Compound Detail
CHEMBL476259
GSK-1326255A Enter ChEMBL ID:
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CCCN1CCC(c2ccc(Nc3nc(Nc4cc(F)ccc4C(N)=O)c4cc[nH]c4n3)c(OC)c2)CC1
Basic Information
| ChEMBL ID | CHEMBL476259 |
| Name | GSK-1326255A |
| Phase | Preclinical |
| Structure Type | MOL |
| InChI Key | UKKOZAHWQFYYRW-UHFFFAOYSA-N |
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names
Molecular Properties
517.6
MW (Da)
5.28
ALogP
7
HBA
4
HBD
121.2
PSA (Ų)
0.24
QED
2
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Availability | Unknown |
| Chirality | Unknown |
Activity Summary
IC50 5 meas. best 9.52
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Insulin-like growth factor 1 receptor CHEMBL1957 | IC50 | 9.52 | 8.425 | 0.3 | 2 |
| G protein-coupled receptor kinase 5 CHEMBL5678 | IC50 | 5.6 | 5.6 | 2500.0 | 1 |
| Beta-adrenergic receptor kinase 1 CHEMBL4079 | IC50 | 5.1 | 5.1 | 7900.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Insulin-like growth factor 1 receptor | IC50 | = | 0.3 | nM | 9.52 | Inhibition of GST-tagged human IGF1R expressed in Sf9 cells by Wallac Victor flu... | 19056263 |
| Insulin-like growth factor 1 receptor | IC50 | = | 47.0 | nM | 7.33 | Inhibition of human IGF1R phosphorylation expressed in HEK293 cells by DELFIA | 19056263 |
| G protein-coupled receptor kinase 5 | IC50 | = | 2500.0 | nM | 5.6 | Displacement of BODIPY TR-ADP from GRK5 (unknown origin) preincubated for 10 min... | 31857838 |
| Beta-adrenergic receptor kinase 1 | IC50 | = | 7900.0 | nM | 5.1 | Displacement of BODIPY TR-ADP from human GRK2 preincubated for 10 mins followed ... | 31857838 |
| Beta-adrenergic receptor kinase 1 | IC50 | = | 7900.0 | nM | 5.1 | Inhibition of GRK2 (unknown origin) | 36055000 |
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 | Platelet-derived growth factor receptor alpha | 8 |
| - | 10.6019/CHEMBL1961873 | Mast/stem cell growth factor receptor Kit | 8 |
| - | 10.6019/CHEMBL1961873 | Proto-oncogene tyrosine-protein kinase receptor Ret | 6 |
| - | 10.6019/CHEMBL1961873 | Leucine-rich repeat serine/threonine-protein kinase 2 | 4 |
| - | 10.6019/CHEMBL1961873 | Tyrosine-protein kinase Lyn | 4 |
| - | 10.6019/CHEMBL1961873 | Serine/threonine-protein kinase B-raf | 4 |
| - | 10.6019/CHEMBL1961873 | Protein kinase C beta type | 4 |
| - | 10.6019/CHEMBL1961873 | Receptor-type tyrosine-protein kinase FLT3 | 4 |
| - | 10.6019/CHEMBL1961873 | Cyclin-dependent kinase 2 | 4 |
| - | 10.6019/CHEMBL1961873 | Ribosomal protein S6 kinase beta-1 | 2 |
| - | 10.6019/CHEMBL1961873 | Protein kinase C alpha type | 2 |
| - | 10.6019/CHEMBL1961873 | cAMP-dependent protein kinase catalytic subunit alpha | 2 |
| - | 10.6019/CHEMBL1961873 | Ribosomal protein S6 kinase alpha-5 | 2 |
| - | 10.6019/CHEMBL1961873 | Serine/threonine-protein kinase MRCK beta | 2 |
| - | 10.6019/CHEMBL1961873 | Rhodopsin kinase GRK7 | 2 |
| - | 10.6019/CHEMBL1961873 | G protein-coupled receptor kinase 6 | 2 |
| - | 10.6019/CHEMBL1961873 | RAC-beta serine/threonine-protein kinase | 2 |
| - | 10.6019/CHEMBL1961873 | RAC-alpha serine/threonine-protein kinase | 2 |
Data from ChEMBL 36 via Core Engine