Page last updated: 2024-09-22

phenthiazamine

Description

phenthiazamine: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID40302
CHEMBL ID175296
SCHEMBL ID44869
MeSH IDM0092785

Synonyms (68)

Synonym
EU-0063644
4-phenyl-2-thiazolamine ,
BB 0245862
UPCMLD0ENAT5678764:001
wf2822rius ,
unii-wf2822rius
2-amino-4-phenylthiazole
2010-06-2
nsc-2528
2-thiazolamine, 4-phenyl-
thiazole, 2-amino-4-phenyl-
nsc2528
wln: t5n csj bz er
4-phenyl-1,3-thiazol-2-amine
MLS000532681
smr000140119
AA-516/30011003
TIMTEC1_005286
4-phenylthiazol-2-amine
OPREA1_292792
STK094617
4-phenyl-thiazol-2-ylamine
2-amino-4-phenylthiazole, 97%
f 1653
nsc 2528
2-amino-4-phenyl-1,3-thiazole
phenthiazamine
einecs 217-926-8
OPREA1_388404
NCGC00173708-01
HMS1549A06
AKOS000104231
thiazol-2-amine, 1
bdbm31190
EC-000.2144
CHEMBL175296
phenylthiazol-2-amine
A23362
HMS2469I21
(4-phenyl-thiazol-2-yl)-amine
AM803994
F0138-3243
F1386-0378
FT-0611135
4-phenyl 2-amino thiazole
4-phenyl-2-aminothiazole
2-amino-4-phenyl-thiazole
2-amino-4-phenylthiazol
SCHEMBL44869
5K-598S
DTXSID4043804
4-phenyl-1,3-thiazol-2-amine #
4-phenyl-2-thiazolylamine
cambridge id 5121788
j37.311g ,
A2846
J-515954
mfcd00039680
J-013012
sr-01000583105
SR-01000583105-1
BCP25122
EN300-02104
Q27292601
SY005299
PD021214
CS-W017405
Z48847603

Protein Targets (10)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency14.12545.623417.292931.6228AID485281
LuciferasePhotinus pyralis (common eastern firefly)Potency33.80780.007215.758889.3584AID588342
ATAD5 protein, partialHomo sapiens (human)Potency14.58100.004110.890331.5287AID504466; AID504467
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency39.81070.035520.977089.1251AID504332
chromobox protein homolog 1Homo sapiens (human)Potency25.11890.006026.168889.1251AID540317
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency18.88760.168316.404067.0158AID720504
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency89.12510.050127.073689.1251AID588590
[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)
Fructose-1,6-bisphosphatase 1Sus scrofa (pig)IC50 (µMol)1,392.00001.10001.32501.6000AID419859
Indoleamine 2,3-dioxygenase 1Homo sapiens (human)IC50 (µMol)1,000.00000.05373.075710.0000AID443993
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (19)

Processvia Protein(s)Taxonomy
regulation of activated T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of T cell tolerance inductionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of chronic inflammatory responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of type 2 immune responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan catabolic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
inflammatory responseIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
female pregnancyIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan catabolic process to kynurenineIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
response to lipopolysaccharideIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of interleukin-10 productionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of interleukin-12 productionIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
multicellular organismal response to stressIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
kynurenic acid biosynthetic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
swimming behaviorIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of T cell proliferationIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
negative regulation of T cell apoptotic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
positive regulation of T cell apoptotic processIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
'de novo' NAD biosynthetic process from tryptophanIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (5)

Processvia Protein(s)Taxonomy
electron transfer activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
heme bindingIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
indoleamine 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
metal ion bindingIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
tryptophan 2,3-dioxygenase activityIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
cytosolIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
smooth muscle contractile fiberIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
stereocilium bundleIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
cytoplasmIndoleamine 2,3-dioxygenase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Current protocols in cytometry, Oct, Volume: Chapter 13Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2006Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5
Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set2010Assay and drug development technologies, Feb, Volume: 8, Issue:1
High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID727599Inhibition of cell migration in human MDA-MB-231 cells assessed as total number of cells at 10 uM after 24 hrs by transwell migration assay relative to control2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a Series of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion.
AID103194Inhibition the IL-6 secretion stimulated at a concentration of 10 ng/ml in osteoblastic MC3T3-E 1 cells.1999Bioorganic & medicinal chemistry letters, Apr-05, Volume: 9, Issue:7
4-Phenylthiazole derivatives inhibit IL-6 secretion in osteoblastic cells and suppress bone weight loss in ovariectomized mice.
AID1460923Binding affinity to full length recombinant N-terminal 6xHis-Smt3 tagged human Ube2T P73K mutant expressed in Escherichia coli BL21(DE3) by ITC2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.
AID1196567Binding affinity to Plasmodium falciparum AMA1 at 200 uM by surface plasmon resonance method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID1196568Binding affinity to SPSB2 (unknown origin) at 200 uM by surface plasmon resonance method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID1196566Binding affinity to oxidoreductase 1 (unknown origin) at 200 uM by surface plasmon resonance method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID419859Inhibition of pig FBPase expressed in Escherichia coli EK1601 by spectrophotometry2009Bioorganic & medicinal chemistry, Jun-01, Volume: 17, Issue:11
A library of novel allosteric inhibitors against fructose 1,6-bisphosphatase.
AID727598Cytotoxicity against human MDA-MB-231 cells assessed as colony formation at 10 uM after 2 weeks relative to control2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Discovery of a Series of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion.
AID1196572Binding affinity to oxidoreductase 1 (unknown origin) at 1 mM by HSQC-NMR analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID1460922Inhibition of full length N-terminal 6xHis-Smt3 tagged human Ube2T expressed in Escherichia coli BL21(DE3) assessed as FANCD2 ubiquitination after 15 mins in presence of fluorescently-labeled Ub/recombinant human E1/ATP by fluorescence assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.
AID1143398Inhibition of recombinant human PCAF catalytic domain (492 to 658 aa) using histone H3 at 100 uM after 1 hr by radiochemical assay in presence of [acetyl-3H]-acetyl coenzyme A2014European journal of medicinal chemistry, Jun-10, Volume: 80Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies.
AID1460924Binding affinity to [1H-15N]-labeled N-terminal 6xHis-Smt3 tagged human Ube2T (1 to 154 residues) expressed in Escherichia coli BL21(DE3) by chemical shift perturbation assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.
AID1196571Binding affinity to oxidoreductase 1 (unknown origin) by STD-NMR analysis2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID1460926Inhibition of full length N-terminal 6xHis-Smt3 tagged human Ube2T expressed in Escherichia coli BL21(DE3) assessed as FANCD2 ubiquitination at 2.5 mM after 15 mins in presence of fluorescently-labeled Ub/recombinant human E1/FANCL in 0.05% Tween20 contai2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.
AID1196565Binding affinity to oxidoreductase 2 (unknown origin) at 200 uM by surface plasmon resonance method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID1487209Inhibition of human IDO1 at 100 uM pre-incubated for 10 mins before L-Trp as substrate addition and measured after 30 mins by colorimetry2017Bioorganic & medicinal chemistry letters, 08-01, Volume: 27, Issue:15
Synthesis of 4- and 5-arylthiazolinethiones as inhibitors of indoleamine 2,3-dioxygenase.
AID1460927Inhibition of UbcH5c (unknown origin) assessed as RNF4 ubiquitination at 2.5 mM after 15 mins in presence of fluorescently-labeled Ub/E2 by fluorescence assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Allosteric Targeting of the Fanconi Anemia Ubiquitin-Conjugating Enzyme Ube2T by Fragment Screening.
AID1143395Inhibition of recombinant human p300 catalytic domain (1284 to 1673 aa) using histone H3 at 100 uM after 1 hr by radiochemical assay in presence of [acetyl-3H]-acetyl coenzyme A2014European journal of medicinal chemistry, Jun-10, Volume: 80Evaluation of a large library of (thiazol-2-yl)hydrazones and analogues as histone acetyltransferase inhibitors: enzyme and cellular studies.
AID443993Inhibition of human recombinant IDO expressed in Escherichia coli BL21 AI2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Rational design of indoleamine 2,3-dioxygenase inhibitors.
AID1196573Binding affinity to SPSB2 (unknown origin) at 3mM by 19F NMR method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID1196570Binding affinity to protein kinase (unknown origin) at 200 uM by surface plasmon resonance method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID694784Inhibition of amyloid beta (1 to 42) self-aggregation at 20 uM after 24 hrs by thioflavin T fluorescence assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Novel multipotent phenylthiazole-tacrine hybrids for the inhibition of cholinesterase activity, β-amyloid aggregation and Ca²⁺ overload.
AID772912Induction of glucose uptake in rat L6 cells pulsed with C14-deoxy glucose at 10 uM after 24 hrs in presence of insulin relative to control2013Bioorganic & medicinal chemistry letters, Oct-15, Volume: 23, Issue:20
Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening.
AID1196569Binding affinity to carbonic anhydrase 2 (unknown origin) at 200 uM by surface plasmon resonance method2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Promiscuous 2-aminothiazoles (PrATs): a frequent hitting scaffold.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
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.
[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-19901 (4.00)18.7374
1990's1 (4.00)18.2507
2000's2 (8.00)29.6817
2010's19 (76.00)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]