GSK2586184: a Janus kinase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 44603362 |
| CHEMBL ID | 3301606 |
| SCHEMBL ID | 2240393 |
| MeSH ID | M000613614 |
| Synonym |
|---|
| solcitinib , |
| n-(5-(4-((3,3-dimethylazetidin-1-yl)carbonyl)phenyl)(1,2,4)triazolo(1,5-a)pyridin-2-yl)cyclopropanecarboxamide |
| gsk2586184a |
| 1206163-45-2 |
| solcitinib [usan:inn] |
| 3v7gq1260k , |
| glpg0778 |
| cyclopropanecarboxamide, n-(5-(4-((3,3-dimethyl-1-azetidinyl)carbonyl)phenyl)(1,2,4)triazolo(1,5-a)pyridin-2-yl)- |
| unii-3v7gq1260k |
| g154578 |
| S5917 |
| CHEMBL3301606 |
| n-(5-(4-(3,3-dimethylazetidine-1-carbonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide |
| gsk2586184 |
| glpg 0778 |
| gsk 2586184 |
| us8796457, 1 |
| bdbm128101 |
| n-(5-(4-((3,3-dimethyl-1-azetidinyl)carbonyl)phenyl)(1,2,4)triazolo(1,5-a)pyridin-2-yl)cyclopropanecarboxamide |
| solcitinib [usan] |
| gsk-2586184a |
| g-154578 |
| solcitinib [who-dd] |
| glpg-0778 |
| gsk-2586184 |
| glpg-0788 |
| solcitinib [inn] |
| HY-16755 |
| CS-5204 |
| cyclopropanecarboxylic acid{5-[4-(3,3-dimethyl-azetidine-1-carbonyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide |
| cyclopropanecarboxylic acid {5-[4-(3,3-dimethyl-azetidine-1-carbonyl)-phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}-amide |
| MPYACSQFXVMWNO-UHFFFAOYSA-N |
| SCHEMBL2240393 |
| D10728 |
| solcitinib (usan/inn) |
| AKOS025289798 |
| compound 1 [wo2010149771] |
| gtpl9697 |
| n-[5-[4-(3,3-dimethylazetidine-1-carbonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide |
| AC-30938 |
| n-{5-[4-(3,3-dimethylazetidine-1-carbonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl}cyclopropanecarboxamide |
| mfcd26960569 |
| NCGC00484062-01 |
| solicitinib |
| solcitinibglpg0778 |
| BCP23893 |
| glpg-0778;solcitinib |
| EX-A2326 |
| SB16965 |
| Q27258083 |
| AS-56075 |
| A892157 |
GSK2586184 is a selective oral Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis.
| Excerpt | Reference | Relevance |
|---|---|---|
| "GSK2586184 is a selective oral Janus kinase (JAK)1 inhibitor being evaluated as a treatment for moderate-to-severe plaque-type psoriasis." | ( Investigation of selective JAK1 inhibitor GSK2586184 for the treatment of psoriasis in a randomized placebo-controlled phase IIa study. Binks, MH; Griffiths, CE; Hanrott, KE; Hicks, KJ; Ludbrook, VJ; Patel, JS; Reich, K; Schifano, LA; Simeoni, M; Watson, J; Wilson, P; Wyres, MR, 2016) | 2.14 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Primary endpoints included interferon-mediated messenger RNA transcription over time, changes in Safety of Estrogen in Lupus National Assessment-SLE Disease Activity Index score, and number/severity of adverse events." | ( Safety, tolerability, efficacy and pharmacodynamics of the selective JAK1 inhibitor GSK2586184 in patients with systemic lupus erythematosus. Binks, M; Condreay, L; Dickson, M; Hachulla, E; Hicks, K; Kahl, L; Layton, M; Leon, G; Machado, D; Patel, J; Schifano, L; Staumont-Sallé, D; van Vollenhoven, RF; Zamuner, S, 2016) | 0.66 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " Shortly thereafter, significant safety data were identified, including elevated liver enzymes in six patients (one confirmed and one suspected case of Drug Reaction with Eosinophilia and Systemic Symptoms), leading to immediate dosing cessation." | ( Safety, tolerability, efficacy and pharmacodynamics of the selective JAK1 inhibitor GSK2586184 in patients with systemic lupus erythematosus. Binks, M; Condreay, L; Dickson, M; Hachulla, E; Hicks, K; Kahl, L; Layton, M; Leon, G; Machado, D; Patel, J; Schifano, L; Staumont-Sallé, D; van Vollenhoven, RF; Zamuner, S, 2016) | 0.66 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 4.1544 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| Interferon beta | Homo sapiens (human) | Potency | 4.1544 | 0.0033 | 9.1582 | 39.8107 | AID1347411 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytokine activity | Interferon beta | Homo sapiens (human) |
| cytokine receptor binding | Interferon beta | Homo sapiens (human) |
| type I interferon receptor binding | Interferon beta | Homo sapiens (human) |
| protein binding | Interferon beta | Homo sapiens (human) |
| chloramphenicol O-acetyltransferase activity | Interferon beta | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| extracellular space | Interferon beta | Homo sapiens (human) |
| extracellular region | Interferon beta | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347412 | qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 5 (62.50) | 24.3611 |
| 2020's | 3 (37.50) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (17.21) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 3 (37.50%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 1 (12.50%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (50.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||