Page last updated: 2024-11-13

ccg-203971

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 CID71681561
CHEMBL ID2398678
SCHEMBL ID17728988
MeSH IDM000595298

Synonyms (30)

Synonym
chembl2398678 ,
bdbm50436236
S8469
gtpl6763
ccg203971
n-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide
ccg-203971 ,
compound 8a [pmid: 23707258]
ccg 203971
1443437-74-8
AKOS025142073
n-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide
n-(4-chlorophenyl)-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide
HERLZBNILRVHQN-UHFFFAOYSA-N
SCHEMBL17728988
ccg-203971, >=98% (hplc)
NCGC00387259-04
CS-0028459
HY-108361
BCP20795
Q27075767
AS-16522
A12055
EX-A1813
3-piperidinecarboxamide, n-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-
SB60873
nsc757973
nsc-757973
A899246
AC-35601

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 (8)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.68370.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency15.09160.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency13.45040.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency15.09160.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency15.09160.01238.964839.8107AID1645842
[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)
Transforming protein RhoAHomo sapiens (human)IC50 (µMol)5.85005.30005.85006.4000AID755569; AID755578
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (116)

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)
endothelial cell migrationTransforming protein RhoAHomo sapiens (human)
positive regulation of neuron differentiationTransforming protein RhoAHomo sapiens (human)
positive regulation of stress fiber assemblyTransforming protein RhoAHomo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisTransforming protein RhoAHomo sapiens (human)
endothelial tube lumen extensionTransforming protein RhoAHomo sapiens (human)
cell morphogenesisTransforming protein RhoAHomo sapiens (human)
neuron migrationTransforming protein RhoAHomo sapiens (human)
kidney developmentTransforming protein RhoAHomo sapiens (human)
angiotensin-mediated vasoconstriction involved in regulation of systemic arterial blood pressureTransforming protein RhoAHomo sapiens (human)
alpha-beta T cell lineage commitmentTransforming protein RhoAHomo sapiens (human)
regulation of systemic arterial blood pressure by endothelinTransforming protein RhoAHomo sapiens (human)
aortic valve formationTransforming protein RhoAHomo sapiens (human)
regulation of transcription by RNA polymerase IITransforming protein RhoAHomo sapiens (human)
cell-matrix adhesionTransforming protein RhoAHomo sapiens (human)
Rho protein signal transductionTransforming protein RhoAHomo sapiens (human)
skeletal muscle tissue developmentTransforming protein RhoAHomo sapiens (human)
negative regulation of cell-substrate adhesionTransforming protein RhoAHomo sapiens (human)
regulation of neuron projection developmentTransforming protein RhoAHomo sapiens (human)
cell migrationTransforming protein RhoAHomo sapiens (human)
substantia nigra developmentTransforming protein RhoAHomo sapiens (human)
cerebral cortex cell migrationTransforming protein RhoAHomo sapiens (human)
forebrain radial glial cell differentiationTransforming protein RhoAHomo sapiens (human)
actin cytoskeleton organizationTransforming protein RhoAHomo sapiens (human)
regulation of cell migrationTransforming protein RhoAHomo sapiens (human)
androgen receptor signaling pathwayTransforming protein RhoAHomo sapiens (human)
cytoplasmic microtubule organizationTransforming protein RhoAHomo sapiens (human)
positive regulation of cytokinesisTransforming protein RhoAHomo sapiens (human)
regulation of actin cytoskeleton organizationTransforming protein RhoAHomo sapiens (human)
negative regulation of intracellular steroid hormone receptor signaling pathwayTransforming protein RhoAHomo sapiens (human)
regulation of osteoblast proliferationTransforming protein RhoAHomo sapiens (human)
cell junction assemblyTransforming protein RhoAHomo sapiens (human)
substrate adhesion-dependent cell spreadingTransforming protein RhoAHomo sapiens (human)
Roundabout signaling pathwayTransforming protein RhoAHomo sapiens (human)
cleavage furrow formationTransforming protein RhoAHomo sapiens (human)
apolipoprotein A-I-mediated signaling pathwayTransforming protein RhoAHomo sapiens (human)
odontogenesisTransforming protein RhoAHomo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionTransforming protein RhoAHomo sapiens (human)
stress fiber assemblyTransforming protein RhoAHomo sapiens (human)
apical junction assemblyTransforming protein RhoAHomo sapiens (human)
beta selectionTransforming protein RhoAHomo sapiens (human)
ossification involved in bone maturationTransforming protein RhoAHomo sapiens (human)
wound healing, spreading of cellsTransforming protein RhoAHomo sapiens (human)
establishment of epithelial cell apical/basal polarityTransforming protein RhoAHomo sapiens (human)
negative regulation of cell sizeTransforming protein RhoAHomo sapiens (human)
positive regulation of alpha-beta T cell differentiationTransforming protein RhoAHomo sapiens (human)
negative chemotaxisTransforming protein RhoAHomo sapiens (human)
positive regulation of stress fiber assemblyTransforming protein RhoAHomo sapiens (human)
regulation of focal adhesion assemblyTransforming protein RhoAHomo sapiens (human)
Wnt signaling pathway, planar cell polarity pathwayTransforming protein RhoAHomo sapiens (human)
positive regulation of lipase activityTransforming protein RhoAHomo sapiens (human)
bone trabecula morphogenesisTransforming protein RhoAHomo sapiens (human)
regulation of microtubule cytoskeleton organizationTransforming protein RhoAHomo sapiens (human)
cellular response to lipopolysaccharideTransforming protein RhoAHomo sapiens (human)
cellular response to cytokine stimulusTransforming protein RhoAHomo sapiens (human)
semaphorin-plexin signaling pathwayTransforming protein RhoAHomo sapiens (human)
positive regulation of podosome assemblyTransforming protein RhoAHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityTransforming protein RhoAHomo sapiens (human)
mitotic spindle assemblyTransforming protein RhoAHomo sapiens (human)
negative regulation of oxidative phosphorylationTransforming protein RhoAHomo sapiens (human)
motor neuron apoptotic processTransforming protein RhoAHomo sapiens (human)
regulation of modification of postsynaptic structureTransforming protein RhoAHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionTransforming protein RhoAHomo sapiens (human)
skeletal muscle satellite cell migrationTransforming protein RhoAHomo sapiens (human)
negative regulation of reactive oxygen species biosynthetic processTransforming protein RhoAHomo sapiens (human)
mitotic cleavage furrow formationTransforming protein RhoAHomo sapiens (human)
positive regulation of vascular associated smooth muscle contractionTransforming protein RhoAHomo sapiens (human)
positive regulation of leukocyte adhesion to vascular endothelial cellTransforming protein RhoAHomo sapiens (human)
regulation of modification of postsynaptic actin cytoskeletonTransforming protein RhoAHomo sapiens (human)
cellular response to chemokineTransforming protein RhoAHomo sapiens (human)
regulation of neural precursor cell proliferationTransforming protein RhoAHomo sapiens (human)
positive regulation of T cell migrationTransforming protein RhoAHomo sapiens (human)
negative regulation of motor neuron apoptotic processTransforming protein RhoAHomo 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 (23)

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)
GTPase activityTransforming protein RhoAHomo sapiens (human)
G protein activityTransforming protein RhoAHomo sapiens (human)
protein bindingTransforming protein RhoAHomo sapiens (human)
GTP bindingTransforming protein RhoAHomo sapiens (human)
myosin bindingTransforming protein RhoAHomo sapiens (human)
protein kinase bindingTransforming protein RhoAHomo 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 (40)

