Compound Detail
CHEMBL2325741
CAPIVASERTIB 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL2325741 |
| Name | CAPIVASERTIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | JDUBGYFRJFOXQC-KRWDZBQOSA-N |
| Therapeutic | ✓ Yes |
58
Targets
103
Activities
3
Assay Types
17
PK Parameters
20
Publications
6
Known Names
19
Indications
1
Mechanisms
Molecular Properties
428.9
MW (Da)
2.10
ALogP
6
HBA
4
HBD
120.2
PSA (Ų)
0.48
QED
0
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2023 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serine/threonine-protein kinase AKT inhibitor | INHIBITOR | Serine/threonine-protein kinase AKT | ✓ | ✓ |
Indications
Breast Neoplasms Breast Neoplasms Neoplasms Neoplasms Prostatic Neoplasms, Castration-Resistant Adenocarcinoma Carcinoma, Non-Small-Cell Lung Carcinoma, Squamous Cell Lymphoma, Follicular Meningioma Multiple Myeloma Prostatic Neoplasms Stomach Neoplasms Stomach Neoplasms Triple Negative Breast Neoplasms Hematologic Neoplasms Hereditary Breast and Ovarian Cancer Syndrome Uterine Cervical Neoplasms Uterine Neoplasms
ATC Classification
L01EX27
capivasertib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 66 meas. best 9.05
Kd 28 meas. best 6.62
EC50 9 meas. best 6.72
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| RAC-alpha serine/threonine-protein kinase CHEMBL4282 | IC50 | 9.05 | 8.3642 | 0.9 | 12 |
| Serine/threonine-protein kinase AKT CHEMBL2111353 | IC50 | 8.52 | 8.52 | 3.0 | 1 |
| RAC-beta serine/threonine-protein kinase CHEMBL2431 | IC50 | 8.3 | 8.15 | 5.0 | 6 |
| Unchecked CHEMBL612545 | IC50 | 8.22 | 6.6277 | 6.0 | 13 |
| RAC-gamma serine/threonine-protein kinase CHEMBL4816 | IC50 | 8.15 | 8.12 | 7.0 | 5 |
| Rho-associated protein kinase 2 CHEMBL2973 | IC50 | 7.25 | 7.25 | 56.0 | 1 |
| LNCaP CHEMBL612518 | IC50 | 6.75 | 6.545 | 178.0 | 2 |
| ZR-75-1 CHEMBL614393 | EC50 | 6.72 | 6.72 | 191.0 | 2 |
| cAMP-dependent protein kinase catalytic subunit beta CHEMBL2918 | Kd | 6.62 | 6.62 | 239.0 | 1 |
| cGMP-dependent protein kinase 1 CHEMBL4273 | Kd | 6.53 | 6.53 | 297.0 | 1 |
| Rho-associated protein kinase 2 CHEMBL2973 | Kd | 6.49 | 6.49 | 324.0 | 1 |
| LIM domain kinase 1 CHEMBL3836 | Kd | 6.45 | 6.45 | 357.0 | 1 |
| cAMP-dependent protein kinase catalytic subunit alpha CHEMBL4101 | Kd | 6.41 | 6.41 | 387.0 | 1 |
| Rho-associated protein kinase 1 CHEMBL3231 | IC50 | 6.33 | 6.33 | 470.0 | 1 |
| Dual specificity protein kinase CLK1 CHEMBL4224 | Kd | 6.32 | 6.32 | 475.0 | 1 |
| T47D CHEMBL614361 | EC50 | 6.32 | 6.32 | 475.0 | 2 |
| LIM domain kinase 2 CHEMBL5932 | Kd | 6.32 | 6.32 | 477.0 | 1 |
| Dual specificity protein kinase CLK4 CHEMBL4203 | Kd | 6.29 | 6.29 | 513.0 | 1 |
| MCF7 CHEMBL387 | EC50 | 6.26 | 6.26 | 555.0 | 1 |
| Rho-associated protein kinase 1 CHEMBL3231 | Kd | 6.15 | 6.15 | 706.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 6.06 | 6.06 | 879.0 | 1 |
| AN3-CA CHEMBL1075392 | EC50 | 6.06 | 6.06 | 869.0 | 2 |
