Compound Detail
CHEMBL185238
GW786460X Enter ChEMBL ID:
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Basic Information
| ChEMBL ID | CHEMBL185238 |
| Name | GW786460X |
| Phase | Preclinical |
| Structure Type | MOL |
| InChI Key | LBPKYPYHDKKRFS-UHFFFAOYSA-N |
2
Targets
8
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names
Molecular Properties
287.3
MW (Da)
3.39
ALogP
4
HBA
1
HBD
67.3
PSA (Ų)
0.61
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Availability | Unknown |
| Chirality | Unknown |
Activity Summary
IC50 8 meas. best 8.4
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| TGF-beta receptor type-1 CHEMBL4439 | IC50 | 8.4 | 7.8971 | 4.0 | 7 |
| Tyrosine-protein kinase ABL1 CHEMBL3099 | IC50 | 4.68 | 4.68 | 21000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| TGF-beta receptor type-1 | IC50 | = | 4.0 | nM | 8.4 | Inhibition of recombinant Activin A receptor type II-like kinase (ALK5) expresse... | 15317461 |
| TGF-beta receptor type-1 | IC50 | = | 4.0 | nM | 8.4 | Inhibition of TGFR1 | 19640613 |
| TGF-beta receptor type-1 | IC50 | = | 4.0 | nM | 8.4 | Inhibition of TGFbetaR1 (unknown origin) | 38626523 |
| TGF-beta receptor type-1 | IC50 | = | 10.0 | nM | 8.0 | Stimulation of Transforming growth factor beta receptor I kinase in HepG2 cells | 15317461 |
| TGF-beta receptor type-1 | IC50 | = | 20.0 | nM | 7.7 | Binding affinity to Activin A receptor type II-like kinase (ALK5) in fluorescenc... | 15317461 |
| TGF-beta receptor type-1 | IC50 | = | 23.0 | nM | 7.64 | Inhibition of TbetaR-1 (unknown origin) | 32092587 |
| TGF-beta receptor type-1 | IC50 | = | 181.0 | nM | 6.74 | Inhibition of human ALK5 expressed in Sf9 insect cells using casein as substrate... | 28135685 |
| Tyrosine-protein kinase ABL1 | IC50 | = | 21000.0 | nM | 4.68 | Inhibition of mouse ABL expressed in Sf9 insect cells using GGEAIYAAPFKK as subs... | 28135685 |
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 | Tyrosine-protein kinase Lyn | 4 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| - | 10.6019/CHEMBL1961873 | Leucine-rich repeat serine/threonine-protein kinase 2 | 4 |
| - | 10.6019/CHEMBL1961873 | Receptor-type tyrosine-protein kinase FLT3 | 4 |
| - | 10.6019/CHEMBL1961873 | Serine/threonine-protein kinase B-raf | 4 |
| - | 10.6019/CHEMBL1961873 | Protein kinase C beta type | 4 |
| - | 10.6019/CHEMBL1961873 | Cyclin-dependent kinase 2 | 4 |
| 15317461 | 10.1021/jm0400247 | TGF-beta receptor type-1 | 3 |
| - | 10.6019/CHEMBL1961873 | RAC-alpha serine/threonine-protein kinase | 2 |
| - | 10.6019/CHEMBL1961873 | RAC-beta serine/threonine-protein kinase | 2 |
| - | 10.6019/CHEMBL1961873 | RAC-gamma serine/threonine-protein kinase | 2 |
| - | 10.6019/CHEMBL1961873 | G protein-coupled receptor kinase 6 | 2 |
| - | 10.6019/CHEMBL1961873 | Protein kinase C theta type | 2 |
| - | 10.6019/CHEMBL1961873 | Serine/threonine-protein kinase D1 | 2 |
| - | 10.6019/CHEMBL1961873 | Serine/threonine-protein kinase D2 | 2 |
Data from ChEMBL 36 via Core Engine