Compound Detail
CHEMBL2103839
RIDAFOROLIMUS 🧪 Phase III
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🧪 Phase III
CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@@H](OP(C)(C)=O)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C
Basic Information
| ChEMBL ID | CHEMBL2103839 |
| Name | RIDAFOROLIMUS |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | BUROJSBIWGDYCN-GAUTUEMISA-N |
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
20
Publications
6
Known Names
19
Indications
1
Mechanisms
Molecular Properties
990.2
MW (Da)
7.74
ALogP
14
HBA
2
HBD
201.5
PSA (Ų)
0.10
QED
3
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serine/threonine-protein kinase mTOR inhibitor | INHIBITOR | Serine/threonine-protein kinase mTOR | ✓ | ✓ |
Indications
Neoplasms Neoplasms Osteosarcoma Osteosarcoma Sarcoma Sarcoma Breast Neoplasms Breast Neoplasms Carcinoma, Non-Small-Cell Lung Endometrial Neoplasms Leiomyosarcoma Leukemia Liposarcoma Lymphoma Myelodysplastic Syndromes Primary Myelofibrosis Prostatic Neoplasms, Castration-Resistant Gliosarcoma Multiple Myeloma
ATC Classification
L01EG03
ridaforolimus
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
Kd 1 meas. best 5.9
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B CHEMBL5543 | Kd | 5.9 | 5.9 | 1262.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Kd | = | 1262.0 | nM | 5.9 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... | 29191878 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 29191878 | 10.1126/science.aan4368 | Unchecked | 5 |
| 29191878 | 10.1126/science.aan4368 | Activin receptor type-1 | 1 |
| 38157838 | 10.1016/j.bmc.2023.117561 | Unchecked | 1 |
| 29191878 | 10.1126/science.aan4368 | Adenylate kinase 2, mitochondrial | 1 |
| 29191878 | 10.1126/science.aan4368 | Beta-adrenergic receptor kinase 1 | 1 |
| 29191878 | 10.1126/science.aan4368 | Adenosine kinase | 1 |
| 29191878 | 10.1126/science.aan4368 | Uncharacterized aarF domain-containing protein kinase 5 | 1 |
| 29191878 | 10.1126/science.aan4368 | Atypical kinase COQ8A, mitochondrial | 1 |
| 29191878 | 10.1126/science.aan4368 | AarF domain-containing protein kinase 1 | 1 |
| 29191878 | 10.1126/science.aan4368 | Activin receptor type-2B | 1 |
| 29191878 | 10.1126/science.aan4368 | Activin receptor type-1B | 1 |
| 29191878 | 10.1126/science.aan4368 | AP2-associated protein kinase 1 | 1 |
| 29191878 | 10.1126/science.aan4368 | Actin-related protein 3 | 1 |
| 29191878 | 10.1126/science.aan4368 | Actin-related protein 2 | 1 |
| 29191878 | 10.1126/science.aan4368 | Long-chain-fatty-acid--CoA ligase 5 | 1 |
| 29191878 | 10.1126/science.aan4368 | Peroxisomal acyl-coenzyme A oxidase 3 | 1 |
| 29191878 | 10.1126/science.aan4368 | Very long-chain specific acyl-CoA dehydrogenase, mitochondrial | 1 |
| 29191878 | 10.1126/science.aan4368 | Acyl-CoA dehydrogenase family member 11 | 1 |
| 29191878 | 10.1126/science.aan4368 | Acyl-CoA dehydrogenase family member 10 | 1 |
| 29191878 | 10.1126/science.aan4368 | Tyrosine-protein kinase ABL2 | 1 |
Data from ChEMBL 36 via Core Engine