Compound Detail
CHEMBL149082
TRAMIPROSATE 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL149082 |
| Name | TRAMIPROSATE |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | SNKZJIOFVMKAOJ-UHFFFAOYSA-N |
3
Targets
5
Activities
2
Assay Types
1
PK Parameters
15
Publications
8
Known Names
1
Indications
1
Mechanisms
Molecular Properties
139.2
MW (Da)
-0.78
ALogP
3
HBA
2
HBD
80.4
PSA (Ų)
0.50
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Amyloid-beta A4 protein stabiliser | STABILISER | Amyloid-beta precursor protein | ✓ | ✓ |
Indications
Alzheimer Disease
Activity Summary
IC50 4 meas. best 6.52
Ki 1 meas.
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| GABA-A receptor; anion channel CHEMBL1907607 | IC50 | 6.52 | 6.52 | 300.0 | 1 |
| GABA B receptor CHEMBL2111474 | IC50 | 5.7 | 5.11 | 2000.0 | 2 |
| Amyloid-beta precursor protein CHEMBL2487 | IC50 | 4.0 | 4.0 | 100000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| T1/2 | 9.0 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| GABA-A receptor; anion channel | IC50 | = | 300.0 | nM | 6.52 | Binding affinity against Gamma-aminobutyric acid A receptor in rat brain synapto... | - |
| GABA B receptor | IC50 | = | 2000.0 | nM | 5.7 | In vitro displacement of [3H]GABA from Gamma-aminobutyric acid type B receptor s... | - |
| GABA B receptor | IC50 | = | 30000.0 | nM | 4.52 | Binding affinity against Gamma-aminobutyric acid type B receptor in rat brain sy... | - |
| Amyloid-beta precursor protein | IC50 | = | 100000.0 | nM | 4.0 | Inhibition of amyloid beta (1 to 42) aggregation (unknown origin) at 4:1 compoun... | 23484434 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 23601707 | 10.1016/j.bmcl.2013.02.104 | Rattus norvegicus | 13 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| - | 10.1016/0960-894X(96)00307-1 | Cavia porcellus | 2 |
| 21955456 | 10.1016/j.bmc.2011.08.058 | Proton-coupled amino acid transporter 1 | 2 |
| 27687671 | 10.1016/j.bmcl.2016.09.009 | CDGSH iron-sulfur domain-containing protein 1 | 2 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.1016/S0960-894X(01)81218-X | GABA B receptor | 1 |
| - | 10.1016/0960-894X(96)00307-1 | GABA B receptor | 1 |
| - | 10.1016/0960-894X(96)00307-1 | GABA-A receptor; anion channel | 1 |
| 23601707 | 10.1016/j.bmcl.2013.02.104 | Mus musculus | 1 |
| 23601707 | 10.1016/j.bmcl.2013.02.104 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 23484434 | 10.1021/jm3017317 | Amyloid-beta precursor protein | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 35841881 | 10.1016/j.ejmech.2022.114578 | ADMET | 1 |
Data from ChEMBL 36 via Core Engine