Compound Detail
CHEMBL146032
LONAPRISAN 🧪 Phase II
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🧪 Phase II
CC(=O)c1ccc([C@H]2C[C@@]3(C)[C@@H](CC[C@@]3(O)C(F)(F)C(F)(F)F)[C@@H]3CCC4=CC(=O)CCC4=C32)cc1
Basic Information
| ChEMBL ID | CHEMBL146032 |
| Name | LONAPRISAN |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | VHZPUDNSVGRVMB-RXDLHWJPSA-N |
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
5
Known Names
1
Indications
1
Mechanisms
Molecular Properties
508.5
MW (Da)
6.72
ALogP
3
HBA
1
HBD
54.4
PSA (Ų)
0.36
QED
2
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Progesterone receptor antagonist | ANTAGONIST | Progesterone receptor | ✓ | ✓ |
Indications
Breast Neoplasms
Activity Summary
IC50 4 meas. best 7.8
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glucocorticoid receptor CHEMBL3144 | IC50 | 7.8 | 7.8 | 16.0 | 1 |
| Androgen receptor CHEMBL1871 | IC50 | 7.27 | 7.27 | 54.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Glucocorticoid receptor | IC50 | = | 16.0 | nM | 7.8 | In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing ... | 11150172 |
| Androgen receptor | IC50 | = | 54.0 | nM | 7.27 | In vitro antagonist potency in transactivation assay in CV-1 cells expressing an... | 11150172 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 11150172 | 10.1021/jm001000c | Progesterone receptor | 10 |
| 11150172 | 10.1021/jm001000c | Androgen receptor | 4 |
| 11150172 | 10.1021/jm001000c | Glucocorticoid receptor | 4 |
| 11150172 | 10.1021/jm001000c | Estrogen receptor | 3 |
| 11150172 | 10.1021/jm001000c | Unchecked | 1 |
Data from ChEMBL 36 via Core Engine