Page last updated: 2024-12-09

ax 20017

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Description

AX 20017: a protein kinase PknG inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID673481
CHEMBL ID379367
SCHEMBL ID3922474
MeSH IDM0469139

Synonyms (43)

Synonym
OPREA1_658271
TIMTEC1_000400
OPREA1_698996
2PZI
2-[(cyclopropylcarbonyl)amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
STK124515
HMS1535C04
bdbm50185119
2-(cyclopropanecarboxamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide
AKOS000494721
DB07398
CHEMBL379367 ,
AB00684161-01
2-(cyclopropanecarbonylamino)-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
axx ,
2-cyclopropaneamido-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide
F0317-0046
329221-38-7
pkng inhibitor
SCHEMBL3922474
2-(cyclopropanecarbonyl-amino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid amide
VATFNEMGBRWLHI-UHFFFAOYSA-N
ax20017 ,
HMS3604K13
sr-01000358283
SR-01000358283-1
CS-6196
HY-14987
J-018941
Z27358469
BS-16585
Q27096619
2-(cyclopropanecarbonylamino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amide
HMS3674K07
BCP31476
ax-20017; ax 20017; pkng inhibitor
N16910
ax 20017
EX-A3186
AC-35666
pkng
mycobacterial protein kinase g inhibitor
EN300-15936605
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Probable serine/threonine-protein kinase pknGMycobacterium tuberculosisIC50 (µMol)0.80000.80000.80000.8000AID977608
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)IC50 (µMol)1.30000.00010.32759.5480AID265353
Serine/threonine-protein kinase PknGMycobacterium tuberculosis H37RvIC50 (µMol)0.90000.90000.90000.9000AID1892535
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (25)

Processvia Protein(s)Taxonomy
hemopoiesisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
leukocyte homeostasisReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
myeloid progenitor cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
pro-B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of cell population proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
response to organonitrogen compoundReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
peptidyl-tyrosine phosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine-mediated signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
B cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
animal organ regenerationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
common myeloid progenitor cell proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor signaling pathwayReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of tyrosine phosphorylation of STAT proteinReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
regulation of apoptotic processReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAP kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of MAPK cascadeReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
lymphocyte proliferationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein autophosphorylationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to cytokine stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cellular response to glucocorticoid stimulusReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
dendritic cell differentiationReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
positive regulation of kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
multicellular organism developmentReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
transmembrane receptor protein tyrosine kinase activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
cytokine receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
vascular endothelial growth factor receptor activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
ATP bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
nuclear glucocorticoid receptor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
protein-containing complex bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
phosphatidylinositol 3-kinase activator activityReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
growth factor bindingReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
endoplasmic reticulumReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endoplasmic reticulum lumenReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
endosome membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
receptor complexReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
plasma membraneReceptor-type tyrosine-protein kinase FLT3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (42)

Assay IDTitleYearJournalArticle
AID1892533Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in human THP-1 cells assessed as reduction in intracellular survival at 1 to 10 uM measured after 24 to 48 hrs2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Cosolvent Sites-Based Discovery of
AID327883Effect on Phorbol 12-myristate 13-acetate-induced cellular morphology in mouse J774 macrophage cells at 20 uM by video microscopy2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327893Inhibition of human PDK12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327907Inhibition of human TGFbeta R12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327896Inhibition of human PKC zeta2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327906Inhibition of human AMPKalpha12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327909Inhibition of human EphA12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327904Inhibition of human MAPKAPK52007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327887Inhibition of Mycobacterium tuberculosis PKnG-I87S/A92S mutant at 25 uM by autoradiography2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327902Inhibition of human PAK42007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327890Inhibition of human JNK12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327900Inhibition of human MAP2K62007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327899Inhibition of human MAP2K12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327888Inhibition of human CDK22007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327894Inhibition of human PKCalpha2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID1892535Inhibition of full length Mycobacterium tuberculosis protein kinase G using His-tagged GarA as substrate in presence of [gamma32P] ATP measured after 12 to 24 hrs by radiometric kinase assay2022Journal of medicinal chemistry, 07-28, Volume: 65, Issue:14
Cosolvent Sites-Based Discovery of
AID327897Inhibition of human ROCK22007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327879Inhibition of Mycobacterium tuberculosis Protein kinase G by radiometric ATP consumptive assay2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327889Inhibition of human GSK3 beta2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID265353Inhibition of FLT32006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
AID327898Inhibition of human AKT12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327895Inhibition of human PKC mu2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327881Effect on protein translation in mouse J774 macrophage cells after 9 hrs2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327911Inhibition of human FGFR12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327903Inhibition of human MST42007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327886Inhibition of Mycobacterium tuberculosis PKnGdeltaN mutant at 63 uM by autoradiography2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327908Inhibition of human EGFR2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327910Inhibition of human FAK2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID265355Antiproliferative activity against human MV4-11 cells2006Bioorganic & medicinal chemistry letters, Jun-15, Volume: 16, Issue:12
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
AID327892Inhibition of human CDK52007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327905Inhibition of human CHK12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327885Effect on Phorbol 12-myristate 13-acetate-induced macropinocytosis in mouse J774 macrophage cells at 20 uM by video microscopy2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327912Inhibition of human FLT32007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327901Inhibition of human PAK12007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327882Effect on phagocytosis of latex beads in mouse J774 macrophage cells after 30 mins2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327891Inhibition of human p38alpha2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327884Effect on Phorbol 12-myristate 13-acetate-induced membrane ruffling in mouse J774 macrophage cells at 20 uM by video microscopy2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID327880Effect on proliferation in mouse J774 macrophage cells assessed as incorporation of [3H]thymidine after 48 hrs2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of 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.
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.
AID977608Experimentally measured binding affinity data (IC50) for protein-ligand complexes derived from PDB2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
AID1811Experimentally measured binding affinity data derived from PDB2007Proceedings of the National Academy of Sciences of the United States of America, Jul-17, Volume: 104, Issue:29
Structural basis for the specific inhibition of protein kinase G, a virulence factor of Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (50.00)29.6817
2010's3 (37.50)24.3611
2020's1 (12.50)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%
Other8 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]