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Compound Detail

CHEMBL1794064

GSK-561866B
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CCn1c(-c2nonc2N)nc2c(C#CCN)ncc(OCCCN)c21.O=C(O)C(F)(F)F

Basic Information

ChEMBL ID CHEMBL1794064
Name GSK-561866B
Phase Preclinical
Structure Type MOL
InChI Key ZNQRTKUBYISFTI-UHFFFAOYSA-N
Parent Compound CHEMBL494280
Active Moiety CHEMBL494280
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

356.4
MW (Da)
0.12
ALogP
10
HBA
3
HBD
156.9
PSA (Ų)
0.41
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H21F3N8O4
MW 470.41
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -0.66

Activity Summary

IC50 3 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Rho-associated protein kinase 1
CHEMBL3231
IC50 6.7 6.7 200.0 1
Ribosomal protein S6 kinase alpha-1
CHEMBL2553
IC50 6.6 6.6 251.0 1
RAC-alpha serine/threonine-protein kinase
CHEMBL4282
IC50 6.1 6.1 794.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL1961873 Tyrosine-protein kinase ABL1 14
- 10.6019/CHEMBL1961873 Epidermal growth factor receptor 10
- 10.6019/CHEMBL1961873 Mast/stem cell growth factor receptor Kit 8
- 10.6019/CHEMBL1961873 Platelet-derived growth factor receptor alpha 8
- 10.6019/CHEMBL1961873 Proto-oncogene tyrosine-protein kinase receptor Ret 6
- 10.6019/CHEMBL1961873 Cyclin-dependent kinase 2 4
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase B-raf 4
- 10.6019/CHEMBL1961873 Leucine-rich repeat serine/threonine-protein kinase 2 4
- 10.6019/CHEMBL1961873 Protein kinase C beta type 4
- 10.6019/CHEMBL1961873 Receptor-type tyrosine-protein kinase FLT3 4
- 10.6019/CHEMBL1961873 Tyrosine-protein kinase Lyn 4
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase MRCK beta 2
- 10.6019/CHEMBL1961873 Ribosomal protein S6 kinase alpha-5 2
- 10.6019/CHEMBL1961873 Ribosomal protein S6 kinase alpha-4 2
- 10.6019/CHEMBL1961873 Ribosomal protein S6 kinase beta-1 2
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase MRCK alpha 2
- 10.6019/CHEMBL1961873 RAC-gamma serine/threonine-protein kinase 2
- 10.6019/CHEMBL1961873 RAC-beta serine/threonine-protein kinase 2
- 10.6019/CHEMBL2007661 Serine/threonine-protein kinase TBK1 2
- 10.6019/CHEMBL1961873 Serine/threonine-protein kinase D2 2

Data from ChEMBL 36 via Core Engine