Page last updated: 2024-12-09

n-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine

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

Description

N-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine: an SK channel inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID772885
CHEMBL ID489770
SCHEMBL ID5155715
MeSH IDM000605452

Synonyms (31)

Synonym
n,4-dipyridin-2-yl-1,3-thiazol-2-amine
CBMICRO_026353
pyridin-2-yl-(4-pyridin-2-yl-thiazol-2-yl)-amine
ICA ,
BIM-0026443.P001
AKOS000361423
TCMDC-124275 ,
n-(4-(pyridin-2-yl)thiazol-2-yl)pyridin-2-amine
bdbm50264020
dndi1317482
gnf-pf-4773 ,
CHEMBL489770 ,
n-[4-(2-pyridinyl)-1,3-thiazol-2-yl]-2-pyridinamine
nsc-751858
nsc751858
n,4-bis(2-pyridyl)thiazol-2-amine
SCHEMBL5155715
mfcd00642222
3374-88-7
n,4-di(pyridin-2-yl)thiazol-2-amine
RYCUBTFYRLAMFA-UHFFFAOYSA-N
cambridge id 5625000
CS-7941
HY-22044
n-(pyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine
pyridin-2-yl-(4-pyridin-2-ylthiazol-2-yl)amine
ams_cnc_id-320211796
smssf-0625057
gw354586x
MS-23583
n-[4-(pyridin-2-yl)-1,3-thiazol-2-yl]pyridin-2-amine

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The orally bioavailable lead imidazolopiperazine confers complete causal prophylactic protection (15 milligrams/kilogram) in rodent models of malaria and shows potent in vivo blood-stage therapeutic activity."( Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
Barnes, SW; Bonamy, GM; Bopp, SE; Borboa, R; Bright, AT; Chatterjee, A; Che, J; Cohen, S; Dharia, NV; Diagana, TT; Fidock, DA; Froissard, P; Gagaring, K; Gettayacamin, M; Glynne, RJ; Gordon, P; Groessl, T; Kato, N; Kuhen, KL; Lee, MC; Mazier, D; McNamara, CW; Meister, S; Nagle, A; Nam, TG; Plouffe, DM; Richmond, W; Roland, J; Rottmann, M; Sattabongkot, J; Schultz, PG; Tuntland, T; Walker, JR; Winzeler, EA; Wu, T; Zhou, B; Zhou, Y, 2011
)
0.37
"48 h) after intravenous administration (1 mg/kg) and exposure (AUC0-24) following oral administration was 362 ng h/mL with absolute bioavailability of 8%."( Aminothiazoles: Hit to lead development to identify antileishmanial agents.
Bhuniya, D; Dere, RT; Deshpande, A; Gopinath, VS; Gupta, S; Launay, D; Martin, D; Moger, M; Mukkavilli, R; Pati, H; Pradhan, A; Puri, SK; Shivahare, R; Verma, A; Vishwakarma, P, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Histamine H1 receptorCavia porcellus (domestic guinea pig)IC50 (µMol)0.54300.00151.307210.0000AID387761
Small conductance calcium-activated potassium channel protein 1Homo sapiens (human)IC50 (µMol)0.04300.00400.02350.0430AID387519
Small conductance calcium-activated potassium channel protein 2Homo sapiens (human)IC50 (µMol)0.33300.01100.18400.5430AID387520; AID387761
Small conductance calcium-activated potassium channel protein 3Homo sapiens (human)IC50 (µMol)0.28600.00400.53462.0000AID387515; AID387516; AID387518
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (5)

Processvia Protein(s)Taxonomy
potassium ion transportSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
chemical synaptic transmissionSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
potassium ion transmembrane transportSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
potassium ion transportSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
potassium ion transmembrane transportSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
membrane repolarization during atrial cardiac muscle cell action potentialSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
regulation of potassium ion transmembrane transportSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
potassium ion transmembrane transportSmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
inward rectifier potassium channel activitySmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
calcium-activated potassium channel activitySmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
small conductance calcium-activated potassium channel activitySmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
calmodulin bindingSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
inward rectifier potassium channel activitySmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
protein bindingSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
calcium-activated potassium channel activitySmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
small conductance calcium-activated potassium channel activitySmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
protein domain specific bindingSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
protein homodimerization activitySmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
alpha-actinin bindingSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
calmodulin bindingSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
inward rectifier potassium channel activitySmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
calmodulin bindingSmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
small conductance calcium-activated potassium channel activitySmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (10)

Processvia Protein(s)Taxonomy
plasma membraneSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
synapseSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
voltage-gated potassium channel complexSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
neuronal cell bodySmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
neuron projectionSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
plasma membraneSmall conductance calcium-activated potassium channel protein 1Homo sapiens (human)
plasma membraneSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
cell surfaceSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
membraneSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
Z discSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
dendritic spineSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
neuronal cell bodySmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
plasma membraneSmall conductance calcium-activated potassium channel protein 2Homo sapiens (human)
cytoplasmSmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
plasma membraneSmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
neuron projectionSmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
plasma membraneSmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
neuronal cell bodySmall conductance calcium-activated potassium channel protein 3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (31)

