AZD0284   Click here for help

GtoPdb Ligand ID: 11711

Synonyms: AZD-0284 | compound 20 [PMID: 34464130]
PDB Ligand Immunopharmacology Ligand
Compound class: Synthetic organic
Comment: AZD0284 is an orally bioavailable inverse agonist of retinoic acid receptor-related orphan receptor C2 (NR1F3; RORγt) [1]. It is proposed for anti-inflammatory potential, principally as a treatment for psoriasis.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 2
Rotatable bonds 8
Topological polar surface area 112.16
Molecular weight 524.08
XLogP 3.2
No. Lipinski's rules broken 0
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Canonical SMILES O=C([C@@H]1N(Cc2c1ccc(c2)S(=O)(=O)C)C(=O)C)Nc1ccc(cc1)C(C(F)(F)F)(C(F)(F)F)O
Isomeric SMILES FC(F)(F)C(O)(C(F)(F)F)c1ccc(cc1)NC(=O)[C@@H]1N(Cc2c1ccc(c2)S(=O)(=O)C)C(=O)C
InChI InChI=1S/C21H18F6N2O5S/c1-11(30)29-10-12-9-15(35(2,33)34)7-8-16(12)17(29)18(31)28-14-5-3-13(4-6-14)19(32,20(22,23)24)21(25,26)27/h3-9,17,32H,10H2,1-2H3,(H,28,31)/t17-/m1/s1
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Summary of Clinical Use Click here for help
AZD0284 was initiated in early clinical studies, with the main indication being plaque psoriasis.
Clinical Trials
Clinical Trial ID Title Type Source Comment References
NCT03310320 Study to Determine if AZD0284 is Effective and Safe in Treating Plaque Psoriasis Phase 1 Interventional AstraZeneca
NCT03029741 Bioavailability of AZD0284 and IV Microtracer Study Phase 1 Interventional AstraZeneca
NCT02976831 Study to Assess the Safety, Tolerability and Pharmacokinetics and Pharmacodynamics of AZD0284 in Healthy Subjects Phase 1 Interventional AstraZeneca