l803087 profile

L803087: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

L-803087 : A fluoroindole that is 1H-indole substituted by phenyl, 4-{[(2S)-5-carbamimidamido-1-methoxy-1-oxopentan-2-yl]amino}-4-oxobutyl, fluoro and fluoro groups at positions 2, 3, 5 and 7, respectively. It is a selective nonpeptidic agonist of the somatostatin subtype-4 (SST4) receptor with Ki of 0.7 nM. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	5311374
CHEMBL ID	1450103
MeSH ID	M0392010

Synonym
gtpl2082
l803087
l-803,087
NCGC00161823-01 ,
methyl (2s)-5-(diaminomethylideneamino)-2-[4-(5,7-difluoro-2-phenyl-1h-indol-3-yl)butanoylamino]pentanoate
l-803087
217480-26-7
CHEMBL1450103
n2-(4-(5,7-difluoro-2-phenyl-1h-indol-3-yl)-1-oxobutyl)-l-arginine methyl ester
CS-0028987
HY-108497
Q27078440
AT23608
MS-29022
AKOS040733566

Role	Description
somatostatin receptor agonist	An agonist that binds to and activates somatostatin receptors.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Class	Description
methyl ester	Any carboxylic ester resulting from the formal condensation of a carboxy group with methanol.
secondary carboxamide	A carboxamide resulting from the formal condensation of a carboxylic acid with a primary amine; formula RC(=O)NHR(1).
benzenes	Any benzenoid aromatic compound consisting of the benzene skeleton and its substituted derivatives.
fluoroindole	An organofluorine compound that is a compound based on an indole skeleton, containing one or more fluorine atoms.
guanidines	Any organonitrogen compound containing a carbamimidamido (guanidino) group. Guanidines have the general structure (R(1)R(2)N)(R(3)R(4)N)C=N-R(5) and are related structurally to amidines and ureas.
L-arginine derivative	A proteinogenic amino acid derivative resulting from reaction of L-arginine at the amino group, the carboxy group, or the guanidyl group, or from the replacement of any hydrogen of L-arginine by a heteroatom.
phenylindole
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (11)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASE	Homo sapiens (human)	Potency	19.9526	0.0040	23.8416	100.0000	AID485290
phosphopantetheinyl transferase	Bacillus subtilis	Potency	56.2341	0.1413	37.9142	100.0000	AID1490
glucocerebrosidase	Homo sapiens (human)	Potency	15.8489	0.0126	8.1569	44.6684	AID2101
euchromatic histone-lysine N-methyltransferase 2	Homo sapiens (human)	Potency	7.9433	0.0355	20.9770	89.1251	AID504332
Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)	Potency	22.3872	0.3162	12.7657	31.6228	AID881
Histamine H2 receptor	Cavia porcellus (domestic guinea pig)	Potency	22.3872	0.0063	8.2350	39.8107	AID881
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Somatostatin receptor type 1	Homo sapiens (human)	IC50 (µMol)	1.0000	0.0001	0.0013	0.0022	AID203255; AID203256; AID203257
Somatostatin receptor type 2	Homo sapiens (human)	IC50 (µMol)	7.0000	0.0004	0.0024	0.0140	AID203392; AID203393; AID203394
Somatostatin receptor type 2	Homo sapiens (human)	Ki	4.7200	0.0000	0.4091	4.7200	AID1571206
Somatostatin receptor type 4	Homo sapiens (human)	IC50 (µMol)	0.0042	0.0001	0.0021	0.0042	AID203554; AID203555; AID203556
Somatostatin receptor type 4	Homo sapiens (human)	Ki	0.0007	0.0006	0.2733	3.2000	AID1571205
Somatostatin receptor type 3	Homo sapiens (human)	IC50 (µMol)	7.0000	0.0004	0.1110	0.8800	AID203412; AID203413; AID203414
Somatostatin receptor type 5	Homo sapiens (human)	IC50 (µMol)	10.0000	0.0002	0.0472	0.3930	AID203573; AID203574; AID203575
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (43)

Process	via Protein(s)	Taxonomy
lipid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
phospholipid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
apoptotic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of cell population proliferation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of macrophage derived foam cell differentiation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
arachidonic acid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of cell migration	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
prostate gland development	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
regulation of epithelial cell differentiation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of chemokine production	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathway	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
positive regulation of keratinocyte differentiation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of cell cycle	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
negative regulation of growth	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
hepoxilin biosynthetic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
endocannabinoid signaling pathway	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
cannabinoid biosynthetic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipoxin A4 biosynthetic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
linoleic acid metabolic process	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipid oxidation	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipoxygenase pathway	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 1	Homo sapiens (human)
glutamate receptor signaling pathway	Somatostatin receptor type 1	Homo sapiens (human)
spermatogenesis	Somatostatin receptor type 1	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 1	Homo sapiens (human)
cerebellum development	Somatostatin receptor type 1	Homo sapiens (human)
forebrain development	Somatostatin receptor type 1	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 1	Homo sapiens (human)
response to starvation	Somatostatin receptor type 1	Homo sapiens (human)
cellular response to leukemia inhibitory factor	Somatostatin receptor type 1	Homo sapiens (human)
cellular response to estradiol stimulus	Somatostatin receptor type 1	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 1	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 2	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Somatostatin receptor type 2	Homo sapiens (human)
spermatogenesis	Somatostatin receptor type 2	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 2	Homo sapiens (human)
cerebellum development	Somatostatin receptor type 2	Homo sapiens (human)
peristalsis	Somatostatin receptor type 2	Homo sapiens (human)
forebrain development	Somatostatin receptor type 2	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 2	Homo sapiens (human)
response to starvation	Somatostatin receptor type 2	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Somatostatin receptor type 2	Homo sapiens (human)
cellular response to estradiol stimulus	Somatostatin receptor type 2	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 2	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 4	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 4	Homo sapiens (human)
cell migration	Somatostatin receptor type 4	Homo sapiens (human)
forebrain development	Somatostatin receptor type 4	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Somatostatin receptor type 4	Homo sapiens (human)
positive regulation of arachidonic acid secretion	Somatostatin receptor type 4	Homo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Somatostatin receptor type 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 3	Homo sapiens (human)
cell-cell signaling	Somatostatin receptor type 3	Homo sapiens (human)
spermatogenesis	Somatostatin receptor type 3	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 3	Homo sapiens (human)
hormone-mediated apoptotic signaling pathway	Somatostatin receptor type 3	Homo sapiens (human)
cerebellum development	Somatostatin receptor type 3	Homo sapiens (human)
forebrain development	Somatostatin receptor type 3	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 3	Homo sapiens (human)
response to starvation	Somatostatin receptor type 3	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Somatostatin receptor type 3	Homo sapiens (human)
cellular response to estradiol stimulus	Somatostatin receptor type 3	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 3	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Somatostatin receptor type 5	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 5	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 5	Homo sapiens (human)
positive regulation of cytokinesis	Somatostatin receptor type 5	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 5	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Somatostatin receptor type 5	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 5	Homo sapiens (human)
regulation of insulin secretion	Somatostatin receptor type 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (13)

