Compound Detail
CHEMBL283120
AXL-1717 🧪 Phase II
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🧪 Phase II
COc1cc([C@@H]2c3cc4c(cc3[C@H](O)[C@H]3COC(=O)[C@@H]23)OCO4)cc(OC)c1OC
Basic Information
| ChEMBL ID | CHEMBL283120 |
| Name | AXL-1717 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | YJGVMLPVUAXIQN-HAEOHBJNSA-N |
4
Targets
7
Activities
2
Assay Types
0
PK Parameters
20
Publications
6
Known Names
8
Indications
1
Mechanisms
Molecular Properties
414.4
MW (Da)
2.41
ALogP
8
HBA
1
HBD
92.7
PSA (Ų)
0.76
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Insulin-like growth factor I receptor inhibitor | INHIBITOR | Insulin-like growth factor 1 receptor | ✓ | ✓ |
Indications
Adenocarcinoma of Lung Carcinoma, Squamous Cell Astrocytoma Carcinoma, Non-Small-Cell Lung Gliosarcoma Hematologic Neoplasms Neoplasms Oligodendroglioma
Activity Summary
IC50 6 meas. best 7.22
Kd 1 meas. best 6.31
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| HT-29 CHEMBL384 | IC50 | 7.22 | 6.22 | 60.0 | 2 |
| P388 CHEMBL389 | IC50 | 7.22 | 6.22 | 60.0 | 2 |
| A549 CHEMBL392 | IC50 | 7.22 | 6.22 | 60.0 | 2 |
| DNA topoisomerase 2-alpha CHEMBL1806 | Kd | 6.31 | 6.31 | 486.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| P388 | IC50 | = | 60.0 | nM | 7.22 | In vitro cytotoxicity against the P-388 (from DBA/2 mouse) neoplastic cell line | 14980682 |
| A549 | IC50 | = | 60.0 | nM | 7.22 | In vitro cytotoxicity against the A-549 (human lung carcinoma) neoplastic cell l... | 14980682 |
| HT-29 | IC50 | = | 60.0 | nM | 7.22 | In vitro cytotoxicity against the HT-29 (human colon carcinoma) neoplastic cell ... | 14980682 |
| DNA topoisomerase 2-alpha | Kd | = | 486.0 | nM | 6.31 | Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase ... | 29191878 |
| P388 | IC50 | = | 6000.0 | nM | 5.22 | Cytotoxicity against mouse P388 cells | 7673931 |
| A549 | IC50 | = | 6000.0 | nM | 5.22 | Cytotoxicity against human A549 cells | 7673931 |
| HT-29 | IC50 | = | 6000.0 | nM | 5.22 | Cytotoxicity against human HT-29 cells | 7673931 |
Literature References
Data from ChEMBL 36 via Core Engine