| Fibroblast growth factor receptor 1 CHEMBL3650 | Kd | 6.06 | 6.06 | 865.0 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | Kd | 5.96 | 5.96 | 1107.0 | 1 |
| Serine/threonine-protein kinase N1 CHEMBL3384 | Kd | 5.8 | 5.8 | 1577.0 | 1 |
| BT-474 CHEMBL614529 | EC50 | 5.79 | 5.79 | 1605.0 | 1 |
| Protein kinase C alpha type CHEMBL299 | Kd | 5.76 | 5.76 | 1733.0 | 1 |
| 5'-AMP-activated protein kinase catalytic subunit alpha-1 CHEMBL4045 | Kd | 5.74 | 5.74 | 1821.0 | 1 |
| Mitogen-activated protein kinase kinase kinase kinase 3 CHEMBL5432 | Kd | 5.72 | 5.72 | 1900.0 | 1 |
| Mitogen-activated protein kinase kinase kinase 11 CHEMBL2708 | Kd | 5.7 | 5.7 | 1999.0 | 1 |
| Serine/threonine-protein kinase D3 CHEMBL2595 | Kd | 5.66 | 5.66 | 2207.0 | 1 |
| Serine/threonine-protein kinase D2 CHEMBL4900 | Kd | 5.65 | 5.65 | 2246.0 | 1 |
| SARS-CoV-2 CHEMBL4303835 | IC50 | 5.63 | 5.63 | 2330.0 | 1 |
| Protein kinase C beta type CHEMBL3045 | Kd | 5.61 | 5.61 | 2431.0 | 1 |
| 5'-AMP-activated protein kinase subunit gamma-1 CHEMBL2393 | Kd | 5.61 | 5.61 | 2445.0 | 1 |
| RAC-beta serine/threonine-protein kinase CHEMBL2431 | Kd | 5.6 | 5.6 | 2490.0 | 1 |
| 5'-AMP-activated protein kinase subunit gamma-2 CHEMBL2453 | Kd | 5.57 | 5.57 | 2711.0 | 1 |
| NCI-H1975 CHEMBL614348 | IC50 | 5.57 | 5.325 | 2700.0 | 2 |
| Protein kinase C delta type CHEMBL2996 | Kd | 5.55 | 5.55 | 2809.0 | 1 |
| RAC-alpha serine/threonine-protein kinase CHEMBL4282 | Kd | 5.41 | 5.41 | 3883.0 | 1 |
| HaCaT CHEMBL614392 | IC50 | 5.38 | 5.38 | 4200.0 | 1 |
| MCF7 CHEMBL387 | IC50 | 5.38 | 5.38 | 4200.0 | 1 |
| Protein kinase C theta type CHEMBL3920 | Kd | 5.37 | 5.37 | 4246.0 | 1 |
| OVCAR-8 CHEMBL612555 | IC50 | 5.35 | 5.245 | 4480.0 | 2 |
| Beta-adrenergic receptor kinase 1 CHEMBL4079 | Kd | 5.31 | 5.31 | 4859.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 5.28 | 5.21 | 5200.0 | 2 |
| HCT-116 CHEMBL394 | IC50 | 5.28 | 5.28 | 5200.0 | 1 |
| SK-OV-3 CHEMBL614925 | IC50 | 5.2 | 5.2 | 6320.0 | 1 |
| HepG2 CHEMBL395 | IC50 | 5.17 | 5.17 | 6700.0 | 1 |
| AGS CHEMBL613860 | IC50 | 5.02 | 5.02 | 9600.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 22.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 95.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 207.0 | mL.min-1.kg-1 | Mus musculus |
| CL | 14.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.g-1 | Mus musculus |
| F | 37.0 | % | Canis lupus familiaris |
| F | 13.0 | % | Rattus norvegicus |
| F | 86.0 | % | Mus musculus |
| Fu | 0.192 | - | Canis lupus familiaris |
| Fu | 0.235 | - | Rattus norvegicus |
| Fu | 0.143 | - | Mus musculus |
| Fu | 0.223 | - | Homo sapiens |
| T1/2 | 1.7 | hr | Canis lupus familiaris |
| T1/2 | 0.5 | hr | Rattus norvegicus |
| T1/2 | 0.2 | hr | Mus musculus |
| T1/2 | 0.55 | hr | Homo sapiens |
| T1/2 | 1.45 | hr | Mus musculus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine