Obeldesivir
GS-5245 (Obeldesivir), an Oral Prodrug of Nucleoside GS-441524 That Exhibits Antiviral Efficacy in SARS-CoV-2-Infected African Green Monkeys
General
Type : Pro-Drug, Drug, Not AlphaBeta Hydrolase target, Propionate, Triazine, Cyanide
Chemical_Nomenclature : [(2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxyoxolan-2-yl]methyl 2-methylpropanoate
Canonical SMILES : CC(C)C(=O)OC[C@@H]1[C@H]([C@H]([C@](O1)(C#N)C2=CC=C3N2N=CN=C3N)O)O
InChI : InChI=1S\/C16H19N5O5\/c1-8(2)15(24)25-5-10-12(22)13(23)16(6-17,26-10)11-4-3-9-14(18)19-7-20-21(9)11\/h3-4,7-8,10,12-13,22-23H,5H2,1-2H3,(H2,18,19,20)\/t10-,12-,13-,16+\/m1\/s1
InChIKey : YIHPGVCWGSURHO-VSBTWAGUSA-N
Other name(s) : ATV006 || Q55KCM7PXB || GS-5245 || RefChem:167337 || ATV 006 || CHEMBL4863829 || SCHEMBL23959875
MW : 361.35
Formula : C16H19N5O5
CAS_number : 2647441-36-7
PubChem : 162513664
UniChem : YIHPGVCWGSURHO-VSBTWAGUSA-N
Target
Structures : No structure
Families : Carb_B_Chordata
References (4)
| Title : Identification of key metabolic enzymes involved in the activation of obeldesivir and remdesivir to the active triphosphate metabolite - Xu_2026_Antimicrob.Agents.Chemother__e0005526 |
| Author(s) : Xu Y , Liclican A , Zhao X , Chen C , Ortega JT , Chuang HC , Soulette C , Chaudhuri S , Zhang J , Wang T , Babusis D , Marchand B , Sun KH , Ramirez R , Ma B , Nayak A , Wang L , Menon S , Belzile JP , Lai Y , Li L , Mackman RL , Bilello JP , Cihlar T , Feng JY , Lad L |
| Ref : Antimicrobial Agents & Chemotherapy , :e0005526 , 2026 |
| Abstract : |
| PubMedSearch : Xu_2026_Antimicrob.Agents.Chemother__e0005526 |
| PubMedID: 42363837 |
| Title : The oral nucleoside prodrug GS-5245 is efficacious against SARS-CoV-2 and other endemic, epidemic, and enzootic coronaviruses - Martinez_2024_Sci.Transl.Med_16_eadj4504 |
| Author(s) : Martinez DR , Moreira FR , Catanzaro NJ , Diefenbacher MV , Zweigart MR , Gully KL , De la Cruz G , Brown AJ , Adams LE , Yount B , Baric TJ , Mallory ML , Conrad H , May SR , Dong S , Scobey DT , Nguyen C , Montgomery SA , Perry JK , Babusis D , Barrett KT , Nguyen AH , Nguyen AQ , Kalla R , Bannister R , Feng JY , Cihlar T , Baric RS , Mackman RL , Bilello JP , Schafer A , Sheahan TP |
| Ref : Sci Transl Med , 16 :eadj4504 , 2024 |
| Abstract : |
| PubMedSearch : Martinez_2024_Sci.Transl.Med_16_eadj4504 |
| PubMedID: 38776389 |
| Title : Discovery of GS-5245 (Obeldesivir), an Oral Prodrug of Nucleoside GS-441524 That Exhibits Antiviral Efficacy in SARS-CoV-2-Infected African Green Monkeys - Mackman_2023_J.Med.Chem_66_11701 |
| Author(s) : Mackman RL , Kalla RV , Babusis D , Pitts J , Barrett KT , Chun K , Du Pont V , Rodriguez L , Moshiri J , Xu Y , Lee M , Lee G , Bleier B , Nguyen AQ , O'Keefe BM , Ambrosi A , Cook M , Yu J , Dempah KE , Bunyan E , Riola NC , Lu X , Liu R , Davie A , Hsiang TY , Dearing J , Vermillion M , Gale M, Jr. , Niedziela-Majka A , Feng JY , Hedskog C , Bilello JP , Subramanian R , Cihlar T |
| Ref : Journal of Medicinal Chemistry , 66 :11701 , 2023 |
| Abstract : |
| PubMedSearch : Mackman_2023_J.Med.Chem_66_11701 |
| PubMedID: 37596939 |
| Title : Potency and pharmacokinetics of GS-441524 derivatives against SARS-CoV-2 - Wei_2021_Bioorg.Med.Chem_46_116364 |
| Author(s) : Wei D , Hu T , Zhang Y , Zheng W , Xue H , Shen J , Xie Y , Aisa HA |
| Ref : Bioorganic & Medicinal Chemistry , 46 :116364 , 2021 |
| Abstract : |
| PubMedSearch : Wei_2021_Bioorg.Med.Chem_46_116364 |
| PubMedID: 34450570 |