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ci 988

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Description

PD 134308: selective cholecystokinin type B receptor antagonist; inhibits growth of LoVo, a human colon cancer cell line; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID108187
CHEMBL ID287735
CHEMBL ID2062154
SCHEMBL ID6895780
MeSH IDM0180339

Synonyms (30)

Synonym
pd-134,308
gtpl873
pd 134308
PDSP1_000899
PDSP2_000885
CHEMBL287735 ,
cid 108187
4-[[(1r)-2-[[(2r)-2-(2-adamantyloxycarbonylamino)-3-(1h-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
butanoic acid, 4-(((1r)-2-(((2r)-3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.1(3,7))dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-
unii-2637pdx9si
130332-27-3
ci 988
pd-134308
ci-988
SCHEMBL6895780
3-[[(1r)-2-[[(2r)-2-(2-adamantyloxycarbonylamino)-3-(1h-indol-3-yl)-2-methyl-propanoyl]amino]-1-phenyl-ethyl]carbamoyl]propanoic acid
NCGC00346874-01
2637pdx9si ,
CHEMBL2062154 ,
4-[[(1r)-2-[[(2r)-3-(1h-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-2-yloxy)carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
bdbm50449787
AKOS024457193
4-(((1r)-2-(((2r)-3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.13,7)dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxobutanoic acid
butanoic acid, 4-(((1r)-2-(((2r)-3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricycle(3.3.1.13,7)dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-
4-(((r)-2-((r)-2-(((adamantan-2-yloxy)carbonyl)amino)-3-(1h-indol-3-yl)-2-methylpropanamido)-1-phenylethyl)amino)-4-oxobutanoic acid
bdbm50230678
4-(((r)-2-((r)-2-(((adamantan-2-yloxy)carbonyl)amino)-3-(1h-indol-3-yl)-2-methylpropanamido)-1-phenylethyl)amino)-4-oxobutanoicacid
HY-105226
CS-0025414
DTXSID701099873

Research Excerpts

Pharmacokinetics

ExcerptReferenceRelevance
" Thus, there was a need to identify an analogue with an improved pharmacokinetic (PK) profile."( Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Boden, P; Eden, JM; Field, MJ; Hill, D; Hinton, JP; Holmes, A; Kneen, C; Padia, JK; Pritchard, MC; Rose, S; Singh, L; Suman-Chauhan, N; Trivedi, BK; Webdale, L; Wright, DS, 1998
)
0.3

Bioavailability

ExcerptReferenceRelevance
" However, during its development, it was determined that CI-988 had low bioavailability in both rodent and nonrodent species."( Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Boden, P; Eden, JM; Field, MJ; Hill, D; Hinton, JP; Holmes, A; Kneen, C; Padia, JK; Pritchard, MC; Rose, S; Singh, L; Suman-Chauhan, N; Trivedi, BK; Webdale, L; Wright, DS, 1998
)
0.3
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" These results indicate that distinct and contrasting dose-response profiles exist for these classical and atypical drugs in an animal model of anxiety based on electric shock."( Differential profile of the CCKB receptor antagonist CI-988 and diazepam in the four-plate test.
Dooley, DJ; Klamt, I, 1993
)
0.29
") were administered 30 min before determination of cocaine dose-response functions using a cumulative dosing method."( Effects of cholecystokinin antagonists on the discriminative stimulus effects of cocaine in rats and monkeys.
Massey, BW; Vanover, KE; Woolverton, WL, 1994
)
0.29
") did not shift the apomorphine dose-response curve (0."( Comparison of the effects of the cholecystokinin-B receptor antagonist, PD 134308, and the cholecystokinin-A receptor antagonist, L-364,718, on dopamine neuronal activity in the substantia nigra and ventral tegmental area.
Christoffersen, CL; Meltzer, LT; Razmpour, A; Serpa, KA, 1993
)
0.29
" The dose-response relationship of a new, potent and selective cholecystokinin B receptor antagonist, CI-988, on the growth of LoVo, a human colon cancer cell line, was studied in vivo."( Dose dependent in vivo inhibition of human colorectal cancer (LoVo) by the gastrin receptor antagonist, CI-988.
Howes, LG; Morris, DL; Romani, R, 1996
)
0.29
" The dose-response curve for RB 101 was shifted to the left and the duration of reflex depression was significantly prolonged."( CI 988, an antagonist of the cholecystokinin-B receptor, potentiates endogenous opioid-mediated antinociception at spinal level.
Elfvin, A; FourniƩ-Zaluski, MC; Hao, JX; Roques, BP; Wiesenfeld-Hallin, Z; Xu, XJ, 1997
)
0.3
" High-dose monkeys were dosed initially at 100 mg/kg, but the dose was not well tolerated and was decreased to 75 mg/kg after 8 days of treatment."( Gastric gland degeneration induced in monkeys by the CCK-B/gastrin receptor antagonist CI-988.
Bestervelt, LL; Breider, MA; Dethloff, LA; Robertson, DG; Tierney, BM,
)
0.13
" Although the compound is less water soluble than CI-988, oral bioavailability in rat was improved nearly 10 times relative to CI-988 when dosed in HP beta CD."( Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
Boden, P; Eden, JM; Field, MJ; Hill, D; Hinton, JP; Holmes, A; Kneen, C; Padia, JK; Pritchard, MC; Rose, S; Singh, L; Suman-Chauhan, N; Trivedi, BK; Webdale, L; Wright, DS, 1998
)
0.3
" Animals dosed with RB 120 (10 mg/kg) failed to develop a discriminative response."( Analgesic doses of the enkephalin degrading enzyme inhibitor RB 120 do not have discriminative stimulus properties.
FourniƩ-Zaluski, M; Hutcheson, DM; Maldonado, R; Pache, DM; Roques, BP; Sewell, RD; Subhan, F, 2000
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (6)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
EWS/FLI fusion proteinHomo sapiens (human)Potency1.34380.001310.157742.8575AID1259255; AID1259256
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)2.86720.00000.43624.3000AID52915; AID53030; AID53045
Cholecystokinin receptor type ARattus norvegicus (Norway rat)Ki0.00010.00010.27892.8900AID50518
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)IC50 (µMol)0.03000.00010.24801.4000AID51442
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)Ki0.09460.00060.11960.6800AID51462; AID51613
Cholecystokinin receptor type AHomo sapiens (human)IC50 (µMol)1.04710.00010.30381.9000AID52751
Gastrin/cholecystokinin type B receptorHomo sapiens (human)IC50 (µMol)0.00010.00010.36154.0000AID51097
Gastrin/cholecystokinin type B receptorHomo sapiens (human)Ki0.00090.00010.03660.3450AID50959; AID50965; AID51102
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.63100.00030.13770.6310AID312995
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (15)

