Page last updated: 2024-11-07

fk 888

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

FK 888: structure given in first source; a potent NK(1) receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID107967
CHEMBL ID1416993
CHEBI ID93463
SCHEMBL ID8079679
MeSH IDM0211484

Synonyms (28)

Synonym
HMS3269A13 ,
BRD-K83508485-001-01-9
gtpl2114
(2s,4r)-4-hydroxy-1-(1-methylindole-3-carbonyl)-n-[(2s)-1-(methyl-(phenylmethyl)amino)-3-naphthalen-2-yl-1-oxopropan-2-yl]pyrrolidine-2-carboxamide
fk-888
PDSP2_000648
NCGC00159560-01
fk 888
(2s,4r)-n-[(2s)-1-[benzyl(methyl)amino]-3-naphthalen-2-yl-1-oxopropan-2-yl]-4-hydroxy-1-(1-methylindole-3-carbonyl)pyrrolidine-2-carboxamide
138449-07-7
l-alaninamide, trans-4-hydroxy-1-((1-methyl-1h-indol-3-yl)carbonyl)-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-
fk888
l-alaninamide, (4r)-4-hydroxy-1-((1-methyl-1h-indol-3-yl)carbonyl)-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-
SCHEMBL8079679
AKOS024457076
CHEMBL1416993
(4r)-4-hydroxy-1-[(1-methyl-1h-indol-3-yl)carbonyl]-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-l-alaninamide
DTXSID70160680
CHEBI:93463
HMS3677K12
Q27077302
HMS3413K12
l-alaninamide, (4r)-4-hydroxy-1-[(1-methyl-1h-indol-3-yl)carbonyl]-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-
HY-105215
CS-0025377
DZQ7B7BPD4
(2s)-n-benzyl-2-{[(2s,4r)-4-hydroxy-1-(1-methyl-1h-indole-3-carbonyl)pyrrolidin-2-yl]formamido}-n-methyl-3-(naphthalen-2-yl)propanamide
l-alaninamide, trans-4-hydroxy-1-[(1-methyl-1h-indol-3-yl)carbonyl]-l-prolyl-n-methyl-3-(2-naphthalenyl)-n-(phenylmethyl)-

Research Excerpts

Treatment

ExcerptReferenceRelevance
"FK 888 treatment decreased efficacy of ileal contraction in both the control and irradiated rat but surprisingly it increased potency at day 3 and decreased it at day 14 in the irradiated rat."( A substance P receptor antagonist (FK 888) modifies gut alterations induced by ionizing radiation.
Esposito, V; Griffiths, NM; Linard, C; Mathe, D; Wysocki, J, 1998
)
1.3

Dosage Studied

ExcerptRelevanceReference
" C or D alone shifted dose-response curves to capsaicin (from 10(-7) M to 10(-3) M) to lower concentrations compared with the control, and C+D further shifted them."( Angiotensin-converting enzyme inhibitor and danazol increase sensitivity of cough reflex in female guinea pigs.
Ebihara, T; Nakazawa, H; Ohrui, T; Sasaki, H; Sekizawa, K, 1996
)
0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
peptideAmide derived from two or more amino carboxylic acid molecules (the same or different) by formation of a covalent bond from the carbonyl carbon of one to the nitrogen atom of another with formal loss of water. The term is usually applied to structures formed from alpha-amino acids, but it includes those derived from any amino carboxylic acid. X = OH, OR, NH2, NHR, etc.
[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 (4)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, CruzipainTrypanosoma cruziPotency8.91250.002014.677939.8107AID1476
Microtubule-associated protein tauHomo sapiens (human)Potency31.62280.180013.557439.8107AID1460
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency22.38720.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency22.38720.00638.235039.8107AID881
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (21)

Processvia Protein(s)Taxonomy
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings 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.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346371Human NK2 receptor (Tachykinin receptors)2002Pharmacology, May, Volume: 65, Issue:2
Effect of YM-44781, YM-44778 and YM-49598, novel tachykinin antagonists, in a drug-induced bladder contraction model.
AID1346346Human NK1 receptor (Tachykinin receptors)1996American journal of respiratory and critical care medicine, Mar, Volume: 153, Issue:3
A neurokinin 1-receptor antagonist improves exercise-induced airway narrowing in asthmatic patients.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (95)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's68 (71.58)18.2507
2000's23 (24.21)29.6817
2010's2 (2.11)24.3611
2020's2 (2.11)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.29

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.

MetricThis Compound (vs All)
Research Demand Index20.29 (24.57)
Research Supply Index4.61 (2.92)
Research Growth Index4.31 (4.65)
Search Engine Demand Index21.17 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.29)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2 (2.06%)5.53%
Reviews1 (1.03%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other94 (96.91%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]