Compound Detail
CHEMBL292376
TECALCET 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL292376 |
| Name | TECALCET |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | ZVQUCWXZCKWZBP-CQSZACIVSA-N |
1
Targets
2
Activities
1
Assay Types
5
PK Parameters
9
Publications
1
Known Names
Molecular Properties
303.8
MW (Da)
4.63
ALogP
2
HBA
1
HBD
21.3
PSA (Ų)
0.75
QED
0
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Activity Summary
EC50 2 meas. best 7.1
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Extracellular calcium-sensing receptor CHEMBL1878 | EC50 | 7.1 | 6.905 | 80.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 0.022 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 65.0 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 0.01382 | nM | Rattus norvegicus |
| F | 5.0 | % | Rattus norvegicus |
| MRT | 1.74 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Extracellular calcium-sensing receptor | EC50 | = | 80.0 | nM | 7.1 | Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hr... | 23465611 |
| Extracellular calcium-sensing receptor | EC50 | = | 194.0 | nM | 6.71 | Activity at human CaSR expressed in HEK293 cells assessed as calcium release by ... | 19835382 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 19835382 | 10.1021/jm9012278 | Rattus norvegicus | 7 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 6 |
| - | 10.6019/CHEMBL4651402 | Vero C1008 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 15149704 | 10.1016/j.bmcl.2004.03.056 | Extracellular calcium-sensing receptor | 1 |
| 10987436 | 10.1016/s0960-894x(00)00382-6 | Extracellular calcium-sensing receptor | 1 |
| 19835382 | 10.1021/jm9012278 | Extracellular calcium-sensing receptor | 1 |
| 23465611 | 10.1016/j.bmcl.2013.01.078 | Extracellular calcium-sensing receptor | 1 |
| - | 10.6019/CHEMBL3301361 | No relevant target | 1 |
Data from ChEMBL 36 via Core Engine