InChIKey	DKULOVKANLVDEA-UHFFFAOYSA-N
Canonical SMILES	NS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1
Clinical Status	Data-mined Candidate
Targets (Human+Pathogen)	2
Pfam Stratification	Homologous
Avg pChEMBL	7.24
Source	ChEMBL;BindingDB

DrugBank ID	DB15059
Drug Name	Aprocitentan
CAS Number	1103522-45-7
Groups	approved
ATC Codes	C02KN01
Description	Aprocitentan is a dual antagonist of endothelin receptors A and B used for treatment-resistant hypertension. It is the active metabolite of [macitentan]. Approximately 10-15% of patients with hypertension have resistant hypertension, defined as uncontrolled high blood pressure despite the combined u...

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Categories: Amides Antihypertensive Agents BCRP/ABCG2 Inhibitors BCRP/ABCG2 Substrates BSEP/ABCB11 Inhibitors Cytochrome P-450 CYP2C18 Inhibitors Cytochrome P-450 CYP2C18 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 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors (strength unknown) Cytochrome P-450 CYP3A Inducers Cytochrome P-450 CYP3A Inhibitors 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 Enzyme Inducers Cytochrome P-450 Enzyme Inhibitors Endothelin Receptor Antagonists P-glycoprotein substrates Sulfones Sulfur Compounds UGT1A1 Inhibitors UGT1A1 Substrates UGT2B7 Inhibitors UGT2B7 substrates

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Cross-references: BindingDB: 50395672 ChEBI: 76609 CHEMBL2165326 ChemSpider: 25027753 RxCUI: 2679059 Wikipedia: Aprocitentan ZINC: ZINC000095553608