Page last updated: 2024-11-10

sag compound

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

Description

SAG1.3: small molecule smoothened agonist and a partial agonist of FZD6 [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

3-chloro-N-[trans-4-(methylamino)cyclohexyl]-N-[3-(pyridin-4-yl)benzyl]-1-benzothiophene-2-carboxamide : A member of the class of 1-benzothiophenes that is 3-chloro-1-benzothiophene-2-carboxamide in which the amide nitrogen is substituted by trans-4-(methylamino)cyclohexyl and 3-(pyridin-4-yl)benzyl groups. A smoothened (Smo) receptor agonist that antagonizes cyclopamine action at the Smo receptor. Activates the Hedgehog signaling pathway in a Patched independent manner. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID5284330
CHEMBL ID1221983
CHEMBL ID2160033
CHEBI ID138438
SCHEMBL ID10029769
SCHEMBL ID8437026
SCHEMBL ID14707297
MeSH IDM0443200

Synonyms (60)

Synonym
CHEMBL1221983 ,
n-(3-(pyridin-4yl)benzyl)-3-chloro-n-(4-(trans-methylamino)cyclohexyl)benzo[b] thiophene-2-carboxamide
SAG ,
CHEBI:138438
3-chloro-n-[trans-4-(methylamino)cyclohexyl]-n-[[3-(4-pyridinyl)phenyl]methyl]benzo[b]thiophene-2-carboxamide
smoothened agonist
912545-86-9
3-chloro-n-[trans-4-(methylamino)cyclohexyl]-n-[3-(pyridin-4-yl)benzyl]-1-benzothiophene-2-carboxamide
3-chloro-n-[4-(methylamino)cyclohexyl]-n-[(3-pyridin-4-ylphenyl)methyl]-1-benzothiophene-2-carboxamide
chembl2160033 ,
bdbm50393851
bdbm50393847
FT-0674498
NCGC00347954-01
smoothened agonist (sag)
364590-63-6
SCHEMBL10029769
c28h28cln3os
3-chloro-n-((1r,4r)-4-(methylamino)cyclohexyl)-n-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
SCHEMBL8437026
SCHEMBL14707297
AKOS025142011
DTXSID80415294
912545-86-9(free base)
sag dihydrochloride
HB3107
AC-33071
HY-12848
mfcd22581513
AKOS026750207
EX-A569
3-chloro-n-[trans-4-(methylamino)cyclohexyl]-n-{[3-(pyridin-4-yl)phenyl]methyl}-1-benzothiophene-2-carboxamide
V0S ,
sag dihydrochloride, >=98% (hplc)
smoothened agonist (sag) free base
NCGC00384168-03
sag (smo agonist) free base
912545-86-9 (free base)
3-chloro-n-(trans-4-(methylamino)cyclohexyl)-n-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
3-chloro-n-[trans-4-(methylamino)cyclohexyl]-n-[[3-(4-pyridinyl)phenyl]methyl]benzo[b]thiophene-2-carboxamide dihydrochloride
sag (smo-agonist)
AS-35219
sag free base
BCP14694
Q15410188
benzo(b)thiophene-2-carboxamide, 3-chloro-n-(trans-4-(methylamino)cyclohexyl)-n-((3-(4-pyridinyl)phenyl)methyl)-
sag (cyclopamine antagonist)
4XN97SZK4J ,
3-chloro-n-(trans-4-(methylamino)cyclohexyl)-n-((3-(4-pyridinyl)phenyl)methyl)benzo(b)thiophene-2-carboxamide
sag (smo agonist)
gtpl10327
sag1.3
compound 22 [pmid: 12391318]
3-chloro-n-[4-(methylamino)cyclohexyl]-n-{[3-(pyridin-4-yl)phenyl]methyl}-1-benzothiophene-2-carboxamide
smo agonist (sag)
3-chloro-n-(4-(methylamino)cyclohexyl)-n-(3-(pyridin-4-yl)benzyl)benzo[b]thiophene-2-carboxamide
unii-4xn97szk4j
(rac)-sag
HY-12848A
CS-0062652

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"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 (13)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fumarate hydrataseHomo sapiens (human)Potency9.34950.00308.794948.0869AID1347053
PPM1D proteinHomo sapiens (human)Potency20.82120.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency0.03380.01237.983543.2770AID1645841
EWS/FLI fusion proteinHomo sapiens (human)Potency25.08310.001310.157742.8575AID1259252; AID1259253; AID1259255; AID1259256
GVesicular stomatitis virusPotency10.68400.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency4.25340.00108.379861.1304AID1645840
polyproteinZika virusPotency9.34950.00308.794948.0869AID1347053
Interferon betaHomo sapiens (human)Potency18.28690.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.68400.01238.964839.8107AID1645842
[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)
Smoothened homologMus musculus (house mouse)EC50 (µMol)0.05900.00200.16390.8000AID1321053; AID1321085; AID1771774
Sonic hedgehog proteinMus musculus (house mouse)EC50 (µMol)0.03530.00881.59514.0000AID694763
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (45)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (18)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (25)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endocytic vesicle membraneSmoothened homologMus musculus (house mouse)
ciliary membraneSmoothened homologMus musculus (house mouse)
extracellular regionSonic hedgehog proteinMus musculus (house mouse)
nucleoplasmSonic hedgehog proteinMus musculus (house mouse)
endoplasmic reticulum lumenSonic hedgehog proteinMus musculus (house mouse)
plasma membraneSonic hedgehog proteinMus musculus (house mouse)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (61)