Process	via Protein(s)	Taxonomy
iron ion binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
calcium ion binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
protein binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
lipid binding	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
linoleate 13S-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
arachidonate 8(S)-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
arachidonate 15-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
linoleate 9S-lipoxygenase activity	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 1	Homo sapiens (human)
protein binding	Somatostatin receptor type 1	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 1	Homo sapiens (human)
protein binding	Somatostatin receptor type 2	Homo sapiens (human)
PDZ domain binding	Somatostatin receptor type 2	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 2	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 2	Homo sapiens (human)
protein binding	Somatostatin receptor type 4	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 4	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 4	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 3	Homo sapiens (human)
signaling receptor binding	Somatostatin receptor type 3	Homo sapiens (human)
protein binding	Somatostatin receptor type 3	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 3	Homo sapiens (human)
G protein-coupled receptor activity	Somatostatin receptor type 3	Homo sapiens (human)
protein binding	Somatostatin receptor type 5	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 5	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Process	via Protein(s)	Taxonomy
nucleus	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
cytosol	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
cytoskeleton	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
plasma membrane	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
adherens junction	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
focal adhesion	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
membrane	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
extracellular exosome	Polyunsaturated fatty acid lipoxygenase ALOX15B	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 1	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 1	Homo sapiens (human)
neuron projection	Somatostatin receptor type 1	Homo sapiens (human)
cytosol	Somatostatin receptor type 2	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 2	Homo sapiens (human)
neuron projection	Somatostatin receptor type 2	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 2	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 4	Homo sapiens (human)
neuron projection	Somatostatin receptor type 4	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 4	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 3	Homo sapiens (human)
cilium	Somatostatin receptor type 3	Homo sapiens (human)
ciliary membrane	Somatostatin receptor type 3	Homo sapiens (human)
non-motile cilium	Somatostatin receptor type 3	Homo sapiens (human)
neuron projection	Somatostatin receptor type 3	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 3	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 5	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 5	Homo sapiens (human)
neuron projection	Somatostatin receptor type 5	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay ID	Title	Year	Journal	Article
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347154	Primary screen GU AMC 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.
AID203412	Binding affinity towards human Somatostatin receptor type 3 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
AID203394	Binding affinity towards human somatostatin receptor type 2 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
AID1571206	Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST2 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
AID203574	Binding affinity at human Somatostatin receptor type 5 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
AID203414	Binding affinity towards human somatostatin receptor type 3 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
AID203555	Binding affinity at human Somatostatin receptor type 4 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
AID203257	Binding affinity towards human somatostatin receptor type 1 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
AID203256	Binding affinity at human Somatostatin receptor type 1 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
AID203413	Binding affinity at human Somatostatin receptor type 3 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
AID1571205	Displacement of 3-[125I]iodotyrosyl25-somatostatin-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 45 mins by scintillation counting method
AID203573	Binding affinity towards human Somatostatin receptor type 5 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
AID203255	Binding affinity towards human Somatostatin receptor type 1 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
AID203575	Binding affinity towards human somatostatin receptor type 5 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
AID203554	Binding affinity towards human Somatostatin receptor type 4 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
AID203392	Binding affinity towards human Somatostatin receptor type 2 using 125I-[Leu,DTrp,Tyr]SRIF-28 as radioligand	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan.
AID203556	Binding affinity towards human somatostatin receptor type 4 using [125I][Leu8,D-Trp22,Tyr25]SRIF-28 as radioligand.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling.
AID203393	Binding affinity at human Somatostatin receptor type 2 by [125I][Leu8,D-Trp22,Tyr25]SRIF-28 displacement.	2003	Journal of medicinal chemistry, Dec-18, Volume: 46, Issue:26	Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8.
AID1346359	Human SST4 receptor (Somatostatin receptors)	1998	Science (New York, N.Y.), Oct-23, Volume: 282, Issue:5389	Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.
[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	1 (5.88)	18.2507
2000's	9 (52.94)	29.6817
2010's	5 (29.41)	24.3611
2020's	2 (11.76)	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	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	18 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
2-amino-5-phosphonovalerate 2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.	2.05	1	non-proteinogenic alpha-amino acid	NMDA receptor antagonist
pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.	2.06	1	pilocarpine	antiglaucoma drug
glutamic acid Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2.	2.05	1	glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid	Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical
colforsin Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.	2.43	2	acetate ester; cyclic ketone; labdane diterpenoid; organic heterotricyclic compound; tertiary alpha-hydroxy ketone; triol	adenylate cyclase agonist; anti-HIV agent; antihypertensive agent; plant metabolite; platelet aggregation inhibitor; protein kinase A agonist
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.	2.04	1	N-[2-(4-bromocinnamylamino)ethyl]isoquinoline-5-sulfonamide
6-cyano-7-nitroquinoxaline-2,3-dione 6-Cyano-7-nitroquinoxaline-2,3-dione: A potent excitatory amino acid antagonist with a preference for non-NMDA iontropic receptors. It is used primarily as a research tool.	2.05	1	quinoxaline derivative
dinoprostone prostaglandin E2 : Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostaglandins.	2.04	1	prostaglandins E	human metabolite; mouse metabolite; oxytocic
l796778 L796778: structure in first source. L-796,778 : A methyl ester resulting from the formal condensation of the carboxy group of N-{[(2S)-1-(4-nitroanilino)-1-oxo-3-phenylpropan-2-yl]carbamoyl}-D-norleucyl-L-lysine with methanol. It is a partial agonist of somatostatin subtype receptor 3 (Ki = 24 nM) that exhibits anticonvulsant effects.	3.28	6	benzenes; C-nitro compound; L-lysine derivative; L-phenylalanine derivative; methyl ester; oligopeptide; secondary carboxamide; ureas	somatostatin receptor agonist
l 779976 L 779976: a somatostatin 2 receptor agonist. L-779976 : A member of the class of indoles that is (betaS)-beta-methyl-D-tryptophan in which the primary amino group undergoes formal condensation with the carboxy group of 4-(2-oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidine-1-carboxylic acid and the carboxy group undegoes formal condensation with the amino group of (1R,3S)-cyclohexane-1,3-diyldimethanamine. It is a selective nonpeptidic agonist of the somatostatin subtype-2 (SST2) receptor with Ki of 0.05 nM.	3.13	5	benzimidazoles; indoles; piperidinecarboxamide; primary amino compound; secondary carboxamide	neuroprotective agent; somatostatin receptor agonist
l797591 L797591: structure in first source	2.71	3
somatostatin, n-tyr(1)- [no description available]	2.01	1
cyn 154806 [no description available]	2.04	1
l 817818 L 817818: somatostatin 5 receptor agonist. L-817818 : A benzoindole that is 1H-benzo[g]indole substituted by naphthalen-2-yl and 2-({(2R)-6-amino-1-[(2S)-2-aminopropoxy]-1-oxohexan-2-yl}amino)-2-oxoethyl groups at positions 2 and 3, respectively. It is a selective nonpeptidic agonist of the somatostatin subtype-5 (SST5) receptor with Ki of 0.4 nM.	2.42	2
piperidines Piperidines: A family of hexahydropyridines.	2.11	1
ch 275 [no description available]	2.05	1