Processvia Protein(s)Taxonomy
neuron migrationCholecystokinin receptor type AHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
axonogenesisCholecystokinin receptor type AHomo sapiens (human)
forebrain developmentCholecystokinin receptor type AHomo sapiens (human)
cholecystokinin signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
G protein-coupled receptor signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
cellular response to hormone stimulusCholecystokinin receptor type AHomo sapiens (human)
regulation of hormone secretionCholecystokinin receptor type AHomo sapiens (human)
gastric acid secretionGastrin/cholecystokinin type B receptorHomo sapiens (human)
cell surface receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cell population proliferationGastrin/cholecystokinin type B receptorHomo sapiens (human)
cholecystokinin signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
pH reductionGastrin/cholecystokinin type B receptorHomo sapiens (human)
digestive tract developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
gland developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
cholecystokinin receptor activityCholecystokinin receptor type AHomo sapiens (human)
peptide hormone bindingCholecystokinin receptor type AHomo sapiens (human)
peptide bindingCholecystokinin receptor type AHomo sapiens (human)
cholecystokinin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
protein bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
gastrin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
peptide hormone bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
type B gastrin/cholecystokinin receptor bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
1-phosphatidylinositol-3-kinase regulator activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
nucleoplasmCholecystokinin receptor type AHomo sapiens (human)
cytosolCholecystokinin receptor type AHomo sapiens (human)
plasma membraneCholecystokinin receptor type AHomo sapiens (human)
membraneCholecystokinin receptor type AHomo sapiens (human)
plasma membraneCholecystokinin receptor type AHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
intracellular membrane-bounded organelleGastrin/cholecystokinin type B receptorHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (66)

