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cholecystokinin antagonist

A hormone antagonist that inhibits the action of the peptide hormone cholecystokinin.

ChEBI ID: 73296

Members (3)

MemberDefinitionClass
asperlicin cA member of the class of asperlicins in which the core 6,7-dihydroquinazolino[3,2-a][1,4]benzodiazepine-5,13-dione skeleton is substituted at the 7 pro-S position by an indol-3-ylmethyl group. It is a cholecystokinin antagonist.asperlicin C
devazepideAn indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.devazepide
proglumideA racemate composed of equal amounts of (R)- and (S)-proglumide. A non-selective CCK antagonist that was used primarily for treatment of stomach ulcers, but has been replaced by newer drugs.N(2)-benzoyl-N,N-dipropyl-alpha-glutamine; proglumide

Research

Studies (1,477)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990330 (22.34)18.7374
1990's822 (55.65)18.2507
2000's223 (15.10)29.6817
2010's85 (5.75)24.3611
2020's17 (1.15)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials98 (6.08%)5.53%
Reviews40 (2.48%)6.00%
Case Studies2 (0.12%)4.05%
Observational0 (0.00%)0.25%
Other1,473 (91.32%)84.16%

Protein Targets (50)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
activating transcription factor 6Homo sapiens (human)Potency26.168422
AR proteinHomo sapiens (human)Potency16.730355
aryl hydrocarbon receptorHomo sapiens (human)Potency10.437522
Ataxin-2Homo sapiens (human)Potency11.883211
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency12.115622
caspase-3Cricetulus griseus (Chinese hamster)Potency23.710111
Caspase-7Cricetulus griseus (Chinese hamster)Potency23.710111
Cellular tumor antigen p53Homo sapiens (human)Potency26.779722
Chain A, Beta-lactamaseEscherichia coli K-12Potency7.943311
Chain A, CruzipainTrypanosoma cruziPotency39.810711
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency63.095711
chromobox protein homolog 1Homo sapiens (human)Potency89.125111
cytochrome P450 2C9, partialHomo sapiens (human)Potency2.754011
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency29.849311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency1.258911
endonuclease IVEscherichia coliPotency14.125411
estrogen nuclear receptor alphaHomo sapiens (human)Potency10.587188
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency5.955711
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency4.698255
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency31.622811
farnesoid X nuclear receptorHomo sapiens (human)Potency13.864022
GVesicular stomatitis virusPotency2.754011
gemininHomo sapiens (human)Potency8.303923
GLI family zinc finger 3Homo sapiens (human)Potency8.911211
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency20.154822
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency6.682411
heat shock protein beta-1Homo sapiens (human)Potency29.847022
histone deacetylase 9 isoform 3Homo sapiens (human)Potency0.059611
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency2.754011
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.832511
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency2.754012
Interferon betaHomo sapiens (human)Potency2.754011
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency16.573422
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency30.106511
peripheral myelin protein 22Rattus norvegicus (Norway rat)Potency16.377622
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency8.582533
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency5.011911
TDP1 proteinHomo sapiens (human)Potency22.425522
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency5.843622
thyroid stimulating hormone receptorHomo sapiens (human)Potency13.333211
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency23.914511
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency6.682411

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Bile salt export pumpHomo sapiens (human)IC5010.000011
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC50400.135012
Cholecystokinin receptor type AHomo sapiens (human)IC500.000233
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC5019.23161213
Cholecystokinin receptor type AHomo sapiens (human)Ki0.000922
Cholecystokinin receptor type ARattus norvegicus (Norway rat)Ki0.000422
Collagenase 3Homo sapiens (human)Ki0.001811
Gastrin/cholecystokinin type B receptorHomo sapiens (human)IC500.245011
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)IC500.000811
Gastrin/cholecystokinin type B receptorHomo sapiens (human)Ki0.056033
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)Ki0.269211
Histamine H2 receptorRattus norvegicus (Norway rat)IC502,500.000011