Condition	Relationship Strength	Studies
Congenital Zika Syndrome [description not available]	2.25	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.52	2
Zika Virus Infection A viral disease transmitted by the bite of AEDES mosquitoes infected with ZIKA VIRUS. Its mild DENGUE-like symptoms include fever, rash, headaches and ARTHRALGIA. The viral infection during pregnancy, in rare cases, is associated with congenital brain and ocular abnormalities, called Congenital Zika Syndrome, including MICROCEPHALY and may also lead to GUILLAIN-BARRE SYNDROME.	2.25	1
Brain Inflammation [description not available]	2.04	1
Encephalitis Inflammation of the BRAIN due to infection, autoimmune processes, toxins, and other conditions. Viral infections (see ENCEPHALITIS, VIRAL) are a relatively frequent cause of this condition.	2.04	1
Absence Seizure [description not available]	2.06	1
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	2.06	1

l803087

Description

Cross-References

Synonyms (15)

Roles (1)

Drug Classes (7)

Protein Targets (11)

Potency Measurements

Inhibition Measurements

Biological Processes (43)

Molecular Functions (13)

Ceullar Components (12)

Bioassays (20)

Research

Studies (17)

Market Indicators

Research Demand Index: 12.46

Study Types

l803087

Description

Cross-References

Synonyms (15)

Roles (1)

Drug Classes (7)

Protein Targets (11)

Potency Measurements

Inhibition Measurements

Biological Processes (43)

Molecular Functions (13)

Ceullar Components (12)

Bioassays (20)

Research

Studies (17)

Market Indicators

Research Demand Index: 12.46

Study Types

Related Drugs (15)

Related Conditions (7)