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Compound Detail

CHEMBL1254209

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COc1ccccc1N1CCN(c2ncnc3[nH]nc(Br)c23)CC1

Basic Information

ChEMBL ID CHEMBL1254209
Phase Preclinical
Structure Type MOL
InChI Key CQXAPCMYRSTDGK-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

389.3
MW (Da)
2.45
ALogP
6
HBA
1
HBD
70.2
PSA (Ų)
0.74
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H17BrN6O
MW 389.26
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -1.43

Activity Summary

IC50 2 meas. best 8.04

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ribosomal protein S6 kinase beta-1
CHEMBL4501
IC50 8.04 8.04 9.1 1
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 4.66 4.66 22000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Ribosomal protein S6 kinase beta-1 IC50 = 9.1 nM 8.04 Inhibition of S6K1 19465931
RAC-alpha serine/threonine-protein kinase IC50 = 22000.0 nM 4.66 Inhibition of AKT1 19465931

Literature References

PubMed DOI Target Context # Activities
19465931 10.1038/nchembio.183 Tyrosine-protein kinase ABL1 5
19465931 10.1038/nchembio.183 RAC-alpha serine/threonine-protein kinase 4
19465931 10.1038/nchembio.183 Epidermal growth factor receptor 3
19465931 10.1038/nchembio.183 Platelet-derived growth factor receptor alpha 3
19465931 10.1038/nchembio.183 Tyrosine-protein kinase JAK2 3
19465931 10.1038/nchembio.183 Proto-oncogene tyrosine-protein kinase receptor Ret 3
19465931 10.1038/nchembio.183 Ribosomal protein S6 kinase beta-1 2
19465931 10.1038/nchembio.183 Fibroblast growth factor receptor 3 2
19465931 10.1038/nchembio.183 Protein kinase C beta type 2
19465931 10.1038/nchembio.183 Receptor-type tyrosine-protein kinase FLT3 2
19465931 10.1038/nchembio.183 Serine/threonine-protein kinase B-raf 2
19465931 10.1038/nchembio.183 Mast/stem cell growth factor receptor Kit 2
19465931 10.1038/nchembio.183 Aurora kinase A 2
19465931 10.1038/nchembio.183 Hepatocyte growth factor receptor 2
19465931 10.1038/nchembio.183 Proto-oncogene tyrosine-protein kinase Src 2
19465931 10.1038/nchembio.183 Tyrosine-protein kinase Lyn 2
19465931 10.1038/nchembio.183 Aurora kinase B 1
19465931 10.1038/nchembio.183 PAS domain-containing serine/threonine-protein kinase 1
19465931 10.1038/nchembio.183 AMP-activated protein kinase (AMPK) alpha-1/beta-1/gamma-1 1
19465931 10.1038/nchembio.183 Beta-adrenergic receptor kinase 1 1

Data from ChEMBL 36 via Core Engine