Silmitasertib
Highest phase reached
Phase 2
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 2
- Drug type
- Small molecule
- Drug name
- Silmitasertib
- Molecular weight
- 349.78
- Structure (SMILES)
- O=C(O)c1ccc2c(c1)nc(Nc1cccc(Cl)c1)c1ccncc12
- benzo c 2 6 naphthyridine 8 carboxylic acid 5 3 chlorophenyl amino
- BENZO(C)-2,6-NAPHTHYRIDINE-8-CARBOXYLIC ACID, 5-((3-CHLOROPHENYL)AMINO)-
- cx 4945
- CX 4945
- cx 4945 free acid
- cx 4945 silmitasertib
- Cx-4945
- CX-4945
- CX-4945 (Influenza virus domain)
- CX-4945 (SARS-CoV-2 domain)
- CX-4945 (SILMITASERTIB)
- Cx-4945 free acid
- CX-4945 FREE ACID
- cx4945
- CX4945
- silmitasertib
- Silmitasertib
- SILMITASERTIB
- SILMITASERTIB (CX-4945)
- silmitasertib [INN]
- Silmitasertib [WHO-DD]
- silmitasertib cx 4945
- silmitasertib inn
- silmitasertib who dd
- CAS registry numbers
- 1009820-21-6
- ChEMBL ID
- CHEMBL1230165
- InChIKey
- MUOKSQABCJCOPU-UHFFFAOYSA-N
- PubChem compound IDs
- 24748573
- FDA ingredient codes (UNII)
- C6RWP0N0L2
- Patents
- 0
- Designations
- 2
- First in class
- No
- Fast track
- No
- Breakthrough designation
- No
- Orphan designation
- No
- Priority review
- No
- Orphan exclusivity
- No
- Accelerated approval
- No
- Pharmacology name
- silmitasertib
- Type
- Synthetic organic
- Drug name stem
- -sertib
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- death associated protein kinase 3
- Gene symbol
- DAPK3
- Protein identifier
- O43293
- Median affinity
- 7.77
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- Pim-1 proto-oncogene, serine/threonine kinase
- Gene symbol
- PIM1
- Protein identifier
- P11309
- Median affinity
- 6.67
- Affinity units
- pIC50
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- casein kinase 2, alpha prime polypeptide subunit
- Gene symbol
- CSNK2A2
- Protein identifier
- P19784
- Median affinity
- 9
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- casein kinase 2, alpha 1 polypeptide subunit
- Gene symbol
- CSNK2A1
- Protein identifier
- P68400
- Median affinity
- 9
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- homeodomain interacting protein kinase 3
- Gene symbol
- HIPK3
- Protein identifier
- Q9H422
- Median affinity
- 7.35
- Affinity units
- pIC50
- Mechanism
- Casein kinase II alpha inhibitor
- Action type
- Inhibitor
- Target
- Casein kinase II subunit alpha
- Protein identifier
- P68400
Open Targets mechanisms
- Mechanism
- Casein kinase II alpha inhibitor
- Action type
- Inhibitor
- Target
- Casein kinase II subunit alpha
- Condition
- Multiple Myeloma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0001378
- Subject identifier
- D009101
- Condition
- Medulloblastoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0002939
- Subject identifier
- D008527
- Condition
- Carcinoma, Basal Cell
- Highest recorded phase
- 1
- Condition identifier
- EFO:0004193
- Subject identifier
- D002280
- Condition
- Cholangiocarcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005221
- Subject identifier
- D018281
- Condition
- Severe Acute Respiratory Syndrome
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0100096
- Subject identifier
- D045169
- Condition identifier
- EFO_0001378
- Highest recorded phase
- 1
- Condition identifier
- EFO_0002939
- Condition identifier
- EFO_0004193
- Highest recorded phase
- 1
- Condition identifier
- EFO_0005221
- Condition identifier
- EFO_0007224
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0009693
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0015564
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0019087
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0020804
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0100096
- Highest recorded phase
- 2
- NCT01199718
- NCT02128282
- NCT03897036
- NCT03904862
- NCT04663737
- NCT04668209
- NCT05817708
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 2
- Polar surface area
- 75.11
- Calculated partition coefficient (ALogP)
- 4.88
- Calculated partition coefficient (XLogP)
- 4.4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 3
- Heavy atoms
- 25
- Molecular formula
- C19H12ClN3O2
- Monoisotopic mass
- 349.0618043
- Natural product
- No
- Recorded assays
- 2,298
- Active assays
- 439
- Confirmatory
- Other
- Screening
Solubility
- Median
- 277,100
- Mean
- 277,100
- Minimum
- 277,100
- Maximum
- 277,100
- Unit
- nM
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- Solubility
Oral bioavailability
- Median
- 48
- Mean
- 39.6667
- Minimum
- 20
- Maximum
- 51
- Unit
- %
- Assays
- 3
- Standard deviation
- 17.0978
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
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- A Phase I, Randomized, Modified Single-blind, Active-controlled (Infants Only), Four-stage, Step-down, Comparative, Multi-center Study
- A Safety and Immunogenicity Study of 3 Doses of Opal Immunotherapy in HIV Infected People
- A Sourcing Study to Collect Human Blood Samples From Healthy Adults
- A Study in Healthy Men to Test if Taking Different Formulations of BI 1358894 With or Without Food Influences the Amount of BI 1358894 in the Blood
- A Study of a Quadrivalent Meningococcal Tetanus Protein Conjugate Vaccine in Infants and Toddlers
- A Study of Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (D/C/F/TAF) Evaluated as a Fixed Dose Combination Regimen in Participants Switching From an Integrase Inhibitor Who Have Experienced Rapid Weight Gain
- A Study of LY3202626 in Healthy Participants and Participants With Alzheimer's Disease
- A Study of Silmitasertib (CX-4945) in Healthy Subject
- A Study to Evaluate Efficacy and Safety of Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (D/C/F/TAF) Fixed Dose Combination (FDC) Versus a Regimen Consisting of Darunavir/Cobicistat FDC With Emtricitabine/Tenofovir Disoproxil Fumarate FDC in Treatment-naive HIV Type 1 Infected Subjects
- A Study to Evaluate Safety, Reactogenicity, and Immune Response of GVGH iNTS-TCV Vaccine Against Invasive Nontyphoidal Salmonella and Typhoid Fever
- A Study to Evaluate the Safety and Immunogenicity of a Candidate Ebola Vaccine in Children
- A Study to Provide Continued Access to Study Drug to Children and Adolescents Who Have Completed Clinical Studies Involving Gilead HIV Treatments
- Adherence With Iron Sprinkles Among High-Risk Infants
- Adjunctive Supplementation of Antioxidants (Vitamins E + C) Plus Omega-3 Fatty Acids
- An Italian Observation of Antiretroviral Treatment in Participants Taking Darunavir/ Cobicistat Plus Emtricitabine and Tenofovir Alafenamide Fumarate
In development for (5)
- Basal cell carcinoma Phase 1
- Cholangiocarcinoma Phase 1
- COVID-19 Phase 2
- Medulloblastoma Phase 1
- Plasma cell myeloma Phase 1
Targets (1)
- CSNK2A1 Casein kinase II alpha inhibitor