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)
cleavage furrowTransforming protein RhoAHomo sapiens (human)
postsynapseTransforming protein RhoAHomo sapiens (human)
glutamatergic synapseTransforming protein RhoAHomo sapiens (human)
nucleusTransforming protein RhoAHomo sapiens (human)
endosomeTransforming protein RhoAHomo sapiens (human)
endoplasmic reticulum membraneTransforming protein RhoAHomo sapiens (human)
cytosolTransforming protein RhoAHomo sapiens (human)
cytoskeletonTransforming protein RhoAHomo sapiens (human)
plasma membraneTransforming protein RhoAHomo sapiens (human)
focal adhesionTransforming protein RhoAHomo sapiens (human)
cell cortexTransforming protein RhoAHomo sapiens (human)
cytoplasmic side of plasma membraneTransforming protein RhoAHomo sapiens (human)
lamellipodiumTransforming protein RhoAHomo sapiens (human)
cell junctionTransforming protein RhoAHomo sapiens (human)
midbodyTransforming protein RhoAHomo sapiens (human)
secretory granule membraneTransforming protein RhoAHomo sapiens (human)
vesicleTransforming protein RhoAHomo sapiens (human)
ruffle membraneTransforming protein RhoAHomo sapiens (human)
dendritic spineTransforming protein RhoAHomo sapiens (human)
apical junction complexTransforming protein RhoAHomo sapiens (human)
extracellular exosomeTransforming protein RhoAHomo sapiens (human)
cell peripheryTransforming protein RhoAHomo sapiens (human)
ficolin-1-rich granule membraneTransforming protein RhoAHomo sapiens (human)
cytosolTransforming protein RhoAHomo sapiens (human)
dendritic spineTransforming protein RhoAHomo sapiens (human)
plasma membraneTransforming protein RhoAHomo sapiens (human)
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 (22)

Assay IDTitleYearJournalArticle
AID755574Effective permeability of the compound by PAMPA2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755576Cytotoxicity against human PC3 cells at 100 uM by WST1 assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755568Cytotoxicity against human SK-MEL-147 cells by WST1 assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID1443379Drug metabolism in CD-1 mouse liver microsomes assessed as oxidative metabolism at 20 uM after 3 mins in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.
AID755571Toxicity in mouse assessed as increase in liver weight at 10 to 100 mg/kg/day, ip administered for 5 days measured on day 82013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755569Inhibition of RhoC-mediated pathway in human SK-Mel-147 cells assessed as inhibition of SRE-regulated gene transcription by luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID1443376Inhibition of Rho/MRTF/SRF pathway (unknown origin) expressed in HEK293T cells assessed as reduction in Galpha12-stimulated MRTF-selective SRE.L promoter-driven luciferase activity after overnight incubation by luminescence assay2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.
AID755577Inhibition of RhoC-mediated pathway in human PC3 cells assessed as inhibition of SRE-regulated gene transcription at 100 uM by luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755570Toxicity in mouse assessed as organism survival at 10 to 100 mg/kg/day, ip after 5 days2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID1443381AUC (0 to 7 hrs) in CD-1 mouse at 10 mg/kg, ip administered as single dose by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.
AID1443378Thermodynamic aqueous solubility of the compound in water by nitrogen detection method2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.
AID755573Kinetic solubility of the compound2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755575Antimetastatic activity against human PC3 cells at 10 uM after 24 hrs by scratch wound assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755578Inhibition of RhoC-mediated pathway in human PC3 cells assessed as inhibition of SRE-regulated gene transcription by luciferase reporter gene assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID755572Antimetastatic activity against human PC3 cells after 24 hrs by scratch wound assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
Optimization of novel nipecotic bis(amide) inhibitors of the Rho/MKL1/SRF transcriptional pathway as potential anti-metastasis agents.
AID1443377Half life in CD-1 mouse liver microsomes at 1 uM in presence of NADPH by LC-MS/MS analysis2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.
AID1443380Inhibition of Rho/MRTF/SRF pathway in human primary dermal fibroblasts assessed as inhibition of TGF-beta-stimulated ACTA2 gene expression by measuring ACTA2 mRNA level at 10 uM after 24 hrs by qRT-PCR method relative to control2017Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8
Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.
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.
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.
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.
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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's3 (60.00)24.3611
2020's2 (40.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 20.35

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 Index20.35 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.51 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (20.35)

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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]