Molecule Details
InChIKeyCUABMPOJOBCXJI-UHFFFAOYSA-N
Compound NameRemibrutinib
Canonical SMILESC=CC(=O)N(C)CCOc1c(N)ncnc1-c1cc(F)cc(NC(=O)c2ccc(C3CC3)cc2F)c1C
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)3
Pfam Stratification Homologous
Avg pChEMBL7.41
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB16852
Drug NameRemibrutinib
CAS Number1787294-07-8
Groups approved investigational
ATC Codes L04AA60
DescriptionRemibrutinib is a selective Bruton's tyrosine kinase inhibitor. The FDA approved remibrutinib on September 30, 2025 as the only oral, targeted treatment for chronic spontaneous urticaria.[L54101] Bruton's tyrosine kinase plays a role in B cell receptor and Fc receptor signalling, releasing histamine...

Categories: Antineoplastic and Immunomodulating Agents BCRP/ABCG2 Inhibitors BSEP/ABCB11 Inhibitors Bruton's Tyrosine Kinase Inhibitors Bruton's tyrosine kinase (BTK) inhibitors Cytochrome P-450 CYP1A2 Inducers Cytochrome P-450 CYP1A2 Inducers (strength unknown) Cytochrome P-450 CYP1A2 Inhibitors Cytochrome P-450 CYP1A2 Inhibitors (strength unknown) Cytochrome P-450 CYP2B6 Inducers Cytochrome P-450 CYP2B6 Inducers (strength unknown) Cytochrome P-450 CYP2B6 Inhibitors Cytochrome P-450 CYP2B6 Inhibitors (strength unknown) Cytochrome P-450 CYP2C19 Inhibitors Cytochrome P-450 CYP2C19 inhibitors (strength unknown) Cytochrome P-450 CYP2C8 Inhibitors Cytochrome P-450 CYP2C8 Inhibitors (strength unknown) Cytochrome P-450 CYP2C9 Inducers Cytochrome P-450 CYP2C9 Inducers (strength unknown) Cytochrome P-450 CYP2C9 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors (strength unknown) Cytochrome P-450 CYP2D6 Inhibitors Cytochrome P-450 CYP2D6 Inhibitors (strength unknown) Cytochrome P-450 CYP3A Inducers Cytochrome P-450 CYP3A Inhibitors Cytochrome P-450 CYP3A Substrates Cytochrome P-450 CYP3A4 Inducers Cytochrome P-450 CYP3A4 Inducers (strength unknown) Cytochrome P-450 CYP3A4 Inhibitors Cytochrome P-450 CYP3A4 Inhibitors (strength unknown) Cytochrome P-450 CYP3A4 Substrates Cytochrome P-450 CYP3A5 Inducers Cytochrome P-450 CYP3A5 Inducers (strength unknown) Cytochrome P-450 CYP3A5 Inhibitors Cytochrome P-450 CYP3A5 Inhibitors (strength unknown) Cytochrome P-450 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Cytochrome P-450 Substrates Enzyme Inhibitors Immunosuppressive Agents Kinase Inhibitor MATE 1 Inhibitors MATE inhibitors OAT1/SLC22A6 inhibitors OAT3/SLC22A8 Inhibitors OATP1B1/SLCO1B1 Inhibitors OATP1B3 inhibitors OCT1 inhibitors OCT2 Inhibitors P-glycoprotein inhibitors P-glycoprotein substrates Protein Kinase Inhibitors Selective Immunosuppressants
Cross-references: BindingDB: 259407 CHEMBL4483575 ChemSpider: 78317000 RxCUI: 2724365
Target Activities (3)
Target Gene Organism Category Pfam pChEMBL Type Source
Q06187 BTK Homo sapiens Human PF00779 PF00169 PF07714 PF00017 PF00018 9.0 IC50 ChEMBL;BindingDB
P42680 TEC Homo sapiens Human PF00779 PF00169 PF07714 PF00017 PF00018 7.0 Kd ChEMBL;BindingDB
P51813 BMX Homo sapiens Human PF00779 PF00169 PF07714 PF00017 6.3 Kd ChEMBL;BindingDB
DrugBank Target Actions (26)
Target Gene Target Name Action Type
P05177 CYP1A2 Cytochrome P450 1A2 inducer enzymes
P08684 CYP3A4 Cytochrome P450 3A4 inducer enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inducer enzymes
P20813 CYP2B6 Cytochrome P450 2B6 inducer enzymes
P20815 CYP3A5 Cytochrome P450 3A5 inducer enzymes
P05177 CYP1A2 Cytochrome P450 1A2 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 inhibitor enzymes
P10632 CYP2C8 Cytochrome P450 2C8 inhibitor enzymes
P10635 CYP2D6 Cytochrome P450 2D6 inhibitor enzymes
P11712 CYP2C9 Cytochrome P450 2C9 inhibitor enzymes
P20813 CYP2B6 Cytochrome P450 2B6 inhibitor enzymes
P20815 CYP3A5 Cytochrome P450 3A5 inhibitor enzymes
P33261 CYP2C19 Cytochrome P450 2C19 inhibitor enzymes
P08684 CYP3A4 Cytochrome P450 3A4 substrate enzymes
Q06187 BTK Tyrosine-protein kinase BTK inhibitor targets
O15244 SLC22A2 Solute carrier family 22 member 2 inhibitor transporters
O15245 SLC22A1 Solute carrier family 22 member 1 inhibitor transporters
O95342 ABCB11 Bile salt export pump inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
Q4U2R8 SLC22A6 Solute carrier family 22 member 6 inhibitor transporters
Q8TCC7 SLC22A8 Organic anion transporter 3 inhibitor transporters
Q96FL8 SLC47A1 Multidrug and toxin extrusion protein 1 inhibitor transporters
Q9NPD5 SLCO1B3 Solute carrier organic anion transporter family member 1B3 inhibitor transporters
Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 inhibitor transporters
Q9Y6L6 SLCO1B1 Solute carrier organic anion transporter family member 1B1 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters