GSK143: a Syk kinase inhibitor; structure in first source
ID Source | ID |
---|---|
PubMed CID | 46865656 |
CHEMBL ID | 1835071 |
SCHEMBL ID | 1312033 |
MeSH ID | M0589706 |
Synonym |
---|
CHEMBL1835071 , |
S19 , |
2-{[(3r,4r)-3-aminotetrahydro-2h-pyran-4-yl]amino}-4-[(4-methylphenyl)amino]pyrimidine-5-carboxamide |
SCHEMBL1312033 |
us8470835, 1 |
bdbm50419247 |
2-{[(3r,4r)-3-aminotetrahydro-2h-pyran-4-yl]amino}-4-[(4-methylphenyl)amino]-5-pyrimidinecarboxamide |
KBPYMFSSFLOJPH-UONOGXRCSA-N |
gsk143 |
Q27465205 |
1240390-27-5 |
2-(((3r,4r)-3-aminotetrahydro-2h-pyran-4-yl)amino)-4-(p-tolylamino)pyrimidine-5-carboxamide |
2-[[(3r,4r)-3-aminooxan-4-yl]amino]-4-(4-methylanilino)pyrimidine-5-carboxamide |
HY-12736 |
CS-0012313 |
AKOS040756569 |
GSK143 is a potent and highly selective SYK inhibitor showing good efficacy in the rat Arthus model.
Excerpt | Reference | Relevance |
---|---|---|
"GSK143 is a potent and highly selective SYK inhibitor showing good efficacy in the rat Arthus model." | ( Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. Atkinson, FL; Barker, MD; Carter, PS; Curtis, NR; Davis, RP; Dickson, MC; Douault, C; Elwes, D; Garton, NS; Gray, M; Hayhow, TG; Hobbs, CI; Jones, E; Leach, S; Leavens, K; Lewis, HD; Liddle, J; McCleary, S; Neu, M; Patel, VK; Preston, AG; Ramirez-Molina, C; Shipley, TJ; Skone, PA; Smithers, N; Somers, DO; Walker, AL; Watson, RJ; Weingarten, GG, 2011) | 1.46 |
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Tyrosine-protein kinase JAK2 | Homo sapiens (human) | IC50 (µMol) | 1.5849 | 0.0001 | 0.3722 | 10.0000 | AID622853 |
Tyrosine-protein kinase Lck | Homo sapiens (human) | IC50 (µMol) | 5.0119 | 0.0002 | 1.3173 | 10.0000 | AID622856 |
Tyrosine-protein kinase Lyn | Homo sapiens (human) | IC50 (µMol) | 3.9811 | 0.0002 | 0.5594 | 5.2000 | AID622855 |
Tyrosine-protein kinase JAK1 | Homo sapiens (human) | IC50 (µMol) | 1.5849 | 0.0003 | 0.2378 | 7.3000 | AID622854 |
Mitogen-activated protein kinase 3 | Homo sapiens (human) | IC50 (µMol) | 0.0794 | 0.0025 | 3.0926 | 9.5820 | AID622870 |
Mitogen-activated protein kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0794 | 0.0003 | 1.6878 | 9.2000 | AID622870 |
Tyrosine-protein kinase ZAP-70 | Homo sapiens (human) | IC50 (µMol) | 19.9526 | 0.0011 | 1.2309 | 9.7000 | AID622955 |
Tyrosine-protein kinase SYK | Homo sapiens (human) | IC50 (µMol) | 0.0316 | 0.0001 | 0.8260 | 10.0000 | AID622954 |
Tyrosine-protein kinase JAK3 | Homo sapiens (human) | IC50 (µMol) | 1.9953 | 0.0001 | 0.4193 | 7.9200 | AID622851 |
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 19.9526 | 0.0009 | 1.9014 | 10.0000 | AID622869 |
Aurora kinase B | Homo sapiens (human) | IC50 (µMol) | 15.8489 | 0.0003 | 0.9634 | 9.8000 | AID622953 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID622868 | Immunomodulatory activity in human primary B cells assessed as induction of CD69 expression after 24 hrs by FITC-conjugated flow cytometry | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622851 | Inhibition of JAK3 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622854 | Inhibition of JAK1 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622954 | Inhibition of human full-length recombinant 6His-SYK assessed as phosphorylation of Biotin-AAAEEIYGEI substrate after 60 mins by by TR-FRET assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622860 | Selectivity for human recombinant SYK over JAK1 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622865 | Half life in rat at 1 mg/kg, iv and 3 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID1128159 | Mutagenicity in Salmonella typhi TA1537 by Ames test | 2014 | Journal of medicinal chemistry, Mar-27, Volume: 57, Issue:6 | Using ovality to predict nonmutagenic, orally efficacious pyridazine amides as cell specific spleen tyrosine kinase inhibitors. |
AID622864 | Volume of distribution at steady state in rat at 1 mg/kg, iv and 3 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622858 | Selectivity for human recombinant SYK over JAK3 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622849 | Antihypersensitivity activity in po dosed CD rat assessed as reduction in ovalbumin-induced cutaneous reverse passive arthus reaction administered orally 1 hr before ovalbumin challenge measured after 4 hrs by Evans blue dye-based spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622870 | Inhibition of Erk1/2 phosphorylation expressed in ramos cells after 30 mins by MSD assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622856 | Inhibition of LCK | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622853 | Inhibition of JAK2 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622866 | Clearance in rat at 1 mg/kg, iv and 3 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622846 | Antihypersensitivity activity in CD rat assessed as reduction in ovalbumin-induced cutaneous reverse passive arthus reaction at 10 mg/kg, po administered 1 hr before ovalbumin challenge measured after 4 hrs by Evans blue dye-based spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622859 | Selectivity for human recombinant SYK over JAK2 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622855 | Inhibition of LYN | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622953 | Inhibition of human recombinant Flag-6His-Thr-tagged Aurora B assessed as phosphorylation of 5FAM-PKA-tide substrate after 150 mins by fuorescence polarisation kinase assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622867 | Oral bioavailability in rat at 3 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622958 | Mutagenic activity in Salmonella Typhimurium TA1537 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622956 | Antihypersensitivity activity in CD rat assessed as reduction in cutaneous reverse passive arthus reaction at 30 mg/kg, po administered 1 hr before ovalbumin challenge measured after 4 hrs by Evans blue dye-based spectrophotometry | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622848 | Fraction unbound in human blood | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622861 | Selectivity for human recombinant SYK over LYN | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622857 | Selectivity for human recombinant SYK over human recombinant Aurora B | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622955 | Inhibition of ZAP70 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622869 | Inhibition of human ERG expressed in CHO-K1 cells after 2 hrs by Cy3b-Dofetilide-based fluorescence polarisation assay | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622863 | Selectivity for human recombinant SYK over ZAP70 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622862 | Selectivity for human recombinant SYK over LCK | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622850 | Aqueous solubility of compound in fed state simulated intestinal fluid at pH 6.5 | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
AID622847 | Distribution coefficient, log D of compound | 2011 | Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20 | Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor. |
[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 (100.00) | 24.3611 |
2020's | 0 (0.00) | 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 (17.90) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 0 (0.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 5 (100.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |