50 1 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein-tyrosine kinase 6
CHEMBL4601
IC50 8.52 8.52 3.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein-tyrosine kinase 6 IC50 = 3.0 nM 8.52 Inhibition of BRK pretreated for 30 mins by microplate reader 21855335

Literature References

PubMed DOI Target Context # Activities
21855335 10.1016/j.bmcl.2011.07.101 Protein-tyrosine kinase 6 2
21855335 10.1016/j.bmcl.2011.07.101 Aurora kinase B 1
21855335 10.1016/j.bmcl.2011.07.101 Tyrosine-protein kinase Lck 1

Data from ChEMBL 36 via Core Engine