Compound Detail
CHEMBL2105773
PRAZARELIX ACETATE Enter ChEMBL ID:
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CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O.CC(=O)O
Basic Information
| ChEMBL ID | CHEMBL2105773 |
| Name | PRAZARELIX ACETATE |
| Phase | Preclinical |
| Structure Type | BOTH |
| InChI Key | UYXOLEHMGDKCEI-OKBORMFFSA-N |
| Parent Compound | CHEMBL409018 |
| Active Moiety | CHEMBL409018 |
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
7
Publications
5
Known Names
Molecular Properties
1613.3
MW (Da)
Drug Information
| Molecule Type | Protein |
| Chirality | Single Enantiomer |
Activity Summary
IC50 4 meas. best 8.87
Kd 1 meas. best 8.8
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor CHEMBL1855 | IC50 | 8.87 | 8.6267 | 1.4 | 3 |
| Gonadotropin-releasing hormone receptor CHEMBL3066 | IC50 | 8.85 | 8.85 | 1.4 | 1 |
| Gonadotropin-releasing hormone receptor CHEMBL1855 | Kd | 8.8 | 8.8 | 1.6 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | IC50 | = | 1.36 | nM | 8.87 | Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibit... | 17402723 |
| Gonadotropin-releasing hormone receptor | IC50 | = | 1.4 | nM | 8.85 | Antagonism of GnRH response in HEK293 cells expressing human GnRH receptor | 16033265 |
| Gonadotropin-releasing hormone receptor | IC50 | = | 1.4 | nM | 8.85 | Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibitio... | 17402723 |
| Gonadotropin-releasing hormone receptor | Kd | = | 1.585 | nM | 8.8 | Competitive antagonism of GnRH-induced response in the reporter gene assay | 11462984 |
| Gonadotropin-releasing hormone receptor | IC50 | = | 6.9 | nM | 8.16 | Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293... | 11462984 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 11462984 | 10.1021/jm0003900 | Rattus norvegicus | 5 |
| 11462984 | 10.1021/jm0003900 | Gonadotropin-releasing hormone receptor | 2 |
| 17402723 | 10.1021/jm0613931 | Gonadotropin-releasing hormone receptor | 2 |
| 17402723 | 10.1021/jm0613931 | Rattus norvegicus | 2 |
| 16033265 | 10.1021/jm050134t | Gonadotropin-releasing hormone receptor | 1 |
| 17402723 | 10.1021/jm0613931 | Unchecked | 1 |
| 17402723 | 10.1021/jm0613931 | No relevant target | 1 |
Data from ChEMBL 36 via Core Engine