Compound Detail
CHEMBL3544988
DAPRODUSTAT 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL3544988 |
| Name | DAPRODUSTAT |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RUEYEZADQJCKGV-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
9
Publications
4
Known Names
5
Indications
1
Mechanisms
Molecular Properties
393.4
MW (Da)
1.26
ALogP
5
HBA
2
HBD
124.1
PSA (Ų)
0.68
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2023 |
| Availability | Discontinued |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Hypoxia-inducible factor prolyl hydroxylase inhibitor | INHIBITOR | Hypoxia-inducible factor prolyl hydroxylase | ✓ | ✓ |
Indications
Anemia Anemia Renal Insufficiency, Chronic Peripheral Vascular Diseases Wounds and Injuries
ATC Classification
B03XA07
daprodustat
Level 1: BLOOD AND BLOOD FORMING ORGANS
Level 2: ANTIANEMIC PREPARATIONS
Drug Warnings
Black Box Warning
General Warning
Activity Summary
IC50 2 meas. best 7.17
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Egl nine homolog 1 CHEMBL5697 | IC50 | 7.17 | 7.17 | 67.0 | 1 |
| Hypoxia-inducible factor 1-alpha inhibitor CHEMBL5909 | IC50 | 4.68 | 4.68 | 21000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| T1/2 | 2.7 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Egl nine homolog 1 | IC50 | = | 67.0 | nM | 7.17 | Inhibition of N-terminal His tagged PHD2 (181 to 426 residues) (unknown origin) ... | 34029087 |
| Hypoxia-inducible factor 1-alpha inhibitor | IC50 | = | 21000.0 | nM | 4.68 | Inhibition of FIH (unknown origin) by solid-phase extraction coupled to MS based... | 34029087 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.1039/C6MD00240D | Homo sapiens | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 29681433 | 10.1016/j.bmcl.2018.04.039 | Homo sapiens | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| 34029087 | 10.1021/acs.jmedchem.1c00415 | Egl nine homolog 1 | 1 |
| 34029087 | 10.1021/acs.jmedchem.1c00415 | Hypoxia-inducible factor 1-alpha inhibitor | 1 |
Data from ChEMBL 36 via Core Engine