Compound Detail
CHEMBL283656
DAZMEGREL 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL283656 |
| Name | DAZMEGREL |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | DEQLGSOHGTZKFB-UHFFFAOYSA-N |
3
Targets
7
Activities
1
Assay Types
0
PK Parameters
15
Publications
3
Known Names
Molecular Properties
283.3
MW (Da)
2.67
ALogP
4
HBA
1
HBD
60.0
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Activity Summary
IC50 7 meas. best 7.55
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Thromboxane-A synthase CHEMBL1835 | IC50 | 7.55 | 7.55 | 28.0 | 3 |
| Homo sapiens CHEMBL372 | IC50 | 5.72 | 5.1433 | 1900.0 | 3 |
| Rattus norvegicus CHEMBL376 | IC50 | 4.92 | 4.92 | 12000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Thromboxane-A synthase | IC50 | = | 28.0 | nM | 7.55 | Activity against human platelet microsome Thromboxane synthase | 9341919 |
| Thromboxane-A synthase | IC50 | = | 28.0 | nM | 7.55 | Inhibitory activity against human platelet microsomal TXA2 synthase | - |
| Thromboxane-A synthase | IC50 | = | 28.0 | nM | 7.55 | Inhibition of TXA2 synthetase from human platelets | 3081722 |
| Homo sapiens | IC50 | = | 1900.0 | nM | 5.72 | In vitro inhibition of ADP-induced aggregation of human platelet rich plasma in ... | 2704033 |
| Homo sapiens | IC50 | = | 2000.0 | nM | 5.7 | Inhibition of ADP-induced platelet aggregation of human PRP in the presence of p... | 1311763 |
| Rattus norvegicus | IC50 | = | 12000.0 | nM | 4.92 | In vitro inhibition of thromboxane A2 production in rat platelet-rich plasma. | 2724303 |
| Homo sapiens | IC50 | = | 97000.0 | nM | 4.01 | Inhibition of ADP-induced platelet aggregation of human PRP without pig aortal m... | 1311763 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 2724303 | 10.1021/jm00126a031 | Rattus norvegicus | 9 |
| 1311763 | 10.1021/jm00082a002 | Mus musculus | 9 |
| 3081722 | 10.1021/jm00153a007 | Thromboxane-A synthase | 6 |
| 2704033 | 10.1021/jm00124a027 | Mus musculus | 5 |
| 2704033 | 10.1021/jm00124a027 | Homo sapiens | 2 |
| 1311763 | 10.1021/jm00082a002 | Homo sapiens | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 9341919 | 10.1021/jm9702793 | Thromboxane-A synthase | 1 |
| - | 10.1016/0960-894X(96)00299-5 | Thromboxane A2 receptor | 1 |
| - | 10.1016/0960-894X(96)00299-5 | Thromboxane-A synthase | 1 |
| 3081722 | 10.1021/jm00153a007 | Prostacyclin synthase | 1 |
| 3081722 | 10.1021/jm00153a007 | Prostaglandin G/H synthase (cyclooxygenase) | 1 |
| 3081722 | 10.1021/jm00153a007 | Cytochrome P450 11B1, mitochondrial | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine