Compound Detail
CHEMBL5314429
TAMNORZATINIB 🧪 Phase II
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🧪 Phase II
COc1cc2nccc(Oc3ccc(NC(=O)c4cc5c(n(-c6ccccc6)c4=O)CCCC5=O)nc3)c2cc1OC
Basic Information
| ChEMBL ID | CHEMBL5314429 |
| Name | TAMNORZATINIB |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | WHMMKPWGWNYYFE-UHFFFAOYSA-N |
2
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
3
Known Names
1
Indications
Molecular Properties
562.6
MW (Da)
5.36
ALogP
9
HBA
1
HBD
121.6
PSA (Ų)
0.28
QED
2
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Indications
Neoplasms
Activity Summary
IC50 3 meas. best 9.15
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Tyrosine-protein kinase receptor UFO CHEMBL4895 | IC50 | 9.15 | 8.905 | 0.7 | 2 |
| Tyrosine-protein kinase Mer CHEMBL5331 | IC50 | 8.01 | 8.01 | 9.8 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase receptor UFO | IC50 | = | 0.7 | nM | 9.15 | Inhibition of AXL (unknown origin) by HTRF kinase assay | 38714043 |
| Tyrosine-protein kinase receptor UFO | IC50 | = | 2.2 | nM | 8.66 | Inhibition of AXL (unknown origin) preincubated for 15 mins followed by substrat... | 38913493 |
| Tyrosine-protein kinase Mer | IC50 | = | 9.8 | nM | 8.01 | Inhibition of MER (unknown origin) preincubated for 15 mins followed by substrat... | 38913493 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 38913493 | 10.1021/acs.jmedchem.4c00400 | ADMET | 5 |
| 38714043 | 10.1016/j.ejmech.2024.116475 | Tyrosine-protein kinase receptor UFO | 1 |
| 38913493 | 10.1021/acs.jmedchem.4c00400 | Tyrosine-protein kinase Mer | 1 |
| 38913493 | 10.1021/acs.jmedchem.4c00400 | Tyrosine-protein kinase receptor UFO | 1 |
| 38913493 | 10.1021/acs.jmedchem.4c00400 | 4T1 | 1 |
| 38913493 | 10.1021/acs.jmedchem.4c00400 | MDA-MB-231 | 1 |
| 38913493 | 10.1021/acs.jmedchem.4c00400 | MC-38 | 1 |
| 38913493 | 10.1021/acs.jmedchem.4c00400 | Hepa 1-6 | 1 |
Data from ChEMBL 36 via Core Engine