Assay IDTitleYearJournalArticle
AID1159588Biochemical screen of P. falciparum CDPK42016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159589Biochemical screen of P. falciparum MAPK22016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159585Biochemical screen of P. falciparum CDPK12016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159586Biochemical screen of P. falciparum PK62016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID1159587Biochemical screen of P. falciparum PK72016PloS one, , Volume: 11, Issue:3
Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds.
AID387761Displacement of [125I]apamin from Kca2.2 channel expressed in HEK293 cells2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID1250476Cytotoxicity in human KB cells assessed as cell viability incubated for 72 hrs by MTT assay2015European journal of medicinal chemistry, Sep-18, Volume: 102Aminothiazoles: Hit to lead development to identify antileishmanial agents.
AID387516Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID779958Antitubercular activity against Mycobacterium tuberculosis H37Rv in Middlebrook 7H9 broth with butyrate after 7 to 14 days by broth microdilution method2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Structure-activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis.
AID387518Displacement of [125I]apamin from Kca2.3 channel expressed in HEK293 cells by scintillation proximity assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID449706NOVARTIS: Inhibition Frequency Index (IFI) - the number of HTS assays where a compound showed > 50% inhibition/induction, expressed as a percentage of the number of assays in which the compound was tested.2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID449705NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID387519Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID1250479Metabolic stability in golden Syrian hamster liver microsomes assessed as drug metabolism at 0.5 uM incubated for 30 mins in presence of NADPH2015European journal of medicinal chemistry, Sep-18, Volume: 102Aminothiazoles: Hit to lead development to identify antileishmanial agents.
AID1250480Metabolic stability in CD1 mouse liver microsomes assessed as drug metabolism at 0.5 uM incubated for 30 mins in presence of NADPH2015European journal of medicinal chemistry, Sep-18, Volume: 102Aminothiazoles: Hit to lead development to identify antileishmanial agents.
AID449704NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID387514Inhibition of Kca2.3 channel expressed in HEK293 cells at 30 uM by thallium flux assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID449703NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay 2008Proceedings of the National Academy of Sciences of the United States of America, Jul-01, Volume: 105, Issue:26
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen.
AID1250477Selectivity index, ratio of CC50 for human KB cells to IC50 for Leishmania donovani MHOM/IN/80/Dd8 amastigotes.2015European journal of medicinal chemistry, Sep-18, Volume: 102Aminothiazoles: Hit to lead development to identify antileishmanial agents.
AID387515Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID387521Inhibition of Kca3.1 channel expressed in HEK293 cells by thallium flux assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID779959Antitubercular activity against Mycobacterium tuberculosis H37Rv in Middlebrook 7H9 broth with glucose after 7 to 14 days by broth microdilution method2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Structure-activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis.
AID602118NOVARTIS: Antimalarial liver stage activity measured as a greater than 50% reduction in Plasmodium yoelii schizont area in HepG2-A16-CD81 cells at 10uM compound concentration, determined by immuno-fluorescence.2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
AID1250475Antileishmanial activity against Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase reporter gene infected in mouse J-774A1 cells assessed as inhibition of amastigote stage formation incubated for 72 hrs by luminometry2015European journal of medicinal chemistry, Sep-18, Volume: 102Aminothiazoles: Hit to lead development to identify antileishmanial agents.
AID779957Antitubercular activity against Mycobacterium tuberculosis H37Rv in GAST media with glycerol and alanine after 7 to 14 days by broth microdilution method2013Bioorganic & medicinal chemistry, Nov-01, Volume: 21, Issue:21
Structure-activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis.
AID1250478Solubility in sodium phosphate buffer at pH 7.4 incubated for 2 hrs at room temperature by UV spectrometry method2015European journal of medicinal chemistry, Sep-18, Volume: 102Aminothiazoles: Hit to lead development to identify antileishmanial agents.
AID387520Inhibition of Kca2.2 channel expressed in HEK293 cells by thallium flux assay2008Bioorganic & medicinal chemistry letters, Oct-01, Volume: 18, Issue:19
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
AID1159537qHTS screening for TAG (triacylglycerol) accumulators in algae2017Plant physiology, Aug, Volume: 174, Issue:4
Identification and Metabolite Profiling of Chemical Activators of Lipid Accumulation in Green Algae.
AID602156Novartis GNF Liver Stage Dataset: Malariabox Annotation2011Science (New York, N.Y.), Dec-09, Volume: 334, Issue:6061
Imaging of Plasmodium liver stages to drive next-generation antimalarial drug discovery.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (18.18)29.6817
2010's8 (72.73)24.3611
2020's1 (9.09)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.59

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 weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.59 (24.57)
Research Supply Index2.48 (2.92)
Research Growth Index5.08 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.59)

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%
Other11 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]