Compounds > tmc 256c1
Page last updated: 2024-10-15

tmc 256c1

Description

TMC 256C1: inhibits IL-4 signal transduction; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135418331
CHEMBL ID454794
SCHEMBL ID15060672
MeSH IDM0441005

Synonyms (8)

Synonym
bdbm50242177
5,8-dihydroxy-10-methoxy-2-propyl-4h-benzo[h]chromen-4-one
5,8-dihydroxy-10-methoxy-2-methyl-4h-benzo[h]chromen-4-one
CHEMBL454794 ,
tmc-256c1
SCHEMBL15060672
5,8-dihydroxy-10-methoxy-2-methyl-benzo[h]chromen-4-one
tmc 256c1
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)12.80000.00401.966610.0000AID489245
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (14)

Processvia Protein(s)Taxonomy
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (14)

Processvia Protein(s)Taxonomy
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID1777029Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 10 uM incubated for 48 hrs in presence of 4.5 uM cisplatin by MTT assay
AID1777041Induction of apoptosis in cisplatin-resistant human A549 cells assessed as necrotic cells at 10 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 0.53%)
AID1777036Inhibition of redox balance in cisplatin-resistant human A549 cells assessed as reduction in ratio of GSH/GSSG measured after 24 hrs
AID333817Inhibition of mammalian 5'-Cap- RNA dependent translation in human HeLa cells after 60 mins by luciferase reporter gene assay2004Journal of natural products, Dec, Volume: 67, Issue:12
A diketopiperazine dimer from a marine-derived isolate of Aspergillus niger.
AID1777044Induction of apoptosis in cisplatin-resistant human A549 cells assessed as late apoptotic cells at 20 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 10.8%)
AID1777035Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 20 uM incubated for 48 hrs in presence of 4.5 uM cisplatin by MTT assay
AID1777043Induction of apoptosis in cisplatin-resistant human A549 cells assessed as early apoptotic cells at 20 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 2.17%)
AID489245Inhibition of ABCG2-mediated drug efflux expressed in human NCI-H460 cells2010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids.
AID1777039Induction of apoptosis in cisplatin-resistant human A549 cells assessed as early apoptotic cells at 10 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 2.17%)
AID1777031Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 15 uM incubated for 48 hrs in presence of 3 uM cisplatin by MTT assay
AID1777038Induction of apoptosis in cisplatin-resistant human A549 cells assessed as viable cells at 10 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 86.5%)
AID1777027Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 10 uM incubated for 48 hrs in presence of 1.5 uM cisplatin by MTT assay
AID333818Inhibition of viral IRES-mediated translation in human HeLa cells after 60 mins by luciferase reporter gene assay2004Journal of natural products, Dec, Volume: 67, Issue:12
A diketopiperazine dimer from a marine-derived isolate of Aspergillus niger.
AID1777050Downregulation of HO-1 protein expression in cisplatin-resistant human A549 cells at 15 uM incubated for 48 hrs by western blot analysis
AID1777033Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 20 uM incubated for 48 hrs in presence of 1.5 uM cisplatin by MTT assay
AID1777040Induction of apoptosis in cisplatin-resistant human A549 cells assessed as late apoptotic cells at 10 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 10.8%)
AID1777030Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 15 uM incubated for 48 hrs in presence of 1.5 uM cisplatin by MTT assay
AID1777034Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 20 uM incubated for 48 hrs in presence of 3 uM cisplatin by MTT assay
AID1777026Anticancer activity against cisplatin-resistant human A549 cells assessed as reduction in cell viability measured after 48 hrs in presence of cisplatin by MTT assay
AID1777032Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 15 uM incubated for 48 hrs in presence of 4.5 uM cisplatin by MTT assay
AID1777028Synergistic antiproliferative activity against cisplatin-resistant human A549 cells assessed as combination index at 10 uM incubated for 48 hrs in presence of 3 uM cisplatin by MTT assay
AID1777042Induction of apoptosis in cisplatin-resistant human A549 cells assessed as viable cells at 20 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 86.5%)
AID1777045Induction of apoptosis in cisplatin-resistant human A549 cells assessed as necrotic cells at 20 uM incubated for 24 hrs by AnnexinV-FITC/PI staining based flow cytometry (Rvb = 0.53%)
AID1777046Downregulation of HO-1 protein expression in cisplatin-resistant human A549 cells at 15 uM incubated for 48 hrs in presence of cisplatin by western blot analysis
AID1777048Downregulation of AKT protein expression in cisplatin-resistant human A549 cells at 15 uM incubated for 48 hrs in presence of cisplatin by western blot analysis
AID1777047Downregulation of NQO-1 protein expression in cisplatin-resistant human A549 cells at 15 uM incubated for 48 hrs in presence of cisplatin by western blot analysis
AID1777037Induction of intracellular ROS generation in cisplatin-resistant human A549 cells measured after 24 hrs by DCFH-DA staining based laser scanning confocal microscopy
AID489244Inhibition of ABCG2 expressed in human NCI-H460 cells assessed as inhibition of PhA accumulation relative to fumitremorgin C2010Bioorganic & medicinal chemistry letters, Jul-01, Volume: 20, Issue:13
Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids.
AID1777049Downregulation of Nrf2 protein expression in cisplatin-resistant human A549 cells at 15 uM incubated for 48 hrs in presence of cisplatin by western blot analysis
[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's2 (40.00)29.6817
2010's2 (40.00)24.3611
2020's1 (20.00)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%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
warfarin
Warfarin: An anticoagulant that acts by inhibiting the synthesis of vitamin K-dependent coagulation factors. Warfarin is indicated for the prophylaxis and/or treatment of venous thrombosis and its extension, pulmonary embolism, and atrial fibrillation with embolization. It is also used as an adjunct in the prophylaxis of systemic embolism after myocardial infarction. Warfarin is also used as a rodenticide.. warfarin : A racemate comprising equal amounts of (R)- and (S)-warfarin. Extensively used as both an anticoagulant drug and as a pesticide against rats and mice.. 4-hydroxy-3-(3-oxo-1-phenylbutyl)-1-benzopyran-2-one : A member of the class of coumarins that is 4-hydroxycoumarin which is substituted at position 3 by a 1-phenyl-3-oxo-1-butyl group.		2.0210benzenes;
hydroxycoumarin;
methyl ketone
ConditionIndicatedRelationship StrengthStudiesTrials