Assay IDTitleYearJournalArticle
AID312994Antagonist activity at CCK2 receptor in stomach-lumen perfused immature rat2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Rationalizing the activities of diverse cholecystokinin 2 receptor antagonists using molecular field points.
AID14266Maximum plasma concentration was evaluated in Hp-beta-CD solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID51613Inhibition by displacing [3H]CCK-8S against Cholecystokinin type B receptor of rat pancreatic membranes2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
AID50959Compound was tested for the affinity against Cholecystokinin type B receptor on guinea pig cortex.1997Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.
AID51462Compound was tested for binding affinity against rat brain Cholecystokinin type B receptor expressed in CHO cells.1997Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.
AID24043Pharmacokinetic parameter tmax was evaluated in Hp-beta-CD solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID110428Concentration in forebrain after intravenous injection evaluated after 10 min. at a dose of 10 mg/kg; Below low level of detection1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID50514Selectivity ratio defined as the ratio of IC50(CCK-A)/IC50(CCK-B)1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Amide bond replacements incorporated into CCK-B selective "dipeptoids".
AID51112Inhibition of [125I]CCK-8 binding to cholecystokinin type B receptor in the mouse cerebral cortex1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Amide bond replacements incorporated into CCK-B selective "dipeptoids".
AID14738Pharmacokinetic parameter AUC was evaluated in saline solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID52915Inhibition of [125I]CCK-8 binding to Cholecystokinin type A receptor in the rat pancreas1992Journal of medicinal chemistry, Apr-17, Volume: 35, Issue:8
Amide bond replacements incorporated into CCK-B selective "dipeptoids".
AID53045Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID51102Inhibition by displacing [3H]CCK-8S against human Cholecystokinin type B receptor2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
AID78501mCCK-8 contraction induced by 30 uM in vitro, normalized to CCK-8 (1 uM)1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID50513Ratio calculated as IC50 ratio of Cholecystokinin type A receptor to that of Cholecystokinin type B receptor1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID17954Absolute oral bioavailability was evaluated in saline solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID53030Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID110430Concentration in forebrain after intravenous injection evaluated after 20 min. at a dose of 10 mg/kg1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID51124Inhibitory concentration against radioligand [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type B receptor in the mouse cerebral cortex1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID51442Inhibition of inositol phosphate production induced by Cholecystokinin type B receptor (0.5 nM)1997Journal of medicinal chemistry, Nov-21, Volume: 40, Issue:24
Synthesis and biological properties of new constrained CCK-B antagonists: discrimination of two affinity states of the CCK-B receptor on transfected CHO cells.
AID51119Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to mouse cerebral cortex Cholecystokinin type B receptor1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID14737Pharmacokinetic parameter AUC was evaluated in Hp-beta-CD solution1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID14267Maximum plasma concentration was evaluated in saline solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID312995Displacement of [125I]BH-CCK-8S from CC1 receptor expressed in guinea pig pancreatic cells2008Journal of medicinal chemistry, Feb-14, Volume: 51, Issue:3
Rationalizing the activities of diverse cholecystokinin 2 receptor antagonists using molecular field points.
AID50965Inhibition by displacing [3H]CCK-8S against Cholecystokinin type B receptor of guinea pig2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
AID110432Concentration in forebrain after intravenous injection evaluated after 5 min. at a dose of 10 mg/kg1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID52751In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID51097In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type B receptor expressed in CHO-K1 cells1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID17953Absolute oral bioavailability was evaluated in Hp-beta-CD solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID24044Pharmacokinetic parameter tmax was evaluated in saline solution at a dose of 20 mg/kg orally1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID50518Inhibition by displacing [3H]CCK-8S against Cholecystokinin type A receptor of rat pancreatic membranes2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Synthesis and SAR of new 5-phenyl-3-ureido-1,5-benzodiazepines as cholecystokinin-B receptor antagonists.
AID229558Ratio of IC50 towards CCK-A receptor and CCK-B receptor1998Journal of medicinal chemistry, Jan-01, Volume: 41, Issue:1
Second generation "peptoid" CCK-B receptor antagonists: identification and development of N-(adamantyloxycarbonyl)-alpha-methyl-(R)-tryptophan derivative (CI-1015) with an improved pharmacokinetic profile.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1346883Human CCK2 receptor (Cholecystokinin receptors)1996Neuropeptides, Aug, Volume: 30, Issue:4
Pharmacological characterization of a Chinese hamster ovary cell line transfected with the human CCK-B receptor gene.
AID1346809Rat CCK1 receptor (Cholecystokinin receptors)1990Proceedings of the National Academy of Sciences of the United States of America, Sep, Volume: 87, Issue:17
Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
AID1346908Mouse CCK2 receptor (Cholecystokinin receptors)1990Proceedings of the National Academy of Sciences of the United States of America, Sep, Volume: 87, Issue:17
Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
AID51280Cholecystokinin type B receptor binding assay performed on homogenized cerebral cortex from male mouse1992Journal of medicinal chemistry, May-01, Volume: 35, Issue:9
Rationally designed "dipeptoid" analogues of CCK. A Free-Wilson/Fujita-Ban analysis of some alpha-methyltryptophan derivatives as CCK-B antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (142)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's109 (76.76)18.2507
2000's17 (11.97)29.6817
2010's10 (7.04)24.3611
2020's6 (4.23)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (5.44%)5.53%
Reviews7 (4.76%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other132 (89.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]