Compound Detail
CHEMBL4297384
GSK-356278 Phase I
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Phase I
Basic Information
| ChEMBL ID | CHEMBL4297384 |
| Name | GSK-356278 |
| Phase | Phase I |
| Structure Type | MOL |
| InChI Key | AWDJJMXJUOHGLC-UHFFFAOYSA-N |
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
12
Publications
3
Known Names
2
Indications
Molecular Properties
439.6
MW (Da)
3.76
ALogP
10
HBA
1
HBD
103.8
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Indications
Depressive Disorder Huntington Disease
Activity Summary
IC50 2 meas. best 9.12
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| High affinity 3',5'-cyclic-AMP phosphodiesterase 7A CHEMBL3012 | IC50 | 9.12 | 9.12 | 0.8 | 1 |
| Phosphodiesterase 3 CHEMBL2094125 | IC50 | 8.3 | 8.3 | 5.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| High affinity 3',5'-cyclic-AMP phosphodiesterase 7A | IC50 | = | 0.76 | nM | 9.12 | Inhibition of PDE7A (unknown origin) | 36796299 |
| Phosphodiesterase 3 | IC50 | = | 5.0 | nM | 8.3 | Inhibition of human recombinant PDE3 expressed in Escherichia coli | 36796299 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 36796299 | 10.1016/j.ejmech.2023.115194 | High affinity 3',5'-cyclic-AMP phosphodiesterase 7A | 1 |
| 36796299 | 10.1016/j.ejmech.2023.115194 | Phosphodiesterase 3 | 1 |
| - | 10.6019/CHEMBL5724796 | Casein kinase I isoform delta | 1 |
| - | 10.6019/CHEMBL5724796 | Cyclin-dependent kinase 2 | 1 |
| - | 10.6019/CHEMBL5724796 | Glycogen synthase kinase-3 beta | 1 |
| - | 10.6019/CHEMBL5724796 | Mitogen-activated protein kinase 1 | 1 |
| - | 10.6019/CHEMBL5724796 | Aurora kinase A | 1 |
| - | 10.6019/CHEMBL5724796 | Tyrosine-protein kinase ABL1 | 1 |
| - | 10.6019/CHEMBL5724796 | Fibroblast growth factor receptor 2 | 1 |
| - | 10.6019/CHEMBL5724796 | Peregrin | 1 |
| - | 10.6019/CHEMBL5724796 | Transcription intermediary factor 1-alpha | 1 |
| - | 10.6019/CHEMBL5724796 | Bromodomain-containing protein 4 | 1 |
Data from ChEMBL 36 via Core Engine