Compound Detail
CHEMBL4085457
RITLECITINIB 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL4085457 |
| Name | RITLECITINIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | CBRJPFGIXUFMTM-WDEREUQCSA-N |
| Therapeutic | ✓ Yes |
12
Targets
44
Activities
2
Assay Types
23
PK Parameters
20
Publications
2
Known Names
13
Indications
2
Mechanisms
Molecular Properties
285.4
MW (Da)
1.94
ALogP
4
HBA
2
HBD
73.9
PSA (Ų)
0.85
QED
0
Ro5 Violations
3
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 |
|---|---|---|---|---|
| Tyrosine-protein kinase JAK3 inhibitor | INHIBITOR | Tyrosine-protein kinase JAK3 | ✓ | ✓ |
| TEC family kinase inhibitor | INHIBITOR | TEC family kinase | ✓ | ✓ |
Indications
Alopecia Areata Vitiligo Alopecia Arthritis, Rheumatoid Celiac Disease Colitis, Ulcerative Crohn Disease Diabetes Mellitus, Type 1 Keloid Mycosis Fungoides Sezary Syndrome Kidney Diseases Liver Diseases
ATC Classification
L04AF08
ritlecitinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: IMMUNOSUPPRESSANTS
Activity Summary
IC50 37 meas. best 9.52
Ki 7 meas. best 7.57
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Tyrosine-protein kinase JAK3 CHEMBL2148 | IC50 | 9.52 | 8.027 | 0.3 | 23 |
| U-937 CHEMBL612794 | IC50 | 7.71 | 7.555 | 19.5 | 2 |
| Tyrosine-protein kinase ITK/TSK CHEMBL2959 | Ki | 7.57 | 7.57 | 26.9 | 1 |
| BaF3 CHEMBL614524 | IC50 | 7.55 | 7.55 | 28.1 | 1 |
| CD4+ve Th CHEMBL613544 | IC50 | 7.32 | 7.32 | 48.0 | 1 |
| Tyrosine-protein kinase TXK CHEMBL4367 | Ki | 6.88 | 6.88 | 131.0 | 1 |
| Tyrosine-protein kinase Tec CHEMBL4246 | IC50 | 6.81 | 6.52 | 155.0 | 2 |
| Tyrosine-protein kinase TXK CHEMBL4367 | IC50 | 6.71 | 6.71 | 193.0 | 1 |
| Cytoplasmic tyrosine-protein kinase BMX CHEMBL3834 | Ki | 6.26 | 6.26 | 545.0 | 1 |
| Cytoplasmic tyrosine-protein kinase BMX CHEMBL3834 | IC50 | 6.22 | 6.22 | 606.0 | 1 |
| Tyrosine-protein kinase BTK CHEMBL5251 | IC50 | 6.22 | 6.22 | 607.0 | 1 |
| Tyrosine-protein kinase Tec CHEMBL4246 | Ki | 6.17 | 6.17 | 679.0 | 1 |
| Tyrosine-protein kinase JAK1 CHEMBL2835 | IC50 | 5.79 | 5.79 | 1640.0 | 2 |
| Tyrosine-protein kinase JAK3 CHEMBL2148 | Ki | 5.2 | 5.2 | 6310.0 | 1 |
| Tyrosine-protein kinase ITK/TSK CHEMBL2959 | IC50 | 5.07 | 5.07 | 8510.0 | 1 |
| Tyrosine-protein kinase Blk CHEMBL2250 | IC50 | 4.72 | 4.72 | 19000.0 | 1 |
| Receptor tyrosine-protein kinase erbB-4 CHEMBL3009 | IC50 | 4.6 | 4.6 | 25200.0 | 1 |
| Tyrosine-protein kinase Blk CHEMBL2250 | Ki | 4.49 | 4.49 | 32400.0 | 1 |
| Tyrosine-protein kinase BTK CHEMBL5251 | Ki | 4.21 | 4.21 | 62300.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 48.0 | mL.min-1.kg-1 | Mus musculus |
| CL | 53.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 42.0 | mL.min-1.kg-1 | Macaca mulatta |
| CL | 8.6 | mL.min-1.kg-1 | Canis lupus familiaris |
| F | 62.0 | % | Mus musculus |
| F | 85.0 | % | Rattus norvegicus |
| F | 56.0 | % | Macaca mulatta |
| F | 109.0 | % | Canis lupus familiaris |
| T1/2 | 6.0 | hr | Homo sapiens |
| T1/2 | 2.683 | hr | Rattus norvegicus |
| T1/2 | 6.0 | hr | Mus musculus |
| T1/2 | 2.683 | hr | Rattus norvegicus |
| T1/2 | 0.6167 | hr | Macaca mulatta |
| T1/2 | 6.0 | hr | Canis lupus familiaris |
| T1/2 | 6.0 | hr | Homo sapiens |
| T1/2 | 5.517 | hr | Homo sapiens |
| T1/2 | 1.3 | hr | Mus musculus |
| T1/2 | 0.3 | hr | Rattus norvegicus |
| T1/2 | 0.7 | hr | Macaca mulatta |
| T1/2 | 1.1 | hr | Canis lupus familiaris |
| T1/2 | 8.0 | hr | Homo sapiens |
| t1/2 | - | - | - |
| T1/2 | 32.0 | hr | - |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine