sl0101 profile

SL0101: p90 Ribosomal S6 Kinase; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	10459196
CHEMBL ID	240954
SCHEMBL ID	4371341
MeSH ID	M0481859

Synonym
sl0101
bdbm50241294
kaempferol-3-o-(3,4-di-o-acetyl-alpha-l-rhamnopyranoside)
kaempferol 3-o-(3'''',4''''-di-o-acetyl-alpha-l-rhamnopyranoside
sl-0101
CHEMBL240954 ,
5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4h-chromen-3-yl 3,4-di-o-acetyl-6-deoxy-alpha-l-mannopyranoside
sl0 ,
SL 0101-1 ,
sl0101-1
77307-50-7
3UBD
SCHEMBL4371341
AC-29057
Z2216897437
AKOS030621758
Q27465395
sl 0101
SXOZSDJHGMAEGZ-IGKKHSBFSA-N
HY-15237
CS-0003824
(2s,3s,4s,5r,6s)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4h-chromen-3-yl)oxy)-5-hydroxy-2-methyltetrahydro-2h-pyran-3,4-diyl diacetate
MS-29586
CDA30750
DTXSID801197567
kaempferol 3-o-(3'',4''-di-o-acetyl-alpha-l-rhamnopyranoside)
(2s,3s,4s,5r,6s)-6-((5,7-dihydroxy-2-(4-hydroxyphenyl)-4-oxo-4h-chromen-3-yl)oxy)-5-hydroxy-2-methyltetrahydro-2h-pyran-3,4-diyldiacetate

Excerpt	Reference	Relevance
"SL0101 is a potent and specific inhibitor of RSK; therefore, we performed an analysis of the structural basis for the inhibitory activity of this lead compound."	( Structural basis for the activity of the RSK-specific inhibitor, SL0101. Hecht, SM; Lannigan, DA; Maloney, DJ; Smith, JA, 2007)	1.3
"SL0101 is a natural product that demonstrates selectivity for RSK inhibition."	( Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101. Lannigan, DA; Li, M; Li, Y; Mrozowski, RM; O'Doherty, GA; Sandusky, ZM; Shan, M; Song, X; Wu, B; Zhang, Q, 2015)	1.36

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	20.6000	0.0001	1.7536	10.0000	AID402936
Cytochrome P450 2D6	Homo sapiens (human)	IC50 (µMol)	50.5000	0.0000	2.0151	10.0000	AID402937
Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)	IC50 (µMol)	0.4242	0.0001	0.5372	9.9900	AID1177369; AID1188772; AID657079; AID727537; AID739291
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, Ribosomal protein S6 kinase alpha-3	Mus musculus (house mouse)	Kd	2.9000	2.9000	2.9000	2.9000	AID977611
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
coumarin metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
isoquinoline alkaloid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 2D6	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 2D6	Homo sapiens (human)
negative regulation of cellular organofluorine metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
arachidonic acid metabolic process	Cytochrome P450 2D6	Homo sapiens (human)
skeletal system development	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
toll-like receptor signaling pathway	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
signal transduction	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
chemical synaptic transmission	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
central nervous system development	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
peptidyl-serine phosphorylation	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
positive regulation of cell growth	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
response to lipopolysaccharide	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
intracellular signal transduction	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
negative regulation of apoptotic process	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic process	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
regulation of translation in response to stress	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
positive regulation of cell differentiation	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 2D6	Homo sapiens (human)
iron ion binding	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 2D6	Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen	Cytochrome P450 2D6	Homo sapiens (human)
heme binding	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 2D6	Homo sapiens (human)
magnesium ion binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein serine/threonine kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
ATP binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein kinase binding	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic process	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
protein serine kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
ribosomal protein S6 kinase activity	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
mitochondrion	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum	Cytochrome P450 2D6	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 2D6	Homo sapiens (human)
cytoplasm	Cytochrome P450 2D6	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 2D6	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
nucleolus	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
cytosol	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
synapse	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
cytoplasm	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
nucleoplasm	Ribosomal protein S6 kinase alpha-3	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (103)

Assay ID	Title	Year	Journal	Article
AID435963	Percentage CK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435726	Percentage JNK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435631	Percentage RSK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID657082	Antiproliferative activity against human MCF7 cells after 48 hrs by CellTiter-GloTM assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID435476	Percentage MNK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435668	Percentage PAK5 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435542	Percentage PKBbeta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435753	Percentage S6K1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435119	Percentage MKK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID402937	Inhibition of human CYP2D6 by radiometric assay	2004	Journal of natural products, Jul, Volume: 67, Issue:7	Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.
AID435367	Percentage NEK6 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID308094	Antiproliferative activity against human MCF7 cells at >100 uM after 48 hrs	2007	Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14	Structural basis for the activity of the RSK-specific inhibitor, SL0101.
AID739291	Inhibition of GST-fused RSK2 (unknown origin) after 10 to 45 mins by immunoblotting analysis	2013	Bioorganic & medicinal chemistry, Apr-01, Volume: 21, Issue:7	Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
AID1177383	Increase in phosphorylation motif of protein kinase A in human MCF7 cells at 100 uM by immunoblotting analysis	2015	ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1	Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
AID435720	Percentage ERK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435426	Percentage PKBalpha activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727543	Dose normalized AUC in CD1 mouse at 1 mg/kg, iv	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435240	Percentage JNK3 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435313	Percentage CHK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435869	Percentage p38alpha activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435173	Percentage PDK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435991	Percentage SGK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID1177370	Antiproliferative activity against human MCF7 cells at 100 uM after 48 hrs by CellTiterGlo assay	2015	ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1	Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
AID657084	Antiproliferative activity against human MCF7 cells at 100 uM after 144 hrs by CellTiter-GloTM assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID1188772	Inhibition of his-tagged active RSK2 (unknown origin) expressed in Sf9 cells after 10 to 45 mins by ELISA	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Kaempferol, a potential cytostatic and cure for inflammatory disorders.
AID727538	Cmax in CD1 mouse plasma at 2.5 mg/kg, ip	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435628	Percentage ROCK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727537	Inhibition of recombinant RSK2 (unknown origin) expressed in baculovirus infected Sf9 cells assessed as decrease in substrate phosphorylation using GST-fusion protein containing ERalpha-Ser167 sequence-RLASTND as substrate by chemiluminescence analysis	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435129	Percentage PKD1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435977	Percentage MNK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID436028	Percentage PHK activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727398	Decrease in cyclin D1 level in human PMA-stimulated MCF7 cells at 100 uM pretreated for 2 hrs prior to PMA addition measured after 20 mins by immunoblot analysis	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID436085	Percentage HIPK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID436064	Percentage Aurora C activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435993	Percentage Src activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID657083	Antiproliferative activity against human MCF7 cells at 100 uM after 48 hrs by CellTiter-GloTM assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID657087	Antiproliferative activity against human MCF7 cells at 50 uM after 48 hrs by CellTiter-GloTM assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID435994	Percentage SRPK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435218	Percentage CaMKKalpha activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435859	Percentage JNK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435745	Percentage PLK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435844	Percentage CaMK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435113	Percentage MAPKAPK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435368	Percentage NEK7 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435741	Percentage PKCzeta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID1177385	Inhibition of RSK in PMA-stimulated human MCF7 cells assessed as decrease in intensity of band at 65 and 27 kDa at 100 uM by immunoblotting analysis	2015	ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1	Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
AID435840	Percentage AMPK activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435172	Percentage PAK6 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435126	Percentage p38-gamma activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435876	Percentage PRAK activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID657088	Antiproliferative activity against human MCF7 cells at 100 uM after 96 hrs by CellTiter-GloTM assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID435603	Percentage HIPK3 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID1177378	Reduction in cyclin D1 in PMA-stimulated human MCF7 cells at 100 uM by immunoblotting analysis	2015	ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1	Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
AID727541	Initial plasma concentration in CD1 mouse at 1 mg/kg, iv	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID402936	Inhibition of human CYP3A4 by radiometric assay	2004	Journal of natural products, Jul, Volume: 67, Issue:7	Sesquiterpenes and flavonol glycosides from Zingiber aromaticum and their CYP3A4 and CYP2D6 inhibitory activities.
AID727396	Inhibition of RSK2 in human PMA-stimulated MCF7 cells assessed as decrease in expression of 27kDa protein harboring (Lys/Arg)X(Lys/Arg)XX(pSer/pThr) motif at 100 uM pretreated for 2 hrs prior to PMA addition measured after 20 mins by immunoblot analysis	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435480	Percentage MSK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727540	Half life in CD1 mouse at 2.5 mg/kg, ip	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435483	Percentage NEK2a activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435824	Percentage PKA activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435356	Percentage IKK-beta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435459	Percentage CK1delta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727539	Half life in CD1 mouse at 1 mg/kg, iv	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID1177376	Inhibition of RSK in PMA-stimulated human MCF7 cells assessed as increase in phosphorylation of eEF2 at 100 uM by immunoblotting analysis	2015	ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1	Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
AID435597	Percentage DYRK1A activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID436038	Percentage PIM2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID657086	Antiproliferative activity against human MCF10A cells at 50 uM after 48 hrs by CellTiter-GloTM assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID436080	Percentage ERK1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727400	Inhibition of RSK2 in human MCF7 cells assessed as reduction of PMA-induced decrease in EF2 kinase phosphorylation at 100 uM pretreated for 2 hrs prior to PMA addition measured after 20 mins by immunoblot analysis	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435121	Percentage MST2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727542	Dose normalized AUC in CD1 mouse at 2.5 mg/kg, ip	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435455	Percentage CDK2-cyclinA activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435705	Percentage BRSK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435812	Percentage PIM1 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435376	Percentage RSK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435488	Percentage p38beta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID727403	Partition coefficient, log P of the compound	2012	ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2	Improving the affinity of SL0101 for RSK using structure-based design.
AID435308	Percentage PKCalpha activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435416	Percentage PAK4 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435341	Percentage CHK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID308093	Antiproliferative activity against human MCF10A cells up to 200 uM after 48 hrs	2007	Bioorganic & medicinal chemistry, Jul-15, Volume: 15, Issue:14	Structural basis for the activity of the RSK-specific inhibitor, SL0101.
AID657079	Inhibition of His-tagged RSK2 expressed in Sf9 cells using ERalpha-Ser167 RLASTND as substrate after 120 mins by chemiluminescence assay	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID435884	Percentage SmMLCK activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435682	Percentage PIM3 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID436073	Percentage CSK activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID436078	Percentage DYRK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435580	Percentage Aurora B activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID657089	Down regulation of cyclin D1 level in human MCF7 cells at 100 uM at 96 hrs by immunoblotting analysis relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID435316	Percentage MELK activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435968	Percentage GSK3-beta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID669363	Fe2+ chelating activity of the compound incubated for 5 mins prior to ferrozine-addition measured after 10 mins by spectrophotometry	2012	Bioorganic & medicinal chemistry letters, Jun-01, Volume: 22, Issue:11	Spectaflavoside A, a new potent iron chelating dimeric flavonol glycoside from the rhizomes of Zingiber spectabile Griff.
AID436067	Percentage CaMKKbeta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435967	Percentage ERK8 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID1177369	Inhibition of RSK2 (unknown origin) assessed as phosphorylation by Western lightning enhanced chemiluminescent reagent/HRP activity assay	2015	ACS medicinal chemistry letters, Jan-08, Volume: 6, Issue:1	Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
AID435966	Percentage EF2K activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435971	Percentage MAPKAPK3 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435241	Percentage Lck activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435850	Percentage DYRK3 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435494	Percentage PRK2 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID657085	Down regulation of cyclin D1 level in human MCF7 cells at 100 uM at 48 hrs by immunoblotting analysis relative to control	2012	Bioorganic & medicinal chemistry letters, May-01, Volume: 22, Issue:9	Analogs of the RSK inhibitor SL0101: optimization of in vitro biological stability.
AID435973	Percentage MARK3 activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID435622	Percentage p38delta activity remaining in the presence of 10uM inhibitor	2007	The Biochemical journal, Dec-15, Volume: 408, Issue:3	The selectivity of protein kinase inhibitors: a further update.
AID977611	Experimentally measured binding affinity data (Kd) for protein-ligand complexes derived from PDB	2012	Biochemistry, Aug-21, Volume: 51, Issue:33	Insights into the inhibition of the p90 ribosomal S6 kinase (RSK) by the flavonol glycoside SL0101 from the 1.5 Å crystal structure of the N-terminal domain of RSK2 with bound 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	10 (33.33)	29.6817
2010's	18 (60.00)	24.3611
2020's	2 (6.67)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (3.33%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	29 (96.67%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
phosphoserine Phosphoserine: The phosphoric acid ester of serine.	2.08	1	non-proteinogenic alpha-amino acid; O-phosphoamino acid; serine derivative	human metabolite
carbamates [no description available]	2.31	1	amino-acid anion
pteridines [no description available]	3.19	5	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; pteridines
go 6976 [no description available]	2.03	1	indolocarbazole; organic heterohexacyclic compound	EC 2.7.11.13 (protein kinase C) inhibitor
n-(2-(methylamino)ethyl)-5-isoquinolinesulfonamide [no description available]	2.03	1	isoquinolines; sulfonamide
fasudil fasudil: intracellular calcium antagonist; structure in first source. fasudil : An isoquinoline substituted by a (1,4-diazepan-1-yl)sulfonyl group at position 5. It is a Rho-kinase inhibitor and its hydrochloride hydrate form is approved for the treatment of cerebral vasospasm and cerebral ischemia.	2.03	1	isoquinolines; N-sulfonyldiazepane	antihypertensive agent; calcium channel blocker; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; geroprotector; neuroprotective agent; nootropic agent; vasodilator agent
harmaline Harmaline: A beta-carboline alkaloid isolated from seeds of PEGANUM.. harmaline : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7 and has been reduced across the 3,4 bond.	2.03	1	harmala alkaloid	oneirogen
harmalol harmalol: inhibitor of rat liver microsomal UDP-glucuronyltransferase; RN given refers to parent cpd; structure. harmalol : A harmala alkaloid in which the harman skeleton is hydroxy-substituted at C-7 and has been reduced across the 3,4 bond.	2.03	1	harmala alkaloid	algal metabolite; EC 1.4.3.4 (monoamine oxidase) inhibitor
ic 261 [no description available]	2.03	1	indoles
nsc 664704 kenpaullone: inhibits CDK1/cyclin B; structure in first source. kenpaullone : An indolobenzazepine that is paullone in which the hydrogen at position 9 is replaced by a bromo substituent. It is an ATP-competitive inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3beta (GSK3beta).	2.03	1	indolobenzazepine; lactam; organobromine compound	cardioprotective agent; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor; geroprotector
ketoconazole 1-acetyl-4-(4-{[2-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy}phenyl)piperazine : A dioxolane that is 1,3-dioxolane which is substituted at positions 2, 2, and 4 by imidazol-1-ylmethyl, 2,4-dichlorophenyl, and [para-(4-acetylpiperazin-1-yl)phenoxy]methyl groups, respectively.	2.02	1	dichlorobenzene; dioxolane; ether; imidazoles; N-acylpiperazine; N-arylpiperazine
2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one 2-(4-morpholinyl)-8-phenyl-4H-1-benzopyran-4-one: specific inhibitor of phosphatidylinositol 3-kinase; structure in first source	2.77	3	chromones; morpholines; organochlorine compound	autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector
1-NA-PP1 [no description available]	2.03	1	pyrazolopyrimidine	tyrosine kinase inhibitor
ag 1879 3-(4-chlorophenyl)-1-(1,1-dimethylethyl)-1H-pyrazolo(3,4-d)pyrimidin-4-amine: Fyn kinase inhibitor	2.03	1	aromatic amine; monochlorobenzenes; pyrazolopyrimidine	beta-adrenergic antagonist; EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor; geroprotector
ro 31-8220 Ro 31-8220: a protein kinase C inhibitor	2.74	3	imidothiocarbamic ester; indoles; maleimides	EC 2.7.11.13 (protein kinase C) inhibitor
sb 202190 4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase	2.03	1	imidazoles; organofluorine compound; phenols; pyridines	apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
zm 336372 N-(5-(3-dimethylaminobenzamido)-2-methylphenyl)-4-hydroxybenzamide: an inhibitor of c-Raf; activates Raf-1; structure in first source	2.03	1	benzamides
serine Serine: A non-essential amino acid occurring in natural form as the L-isomer. It is synthesized from GLYCINE or THREONINE. It is involved in the biosynthesis of PURINES; PYRIMIDINES; and other amino acids.. serine : An alpha-amino acid that is alanine substituted at position 3 by a hydroxy group.	2.04	1	L-alpha-amino acid; proteinogenic amino acid; serine family amino acid; serine zwitterion; serine	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.21	1	pyrrole; secondary amine
pyrazolanthrone pyrazolanthrone: JNK (c-Jun N-terminal kinase) inhibitor; structure in first source. anthra[1,9-cd]pyrazol-6(2H)-one : A member of the class of anthrapyrazoles that is anthra[1,9-cd]pyrazole substituted at position 6 by an oxo group. An inhibitor of c-Jun N-terminal kinase.	2.03	1	anthrapyrazole; aromatic ketone; cyclic ketone	antineoplastic agent; c-Jun N-terminal kinase inhibitor; geroprotector
diphenylamine Diphenylamine: In humans it may be irritating to mucous membranes. Methemoglobinemia has been produced experimentally. In veterinary use, it is one of active ingredients in topical agents for prevention and treatment of screwworm infestation. An indicator in tests for nitrate poisoning.. diphenylamine : An aromatic amine containing two phenyl substituents. It has been used as a fungicide for the treatment of superficial scald in apples and pears, but is no longer approved for this purpose within the European Union.	2.07	1	aromatic amine; bridged diphenyl fungicide; secondary amino compound	antifungal agrochemical; antioxidant; carotogenesis inhibitor; EC 1.3.99.29 [phytoene desaturase (zeta-carotene-forming)] inhibitor; ferroptosis inhibitor; radical scavenger
palladium Palladium: A chemical element having an atomic weight of 106.4, atomic number of 46, and the symbol Pd. It is a white, ductile metal resembling platinum, and following it in abundance and importance of applications. It is used in dentistry in the form of gold, silver, and copper alloys.. palladium : Chemical element (nickel group element atom) with atomic number 46.	7.44	2	metal allergen; nickel group element atom; platinum group metal atom
rhamnose [no description available]	7.76	3	L-rhamnose
procyanidin Proanthocyanidins: Dimers and oligomers of flavan-3-ol units (CATECHIN analogs) linked mainly through C4 to C8 bonds to leucoanthocyanidins. They are structurally similar to ANTHOCYANINS but are the result of a different fork in biosynthetic pathways.	2.07	1	proanthocyanidin
cki 7 N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide: casein kinase I inhibitor; structure given in first source. N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide : A member of the class of isoquinolines that is isoquinoline-8-sulfonamide which is substituted by chlorine at position 5 and in which the sulfonamide nitrogen is substituted by a 2-aminoethyl group. It is an inhibitor of casein kinase I.	2.03	1	isoquinolines; organochlorine compound; primary amino compound; sulfonamide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
ruboxistaurin ruboxistaurin: inhibits protein kinase C beta; structure in first source	2.03	1
birb 796 [no description available]	2.03	1	aromatic ether; morpholines; naphthalenes; pyrazoles; ureas	EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; immunomodulator
cyc 202 seliciclib : 2,6-Diaminopurine carrying benzylamino, (2R)-1-hydroxybutan-2-yl and isopropyl substituents at C-6, C-2-N and N-9 respectively. It is an experimental drug candidate in the family of pharmacological cyclin-dependent kinase (CDK) inhibitors.	2.03	1	2,6-diaminopurines	antiviral drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor
sb 203580 [no description available]	2.03	1	imidazoles; monofluorobenzenes; pyridines; sulfoxide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent
sb 216763 [no description available]	2.03	1	indoles; maleimides
sorafenib [no description available]	2.03	1	(trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; phenylureas; pyridinecarboxamide	angiogenesis inhibitor; anticoronaviral agent; antineoplastic agent; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; ferroptosis inducer; tyrosine kinase inhibitor
sitosterol, (3beta)-isomer Sobatum: tradename; active fraction of Solanum trilobatum; reduces side-effects of radiation-induced toxicity. sitosterol : A member of the class of phytosterols that is stigmast-5-ene substituted by a beta-hydroxy group at position 3.	2.02	1	3beta-hydroxy-Delta(5)-steroid; 3beta-sterol; C29-steroid; phytosterols; stigmastane sterol	anticholesteremic drug; antioxidant; mouse metabolite; plant metabolite; sterol methyltransferase inhibitor
wortmannin [no description available]	2.48	2	acetate ester; cyclic ketone; delta-lactone; organic heteropentacyclic compound	anticoronaviral agent; antineoplastic agent; autophagy inhibitor; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; geroprotector; Penicillium metabolite; radiosensitizing agent
quinidine Quinidine: An optical isomer of quinine, extracted from the bark of the CHINCHONA tree and similar plant species. This alkaloid dampens the excitability of cardiac and skeletal muscles by blocking sodium and potassium currents across cellular membranes. It prolongs cellular ACTION POTENTIALS, and decreases automaticity. Quinidine also blocks muscarinic and alpha-adrenergic neurotransmission.. quinidine : A cinchona alkaloid consisting of cinchonine with the hydrogen at the 6-position of the quinoline ring substituted by methoxy.	2.02	1	cinchona alkaloid	alpha-adrenergic antagonist; anti-arrhythmia drug; antimalarial; drug allergen; EC 1.14.13.181 (13-deoxydaunorubicin hydroxylase) inhibitor; EC 3.6.3.44 (xenobiotic-transporting ATPase) inhibitor; muscarinic antagonist; P450 inhibitor; potassium channel blocker; sodium channel blocker
n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea N-(4-methoxybenzyl)-N'-(5-nitro-1,3-thiazol-2-yl)urea: structure in first source	2.03	1
y 27632 Y 27632: RN given for di-HCl salt; inhibits Rho-associated protein kinase; inhibits calcium sensitization to affect smooth muscle relaxation; structure in first source. Y-27632 : A monocarboxylic acid amide that is trans-[(1R)-1-aminoethyl]cyclohexanecarboxamide in which one of the nitrogens of the aminocarbony group is substituted by a pyridine nucleus. It has been shown to exhibit inhibitory activity against Rho-associated protein kinase (ROCK) enzyme.	2.03	1	aromatic amide
h 1152 (S)-2-methyl-1-(4-methylisoquinoline-5-sulfonyl)-1,4-diazepane : A member of the class of isoquinolines that is the sulfonamide formed by the formal condensation of the sulfo group of 4-methylisoquinoline-5-sulfonic acid with the 1-amino group of (S)-2-methyl-1,4-diazepane.	2.03	1	isoquinolines; N-sulfonyldiazepane	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor
h 89 N-(2-(4-bromocinnamylamino)ethyl)-5-isoquinolinesulfonamide: structure given in first source. N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A member of the class of isoquinolines that is the sulfonamide obtained by formal condensation of the sulfo group of isoquinoline-5-sulfonic acid with the primary amino group of N(1)-[3-(4-bromophenyl)prop-2-en-1-yl]ethane-1,2-diamine. It is a protein kinase A inhibitor.. (E)-N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide : A N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide in which the double bond adopts a trans-configuration.	2.03	1	N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
purvalanol a 6-((3-chloro)anilino)-2-(isopropyl-2-hydroxyethylamino)-9-isopropylpurine: purvalanol A is the (1R)-isomer;	2.03	1	purvalanol
Src Inhibitor-1 Src Inhibitor-1 : A member of the class of quinazolines that is quinazoline which is substituted at position 4 by a p-phenoxyanilino group and at positions 6 and 7 by methoxy groups. It is a potent, competitive dual site (both the ATP- and peptide-binding) Src kinase inhibitor. Src Inhibitor-1 is one of the 'gold standards' for Src kinase inhibition that has been shown to use PP1 or PP2 in parallel with Src-I1 to inhbit Src family kinases.	2.03	1	aromatic ether; polyether; quinazolines; secondary amino compound	EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor
sc 514 SC 514: inhibits IkappaB kinase-2; structure in first source	2.03	1	ring assembly; thiophenes
u 0126 U 0126: protein kinase kinase inhibitor; structure in first source	2.48	2	aryl sulfide; dinitrile; enamine; substituted aniline	antineoplastic agent; antioxidant; apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; osteogenesis regulator; vasoconstrictor agent
7-epi-hydroxystaurosporine [no description available]	2.03	1
sb 415286 3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione: a glycogen synthase kinase-3 inhibitor; structure in first source	2.03	1	C-nitro compound; maleimides; monochlorobenzenes; phenols; secondary amino compound; substituted aniline	antioxidant; apoptosis inducer; EC 2.7.11.26 (tau-protein kinase) inhibitor; neuroprotective agent
alsterpaullone alsterpaullone: structure in first source. alsterpaullone : An organic heterotetracyclic compound that is 1,3-dihydro-2H-1-benzazepin-2-one which shares its 4-5 bond with the 3-2 bond of 5-nitro-1H-indole.	2.03	1	C-nitro compound; caprolactams; organic heterotetracyclic compound	anti-HIV-1 agent; antineoplastic agent; apoptosis inducer; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; EC 2.7.11.26 (tau-protein kinase) inhibitor
1-tert-butyl-3-naphthalen-1-ylmethyl-1h-pyrazolo(3,4-d)pyrimidin-4-ylemine [no description available]	2.03	1	pyrazolopyrimidine	tyrosine kinase inhibitor
3-methylkaempferol 3-methylkaempferol: structure in first source. 3-methoxyapigenin : A trihydroxyflavone that is apigenin substituted by a methoxy group at position 3.	2.02	1	monomethoxyflavone; trihydroxyflavone	plant metabolite
kaempferol [no description available]	2.73	3	7-hydroxyflavonol; flavonols; tetrahydroxyflavone	antibacterial agent; geroprotector; human blood serum metabolite; human urinary metabolite; human xenobiotic metabolite; plant metabolite
harmine Harmine: Alkaloid isolated from seeds of PEGANUM HARMALA; ZYGOPHYLLACEAE. It is identical to banisterine, or telepathine, from Banisteria caapi and is one of the active ingredients of hallucinogenic drinks made in the western Amazon region from related plants. It has no therapeutic use, but (as banisterine) was hailed as a cure for postencephalitic PARKINSON DISEASE in the 1920's.. harmine : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7.	2.03	1	harmala alkaloid	anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; metabolite
harman harman: a beta-carboline; RN given refers to parent cpd; structure. harman : An indole alkaloid fundamental parent with a structure of 9H-beta-carboline carrying a methyl substituent at C-1. It has been isolated from the bark of Sickingia rubra, Symplocus racemosa, Passiflora incarnata, Peganum harmala, Banisteriopsis caapi and Tribulus terrestris, as well as from tobacco smoke. It is a specific, reversible inhibitor of monoamine oxidase A.	2.03	1	harmala alkaloid; indole alkaloid fundamental parent; indole alkaloid	anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; plant metabolite
shogaol shogaol: from ginger, ZINGIBER OFFICINALE; less mutagenic than GINGEROL; structure given in first source	2.02	1	enone; monomethoxybenzene; phenols
rottlerin rottlerin: an angiogenesis inhibitor; an inhibitor of protein kinase Cdelta (PKCdelta) and calmodulin kinase III; RN refers to (E)-isomer; do not confuse this chalcone with an anthraquinone that is also called rottlerin (RN 481-72-1);. rottlerin : A chromenol that is 2,2-dimethyl-2H-chromene substituted by hydroxy groups at positions 5 and 7, a 3-acetyl-2,4,6-trihydroxy-5-methylbenzyl group at position 6 and a (1E)-3-oxo-1-phenylprop-1-en-3-yl group at position 8. A potassium channel opener, it is isolated from Mallotus philippensis.	2.03	1	aromatic ketone; benzenetriol; chromenol; enone; methyl ketone	anti-allergic agent; antihypertensive agent; antineoplastic agent; apoptosis inducer; K-ATP channel agonist; metabolite
sirolimus Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.	2.77	3	antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol	antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor
su 6656 SU 6656: a c-Src kinase inhibitor; used to probe growth signaling; structure in first source. SU6656 : A member of the class of oxindoles that is 3-methyleneoxindole in which the hydrogeh at position 5 has been replaced by a dimethylaminosulfonyl group and in which one of the hydrogens of the methylene group has been replaced by a 4,5,6,7-tetrahydro-indol-2-yl group. It is a specific inhibitor of Src family kinase.	2.03	1
kaempferol 3-o-rhamnoside kaempferol 3-O-rhamnoside: from apple (Malus domestica) leaves; structure in first source. afzelin : A glycosyloxyflavone that is kaempferol attached to an alpha-L-rhamnosyl residue at position 3 via a glycosidic linkage.	2.73	3	glycosyloxyflavone; monosaccharide derivative; trihydroxyflavone	anti-inflammatory agent; antibacterial agent; plant metabolite
orantinib orantinib: an antiangiogenic agent. orantinib : An oxindole that is 3-methyleneoxindole in which one of the hydrogens of the methylene group is substituted by a 2-(2-carboxyethyl)-3,5-dimethylpyrrol-3-yl group. It is an ATP-competitive inhibitor of the tyrosine kinase activity of fibroblast growth factor receptor 1.	2.03	1
ermanin ermanin: from Tanacetum microphyllum; structure given in first source. 3,4'-dimethylkaempferol : A dimethoxyflavone that is kaempferol in which the hydroxy groups at position 3 and 4' have been replaced by methoxy groups. It is a component of bee glue and isolated from several plant species including Tanacetum microphyllum.	2.02	1	dihydroxyflavone; dimethoxyflavone	anti-inflammatory agent; antimycobacterial drug; antineoplastic agent; apoptosis inducer; plant metabolite
vinblastine sulfate [no description available]	2.07	1
zerumbone zerumbone: RN given for (E,E,E)-isomer; structure in first source. zerumbone : A sesquiterpenoid and cyclic ketone that is (1E,4E,8E)-alpha-humulene which is substituted by an oxo group at the carbon atom attached to two double bonds. It is obtained by steam distillation from a type of edible ginger, Zingiber zerumbet Smith, grown particularly in southeast Asia.	2.02	1	cyclic ketone; sesquiterpenoid	anti-inflammatory agent; glioma-associated oncogene inhibitor; plant metabolite
vx680 [no description available]	2.03	1	N-arylpiperazine
d 4476 [no description available]	2.03	1	imidazoles
pd 184352 2-(2-chloro-4-iodophenylamino)-N-cyclopropylmethoxy-3,4-difluorobenzamide: inhibits MAP kinase kinase; structure in first source	2.03	1	aminobenzoic acid
bms345541 4(2'-aminoethyl)amino-1,8-dimethylimidazo(1,2-a)quinoxaline: structure in first source	2.03	1	quinoxaline derivative
pd 0325901 mirdametinib: has antineoplastic activity; appears to be a MEK inhibitor. PD 0325901 : A hydroxamic acid ester that is benzhydroxamic acid (N-hydroxybenzamide) in which the hydroxamic acid group has been converted to the corresponding 2,3-dihydroxypropyl ester and in which the benzene ring has been substituted at position 2 by a (2-fluoro-4-iodophenyl)amino group and at positions 3 and 4 by fluorines (the R enantiomer).	2.46	2	difluorobenzene; hydroxamic acid ester; monofluorobenzenes; organoiodine compound; propane-1,2-diols; secondary amino compound	antineoplastic agent; EC 2.7.12.2 (mitogen-activated protein kinase kinase) inhibitor
pi103 PI103: pyridofuropyrimidine antineoplastic; a potent inhibitor of class I phosphatidylinositide 3-kinases (PI3K); structure in first soruce	2.03	1	aromatic amine; morpholines; organic heterotricyclic compound; phenols; tertiary amino compound	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor
ps1145 PS1145: IkappaB kinase inhibitor; structure in first source	2.03	1	beta-carbolines
chir 99021 Chir 99021: structure in first source. CHIR 99021 : A member of the class of aminopyrimidines that is 2-aminopyrimidine substituted at positions N2, 5 and 6 by (5-cyanopyridin-2-yl)ethyl, 4-methylimidazol-2-yl and 2,4-dichlorophenyl groups respectively.	2.03	1	aminopyridine; aminopyrimidine; cyanopyridine; diamine; dichlorobenzene; imidazoles; secondary amino compound	EC 2.7.11.26 (tau-protein kinase) inhibitor
bx795 BX795: structure in first source	2.03	1	ureas
a 443654 A 443654: an Akt kinase inhibitor; structure in first source	2.03	1	indoles
dorsomorphin dorsomorphin: an AMPK inhibitor. dorsomorphin : A pyrazolopyrimidine that is pyrazolo[1,5-a]pyrimidine which is substituted at positions 3 and 6 by pyridin-4-yl and p-[2-(piperidin-1-yl)ethoxy]phenyl groups, respectively. It is a potent, selective, reversible, and ATP-competitive inhibitor of AMPK (AMP-activated protein kinase, EC 2.7.11.31) and a selective inhibitor of bone morphogenetic protein (BMP) signaling.	2.03	1	aromatic ether; piperidines; pyrazolopyrimidine; pyridines	bone morphogenetic protein receptor antagonist; EC 2.7.11.31 {[hydroxymethylglutaryl-CoA reductase (NADPH)] kinase} inhibitor
cgp 57380 CGP 57380: inhibits the mitogen-activated protein kinase-interacting kinase Mnk1	2.03	1	pyrazolopyrimidine
mdv 3100 [no description available]	2.1	1	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
bi d1870 [no description available]	2.03	1
pf-4708671 [no description available]	2.15	1
akt-i-1,2 compound Akt-I-1,2 compound: an aminopeptidase P inhibitor; structure in first source	2.03	1

