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Compound Detail

CHEMBL1836865

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CC1(C)CN(C(=O)c2ccc(Nc3nc(C4CC4)cn4c(-c5cn[nH]c5)cnc34)c(F)c2)CCN1

Basic Information

ChEMBL ID CHEMBL1836865
Phase Preclinical
Structure Type MOL
InChI Key VQUVLPVWCDXSOK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

474.5
MW (Da)
3.70
ALogP
7
HBA
3
HBD
103.2
PSA (Ų)
0.41
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27FN8O
MW 474.54
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.60

Activity Summary

IC50 1 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein-tyrosine kinase 6
CHEMBL4601
IC50 8.22 8.22 6.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein-tyrosine kinase 6 IC50 = 6.0 nM 8.22 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