Remibrutinib (LOU064) structure
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Common Name | Remibrutinib (LOU064) | ||
|---|---|---|---|---|
| CAS Number | 1787294-07-8 | Molecular Weight | 507.53 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C27H27F2N5O3 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Remibrutinib (LOU064)Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2]. |
| Name | Remibrutinib |
|---|
| Description | Remibrutinib, is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood[1]. Remibrutinib has the potential for Chronic urticaria (CU) treatment[2]. |
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| Related Catalog | |
| Target |
IC50: 1 nM (BTK)[1] |
| In Vitro | In a biochemical enzyme assay,Remibrutinib (example 6) inhibits Btk enzymatic activity with an IC50 value of 1 nM[1]. In vitro B cell activation assay, Remibrutinib inhibits Btk enzymatic activity in blood with an IC50 value of 0.023 μM, the whole blood is collected from the abdominal aorta of anaesthetized adult male Lewis rats[1]. |
| References |
[1]. Daniela Angst, et al. Novel amino pyrimidine derivatives. Patent WO2015079417A1. [2]. Kolkhir P, et al. New treatments for chronic urticaria. Ann Allergy Asthma Immunol. 2019 Aug 23. |
| Molecular Formula | C27H27F2N5O3 |
|---|---|
| Molecular Weight | 507.53 |
| InChIKey | CUABMPOJOBCXJI-UHFFFAOYSA-N |
| SMILES | C=CC(=O)N(C)CCOc1c(N)ncnc1-c1cc(F)cc(NC(=O)c2ccc(C3CC3)cc2F)c1C |
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Name: Inhibition of Btk Enzymatic Activity Assay from US Patent US11673868: "Amino pyrimidi...
Source: BindingDB
Target: N/A
External Id: BindingDB_11294_1
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Name: Inhibition of CD69 expression on CD19 positive B cells in anti-IgD stimulated human w...
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133804
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Name: Metabolic stability in human liver microsomes assessed as intrinsic clearance
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133805
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Name: Metabolic stability in rat liver microsomes assessed as intrinsic clearance
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133806
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Name: Inhibition of BTK (unknown origin) assessed as log ratio of Kinact/Ki
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL5133802
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Name: Clearance in iv dosed Sprague-Dawley rat
Source: ChEMBL
Target: N/A
External Id: CHEMBL5133803
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Name: Inhibition of BTK (unknown origin)
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL5133797
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Name: Inhibition of Btk Enzymatic Activity from US Patent US10457647: "Amino pyrimidine der...
Source: BindingDB
Target: N/A
External Id: BindingDB_8763_1
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Name: Intrinsic clearance in rat liver microsomes
Source: ChEMBL
Target: N/A
External Id: CHEMBL4358490
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Name: Inhibition of BTK in human B cells assessed as reduction in anti-IgM/IL4-stimulated C...
Source: ChEMBL
Target: Tyrosine-protein kinase BTK
External Id: CHEMBL4358489
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