Condition	Relationship Strength	Studies
Breast Cancer [description not available]	3.14	5
Cancer of Prostate [description not available]	2.08	1
Breast Neoplasms Tumors or cancer of the human BREAST.	3.14	5
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	2.08	1
Innate Inflammatory Response [description not available]	3.01	1
Benign Neoplasms [description not available]	3.01	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	3.01	1
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	3.01	1
Androgen-Independent Prostatic Cancer [description not available]	2.1	1
Prostatic Neoplasms, Castration-Resistant Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.	2.1	1
Astrocytoma, Grade IV [description not available]	2.11	1
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	2.11	1
ER-Negative PR-Negative HER2-Negative Breast Cancer [description not available]	2.13	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.13	1
Metastase [description not available]	2.13	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	2.13	1
Triple Negative Breast Neoplasms Breast neoplasms that do not express ESTROGEN RECEPTORS; PROGESTERONE RECEPTORS; and do not overexpress the NEU RECEPTOR/HER-2 PROTO-ONCOGENE PROTEIN.	2.13	1
Acute Lymphoid Leukemia [description not available]	2.15	1
Precursor Cell Lymphoblastic Leukemia-Lymphoma A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.	2.15	1
Basal Cell Cancer [description not available]	2.04	1
Adjuvant Arthritis [description not available]	2.07	1

sl0101

Description

Cross-References

Synonyms (27)

Research Excerpts

Overview

Protein Targets (4)

Inhibition Measurements

Activation Measurements

Biological Processes (39)

Molecular Functions (32)

Ceullar Components (9)

Bioassays (103)

Research

Studies (30)

Market Indicators

Research Demand Index: 31.71

Study Types

sl0101

Description

Cross-References

Synonyms (27)

Research Excerpts

Overview

Protein Targets (4)

Inhibition Measurements

Activation Measurements

Biological Processes (39)

Molecular Functions (32)

Ceullar Components (9)

Bioassays (103)

Research

Studies (30)

Market Indicators

Research Demand Index: 31.71

Study Types

Related Drugs (75)

Related Conditions (21)