Compounds > sen 12333
Page last updated: 2024-11-13

sen 12333

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

Cross-References

ID SourceID
PubMed CID45484303
CHEMBL ID565540
CHEMBL ID1084615
SCHEMBL ID676043
MeSH IDM0535882

Synonyms (32)

Synonym
sen-12333
CHEMBL565540 ,
way-317538
CHEMBL1084615 ,
5-morpholin-4-ylpentanoic acid(4-pyridin-3-ylphenyl)amide hydrochloride
bdbm50300802
n-[4-(3-pyridinyl)phenyl]-4-morpholinepentanamide
way 317538
874450-44-9
sen 12333
SCHEMBL676043
AKOS024458162
DTXSID30670437
5-(morpholin-4-yl)-n-[4-(pyridin-3-yl)phenyl]pentanamide
5-morpholin-4-yl-pentanoic acid (4-pyridin-3-yl-phenyl)-amide
NCGC00379128-01
5-(4-morpholinyl)-n-(4-(3-pyridyl)phenyl)pentanamide
XCHIZTUBUXZESJ-UHFFFAOYSA-N ,
4-morpholinepentanamide, n-(4-(3-pyridinyl)phenyl)-
M92TU1EZ75 ,
n-(4-(3-pyridinyl)phenyl)-4-morpholinepentanamide
unii-m92tu1ez75
EX-A3487
5-morpholin-4-yl-n-(4-pyridin-3-ylphenyl)pentanamide
MS-25175
HY-107678
sen12333
5-morpholino-n-(4-(pyridin-3-yl)phenyl)pentanamide ,
BS171067
CS-0029164
F88156
AC-36424

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" One of the compounds of the series containing a urea moiety (16) was further shown to be a selective agonist of the alpha7 nAChR with excellent in vitro and in vivo profiles, brain penetration, and oral bioavailability and demonstrated in vivo efficacy in multiple behavioral cognition models."( Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-
Aschmies, S; Bothmann, H; Castaldo, C; Cocconcelli, G; Comery, TA; Di, L; Dunlop, J; Ghiron, C; Grauer, S; Harrison, B; Haydar, SN; Jow, F; Kowal, D; Kramer, A; La Rosa, S; Lock, T; Maccari, L; Marquis, KL; Micco, I; Nencini, A; Quinn, J; Robichaud, AJ; Roncarati, R; Scali, C; Terstappen, GC; Turlizzi, E; Valacchi, M; Varrone, M; Zanaletti, R; Zanelli, U, 2010)		0.36
"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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (7)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency21.31740.01237.983543.2770AID1645841
cytochrome P450 2D6Homo sapiens (human)Potency6.00810.00108.379861.1304AID1645840
[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)
Neuronal acetylcholine receptor subunit alpha-3Rattus norvegicus (Norway rat)Ki10.00000.00000.352210.0000AID1183536; AID1203762; AID654105
Neuronal acetylcholine receptor subunit alpha-4Rattus norvegicus (Norway rat)Ki10.00000.00000.12345.5000AID1183535; AID1203761; AID654104
Neuronal acetylcholine receptor subunit beta-2Rattus norvegicus (Norway rat)Ki10.00000.00000.10825.5000AID1183535; AID1203761; AID654104
Neuronal acetylcholine receptor subunit beta-4Rattus norvegicus (Norway rat)Ki10.00000.00000.296310.0000AID1183536; AID1203762; AID654105
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)Ki0.61330.00000.73078.0000AID1183534; AID1203760; AID654106
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)EC50 (µMol)9.39120.00021.848110.0000AID1183537; AID1203763; AID1203764; AID483822; AID654106; AID654108
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (21)

Assay IDTitleYearJournalArticle
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.
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine 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.
AID1203765Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells by patch-clamp electrophysiology assay relative to acetylcholine2015European journal of medicinal chemistry, May-05, Volume: 95Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
AID1203762Displacement of [3H]epibatidine from rat alpha3beta4 nAChR transfected in HEK293 cells by liquid scintillation counting2015European journal of medicinal chemistry, May-05, Volume: 95Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
AID1183537Agonist activity at rat nAChR alpha7 expressed in GH4C1 cells by fluorescent calcium assay2014European journal of medicinal chemistry, Sep-12, Volume: 84Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.
AID654107Partial agonist activity at wild type rat alpha7 nAChR expressed in Xenopus oocyte by voltage clamp electrophysiology assay relative to acetylcholine2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
AID654105Displacement of [3H]epibatidine from rat alpha3beta4 nAChR expressed in HEK292 cells after 4 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
AID1203764Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells by patch-clamp electrophysiology assay2015European journal of medicinal chemistry, May-05, Volume: 95Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
AID654104Displacement of [3H]epibatidine from rat alpha4beta2 nAChR expressed in HEK292 cells after 4 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
AID1203760Displacement of [3H]epibatidine from rat alpha7 nAChR transfected in HEK293 cells by liquid scintillation counting2015European journal of medicinal chemistry, May-05, Volume: 95Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
AID1183534Displacement of [3H]EB from rat nAChR alpha7 expressed in HEK293 cell membranes by liquid scintillation counting2014European journal of medicinal chemistry, Sep-12, Volume: 84Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.
AID654106Displacement of [3H]epibatidine from rat alpha7 nAChR expressed in HEK292 cells after 4 hrs by liquid scintillation counting2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
AID1183536Displacement of [3H]EB from rat nAChR alpha3beta4 expressed in HEK293 cell membranes by liquid scintillation counting2014European journal of medicinal chemistry, Sep-12, Volume: 84Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.
AID654108Partial agonist activity at wild type rat recombinant alpha7 nAChR expressed in Xenopus oocyte by voltage clamp electrophysiology assay2012Bioorganic & medicinal chemistry letters, Apr-01, Volume: 22, Issue:7
Consequences of linker length alteration of the α7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333.
AID1203761Displacement of [3H]epibatidine from rat alpha4beta2 nAChR transfected in HEK293 cells by liquid scintillation counting2015European journal of medicinal chemistry, May-05, Volume: 95Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
AID1203763Agonist activity at rat alpha7 nAChR expressed in GH4C1 cells by fluorescent calcium assay2015European journal of medicinal chemistry, May-05, Volume: 95Structure-activity relationship studies of SEN12333 analogues: determination of the optimal requirements for binding affinities at α7 nAChRs through incorporation of known structural motifs.
AID1183535Displacement of [3H]EB from rat nAChR alpha4beta2 expressed in HEK293 cell membranes by liquid scintillation counting2014European journal of medicinal chemistry, Sep-12, Volume: 84Investigations of amide bond variation and biaryl modification in analogues of α7 nAChR agonist SEN12333.
AID483822Agonist activity at rat alpha7 nAChR expressed in rat GH4C1 cells assessed as calcium flux by FLIPR2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
Novel alpha-7 nicotinic acetylcholine receptor agonists containing a urea moiety: identification and characterization of the potent, selective, and orally efficacious agonist 1-[6-(4-fluorophenyl)pyridin-3-yl]-3-(4-piperidin-1-ylbutyl) urea (SEN34625/WYE-
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's5 (71.43)24.3611
2020's2 (28.57)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.43

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 Index18.43 (24.57)
Research Supply Index2.08 (2.92)
Research Growth Index5.33 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.43)

All Compounds (24.57)

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%
Other7 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
ConditionIndicatedRelationship StrengthStudiesTrials
Congenital Zika Syndrome
[description not available]		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.2510
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.		02.2510