Assay IDTitleYearJournalArticle
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.
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.
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.
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.
AID694766Cytotoxicity against HUVEC after 24 hrs by WST-1 assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1321072Agonist activity at Smo in mouse C3H10T1/2 cells assessed as effect on Gli2 expression at 1 uM after 48 hrs by RT-PCR method relative to vehicle-treated control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321053Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast incubated for 6 days by alkaline phosphatase assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321082Induction of Renilla reniformis luciferase activity at 10 uM relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321079Agonist activity at Smo in mouse C3H10T1/2 cells assessed as effect on Smo expression at 1 uM after 48 hrs by RT-PCR method relative to vehicle-treated control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID694765Cytotoxicity against HUVEC up to 10 uM after 24 hrs by WST-1 assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1321063Agonist activity at Smo in cerebellar granule cell precursors isolated from rat at postnatal day 8 assessed as stimulation of proliferation by [3H]-thymidine incorporation assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321057Induction of mouse C3H10T1/2 cell differentiation into osteoblast at 0.3 uM in presence of smo ShRNA incubated for 6 days by alkaline phosphatase assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID694773Induction of angiogenesis in HUVEC assessed as formation of cell sprouts after 48 hrs by BrdU incorporation assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1321085Agonist activity at Smo in mouse NIH/3T3 cells transfected with Gli-dependent firefly luciferase reporter assessed as stimulation of Gli transcription factor2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1771774Agonist activity at SMO in mouse NIH3T3 cells incubated for 2 hrs by Bright-Glo luciferase assay2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement.
AID502885Activation of Shh in ptch1 gene-deficient MEF assessed as beta-galactosidase activity after 30 hrs by chemiluminescence assay in presence of 100 nM 3-keto-N-aminoethyl-N'-aminocaproyldihydrocinnamoyl cyclopamine2006Nature chemical biology, Jan, Volume: 2, Issue:1
Purmorphamine activates the Hedgehog pathway by targeting Smoothened.
AID694769Activation of Shh pathway in human foreskin fibroblasts assessed as increase in VEGF expression at 0.1 to 1 uM after 48 hrs by ELISA relative to control2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1321069Induction of Smo translocation to primary cilium in mouse NIH/3T3 cells at 1 uM after overnight incubation by DAPI staining-based immunofluorescence assay relative to control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321071Agonist activity at Smo in mouse C3H10T1/2 cells assessed as effect on Gli1 expression at 1 uM after 48 hrs by RT-PCR method relative to vehicle-treated control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321054Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast at 10 uM incubated for 6 days by alkaline phosphatase assay relative to GSA-102016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1771772Agonist activity at SMO in mouse NIH3T3 cells assessed as induction of SMO accumulation in primary cilia incubated for 12 hrs by fluorescence method2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement.
AID694772Induction of HUVEC proliferation after 48 hrs by BrdU-incorporation assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1771773Agonist activity at SMO in mouse NIH3T3 cells assessed as fluorescent intensity of ciliary SMO incubated for 12 hrs by fluorescence method2021Journal of medicinal chemistry, 09-23, Volume: 64, Issue:18
Elucidation of Distinct Modular Assemblies of Smoothened Receptor by Bitopic Ligand Measurement.
AID694768Activation of Shh pathway in human foreskin fibroblasts assessed as increase in VEGF expression after 48 hrs by ELISA2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1321066Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast at 0.3 uM in presence of adenylate cyclase activator forskolin incubated for 6 days by alkaline phosphatase assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321062Agonist activity at Smo in mouse NIH/3T3 cells transfected with Gli-dependent firefly luciferase reporter assessed as stimulation of Gli transcription factor incubated for 40 hrs2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321067Agonist activity at Smo in mouse C3H10T1/2 cells assessed as induction of cell differentiation into osteoblast at 0.3 uM in presence of phosphodiesterase inhibitor IBMX incubated for 6 days by alkaline phosphatase assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID1321074Agonist activity at Smo in mouse C3H10T1/2 cells assessed as effect on Ptc1 expression at 1 uM after 48 hrs by RT-PCR method relative to vehicle-treated control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID509545Agonist activity at hedgehog receptor2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Modulators of the hedgehog signaling pathway.
AID694770Activation of Shh pathway in human foreskin fibroblasts assessed as induction of maximum VEGF expression at 0.5 uM after 48 hrs by ELISA relative to control2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1321073Agonist activity at Smo in mouse C3H10T1/2 cells assessed as effect on Gli3 expression at 1 uM after 48 hrs by RT-PCR method relative to vehicle-treated control2016European journal of medicinal chemistry, Oct-04, Volume: 121Design, synthesis and biological characterization of a new class of osteogenic (1H)-quinolone derivatives.
AID694763Activation of Shh pathway in mouse Shh-Light II cells assessed as induction of gli1 expression after 48 hrs by renilla luminescence assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID694771Activation of Shh pathway in human foreskin fibroblasts assessed as induction of maximum VEGF expression at 1 uM after 48 hrs by ELISA relative to control2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
Potent small molecule Hedgehog agonists induce VEGF expression in vitro.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (14)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (7.14)29.6817
2010's5 (35.71)24.3611
2020's8 (57.14)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.48

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 Index12.48 (24.57)
Research Supply Index2.71 (2.92)
Research Growth Index5.18 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.48)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (7.14%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other13 (92.86%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]