Page last updated: 2024-11-07

cgp 46381

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

Description

3-aminopropyl-cyclohexylmethylphosphinic acid: GABA-B receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID130022
SCHEMBL ID398615
MeSH IDM0228308

Synonyms (29)

Synonym
123691-14-5
cgp-46381
3-aminopropyl-(cyclohexylmethyl)phosphinic acid
cgp46381
gtpl1086
PDSP2_000414
PDSP1_000416
NCGC00025076-01
tocris-1247
BPBIO1_000552
cgp 46381
3-aminopropyl-cyclohexylmethylphosphinic acid
NCGC00025076-02
BIOMOL-NT_000238
L024114
3-aminopropyl(cyclohexylmethyl)phosphinic acid
phosphinic acid, (3-aminopropyl)(cyclohexylmethyl)-
XOESDNIUAWGCLU-UHFFFAOYSA-N
3-aminopropyl-(cyclohexylmethyl)-phosphinic acid
SCHEMBL398615
(3-aminopropyl)(cyclohexylmethyl)phosphinic acid
AKOS024456487
phosphinic acid, p-(3-aminopropyl)-p-(cyclohexylmethyl)-
DTXSID30154065
phosphinic acid,p-(3-aminopropyl)-p-(cyclohexylmethyl)-
J-004973
sr-01000597423
SR-01000597423-3
Q27075907

Research Excerpts

Treatment

ExcerptReferenceRelevance
"CGP 46381-treated rats took longer to learn the location of the escape platform and travelled a greater distance over the acquisition trials."( Hippocampal long-term potentiation and spatial learning in the rat: effects of GABAB receptor blockade.
Brucato, FH; Levin, ED; Lewis, DV; Mott, DD; Swartzwelder, HS; Wilson, WA, 1996
)
1.02
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
regulator of G-protein signaling 4Homo sapiens (human)Potency0.00600.531815.435837.6858AID504845
[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)
Gamma-aminobutyric acid type B receptor subunit 2Rattus norvegicus (Norway rat)IC50 (µMol)4.00000.00001.01016.8100AID71394
Gamma-aminobutyric acid type B receptor subunit 1Rattus norvegicus (Norway rat)IC50 (µMol)4.00000.00001.05326.8100AID71394
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

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.
AID175287The compound was tested for enhancement of electrically induced release of [3H]GABA from rat cortical slices.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.
AID71394Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Phosphinic acid analogues of GABA. 2. Selective, orally active GABAB antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's8 (32.00)18.2507
2000's12 (48.00)29.6817
2010's3 (12.00)24.3611
2020's2 (8.00)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 (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other25 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]