Compound Detail
CHEMBL505915
GSK-1751853A Enter ChEMBL ID:
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COc1cc2c(cc1Nc1nc(Nc3cccc(F)c3C(N)=O)c3cc[nH]c3n1)N(C(=O)CN1CCN(C(C)C)CC1)CC2
Basic Information
| ChEMBL ID | CHEMBL505915 |
| Name | GSK-1751853A |
| Phase | Preclinical |
| Structure Type | MOL |
| InChI Key | NYPPEWQPHYILTM-UHFFFAOYSA-N |
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names
Molecular Properties
601.7
MW (Da)
3.61
ALogP
9
HBA
4
HBD
144.7
PSA (Ų)
0.23
QED
1
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Availability | Unknown |
| Chirality | Unknown |
Activity Summary
IC50 3 meas. best 7.5
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Insulin-like growth factor 1 receptor CHEMBL1957 | IC50 | 7.5 | 6.96 | 32.0 | 2 |
| Mitogen-activated protein kinase 8 CHEMBL2276 | IC50 | 5.8 | 5.8 | 1585.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Insulin-like growth factor 1 receptor | IC50 | = | 32.0 | nM | 7.5 | Inhibition of IGF-1R | 19071018 |
| Insulin-like growth factor 1 receptor | IC50 | = | 376.0 | nM | 6.42 | Inhibition of phospho IGFR1 by cellular assay | 19071018 |
| Mitogen-activated protein kinase 8 | IC50 | = | 1585.0 | nM | 5.8 | Inhibition of His-tagged JNK1 | 19071018 |
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/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 |
| - | 10.6019/CHEMBL1961873 | Receptor-type tyrosine-protein kinase FLT3 | 4 |
| - | 10.6019/CHEMBL1961873 | Leucine-rich repeat serine/threonine-protein kinase 2 | 4 |
| - | 10.6019/CHEMBL1961873 | Mitogen-activated protein kinase 9 | 2 |
| - | 10.6019/CHEMBL1961873 | SRSF protein kinase 3 | 2 |
| - | 10.6019/CHEMBL1961873 | Mitogen-activated protein kinase 3 | 2 |
| - | 10.6019/CHEMBL1961873 | Mitogen-activated protein kinase 1 | 2 |
| - | 10.6019/CHEMBL1961873 | Dual specificity protein kinase CLK2 | 2 |
| - | 10.6019/CHEMBL1961873 | Homeodomain-interacting protein kinase 1 | 2 |
| - | 10.6019/CHEMBL1961873 | Glycogen synthase kinase-3 beta | 2 |
| - | 10.6019/CHEMBL1961873 | Dual specificity tyrosine-phosphorylation-regulated kinase 2 | 2 |
| - | 10.6019/CHEMBL1961873 | Dual specificity tyrosine-phosphorylation-regulated kinase 1B | 2 |
Data from ChEMBL 36 via Core Engine