Compound Detail
CHEMBL4072756
AZD-5423 🧪 Phase II
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🧪 Phase II
COc1cccc([C@@H](Oc2ccc3c(cnn3-c3ccc(F)cc3)c2)[C@H](C)NC(=O)C(F)(F)F)c1
Basic Information
| ChEMBL ID | CHEMBL4072756 |
| Name | AZD-5423 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | FCNQMDSJHADDFT-WNSKOXEYSA-N |
3
Targets
5
Activities
1
Assay Types
7
PK Parameters
10
Publications
3
Known Names
2
Indications
1
Mechanisms
Molecular Properties
487.4
MW (Da)
5.36
ALogP
5
HBA
1
HBD
65.4
PSA (Ų)
0.36
QED
1
Ro5 Violations
7
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glucocorticoid receptor modulator | MODULATOR | Glucocorticoid receptor | ✓ | ✓ |
Indications
Asthma Pulmonary Disease, Chronic Obstructive
Activity Summary
IC50 5 meas. best 10.31
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glucocorticoid receptor CHEMBL2034 | IC50 | 10.31 | 9.72 | 0.0 | 3 |
| Glucocorticoid receptor CHEMBL3368 | IC50 | 9.85 | 9.85 | 0.1 | 1 |
| Progesterone receptor CHEMBL208 | IC50 | 5.75 | 5.75 | 1760.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 8774.1 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 38.0 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 122.0 | nM | Rattus norvegicus |
| F | 37.0 | % | Rattus norvegicus |
| MRT | 1.5 | hr | Rattus norvegicus |
| T1/2 | 4.7 | hr | Rattus norvegicus |
| T1/2 | 7.5 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Glucocorticoid receptor | IC50 | = | 0.049 | nM | 10.31 | Transrepression of glucocorticoid receptor in PMA-stimulated human ChaGoK1 cells... | 28937774 |
| Glucocorticoid receptor | IC50 | = | 0.14 | nM | 9.85 | Transrepression of glucocorticoid receptor in Wistar rat PBMC assessed as inhibi... | 28937774 |
| Glucocorticoid receptor | IC50 | = | 0.16 | nM | 9.8 | Transrepression of glucocorticoid receptor in human PBMC assessed as inhibition ... | 28937774 |
| Glucocorticoid receptor | IC50 | = | 0.9 | nM | 9.05 | Displacement of fluormone labelled GS Red from human recombinant glucocorticoid ... | 28937774 |
| Progesterone receptor | IC50 | = | 1760.0 | nM | 5.75 | Displacement of fluormone labelled PL Red from human recombinant progesterone re... | 28937774 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Rattus norvegicus | 9 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Glucocorticoid receptor | 7 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Lung | 6 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | ADMET | 2 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | No relevant target | 2 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Mineralocorticoid receptor | 1 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Androgen receptor | 1 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Estrogen receptor | 1 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Estrogen receptor beta | 1 |
| 28937774 | 10.1021/acs.jmedchem.7b01215 | Progesterone receptor | 1 |
Data from ChEMBL 36 via Core Engine