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Found 906 Enz. Inhib. hit(s) with Target = 'Cytochrome P450 2C8'
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM155254(US10098888, Compound 2 | US9006242, 2)
Affinity DataIC50: >1.00E+5nMpH: 7.4Assay Description:The potential inhibition of enzyme activities of human cytochromes P450 (CYP) of Compound 1, 2, or 105 was evaluated using pooled human liver microso...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM106203(US9695174, I-1)
Affinity DataIC50: >3.00E+4nMpH: 7.4 T: 2°CAssay Description:Human liver microsomes (HLMs) (0.3 mg/mL in 0.1-M potassium phosphate buffer, pH 7.4) are incubated with CYP (cytochromes P450) isozyme-selective sub...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50305083(3-((3S,6S)-6-Isobutyl-9-methoxy-1,4-dioxo-1,2,3,4,...)
Affinity DataIC50: >3.00E+4nMpH: 7.4 T: 2°CAssay Description:Human liver microsomes (HLMs) (0.3 mg/mL in 0.1-M potassium phosphate buffer, pH 7.4) are incubated with CYP (cytochromes P450) isozyme-selective sub...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM155255(US10098888, Compound 105 | US11642348, Compound 10...)
Affinity DataIC50:  4.74E+4nMpH: 7.4Assay Description:The potential inhibition of enzyme activities of human cytochromes P450 (CYP) of Compound 1, 2, or 105 was evaluated using pooled human liver microso...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM155253(US10098888, Compound 1 | US9006242, 1)
Affinity DataIC50: >1.00E+5nMpH: 7.4Assay Description:The potential inhibition of enzyme activities of human cytochromes P450 (CYP) of Compound 1, 2, or 105 was evaluated using pooled human liver microso...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211754(US9290459, 9A | US9670166, 9A)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211750(US9290459, 7.2A | US9670166, 7.2A)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211836(US9290459, 41A | US9670166, 41A)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211757(US9290459, 10A | US9290459, 47.21 | US9670166, 10A)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50120439(CHEMBL3617975 | US9290459, 47.1 | US9670166, 47.1)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211887(US9290459, 47.2 | US9670166, 47.2)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM191369(WO2005082863, Example 8A | example 8A disclosed in...)
Affinity DataIC50:  1.09E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50120423(CHEMBL3617971 | US9290459, 1A | US9670166, 1A)
Affinity DataIC50: >5.00E+4nMpH: 7.5 T: 2°CAssay Description:Materials: Human neutrophil elastase was purchased from Calbiochem (Cat. No.: 324681) and the elastase substrate MeOSuc-Ala-Ala-Pro-Val-AMC from Bach...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50240713(CHEMBL4066318)
Affinity DataKi:  22nMAssay Description:Inhibition constants against ATP substrate site of M-2 (kidney form) variant of rat Methionine adenosyltransferaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50240713(CHEMBL4066318)
Affinity DataKi:  52nMAssay Description:Inhibition constants against Met (L-methionine)P substrate site of M-T (Novikoff Ascitic Hepatoma form) variant of rat Methionine adenosyltransferaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50363928(CHEMBL1951575)
Affinity DataKi:  1.10E+3nMAssay Description:Competitive inhibition of CYP2C8 in human liver microsomes assessed as paclitaxel 6-hydroxylation after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50105417(CHEMBL1089 | Nardil | PHENELZINE | Phenethyl-hydra...)
Affinity DataKi:  1.20E+3nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM18957((2-{4-[(2-butyl-1-benzofuran-3-yl)carbonyl]-2,6-di...)
Affinity DataKi:  1.50E+3nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50363928(CHEMBL1951575)
Affinity DataKi:  1.80E+3nMAssay Description:Biphasic inhibition of CYP2C8 in human liver microsomes assessed as montelukast 36-hydroxylation after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50088490(CHEMBL3526979)
Affinity DataKi:  2.70E+3nMAssay Description:Linear mixed inhibition of CYP2C8 in human liver microsomes assessed as paclitaxel 6-hydroxylation after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50363928(CHEMBL1951575)
Affinity DataKi:  6.00E+3nMAssay Description:Competitive inhibition of CYP2C8 in human liver microsomes assessed as rosiglitazone demethylation after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50088490(CHEMBL3526979)
Affinity DataKi:  6.90E+3nMAssay Description:Linear mixed inhibition of CYP2C8 in human liver microsomes assessed as rosiglitazone demethylation after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50088490(CHEMBL3526979)
Affinity DataKi:  7.30E+3nMAssay Description:Biphasic inhibition of CYP2C8 in human liver microsomes assessed as montelukast 36-hydroxylation after 20 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50088513(CHEMBL3526940)
Affinity DataKi:  9.90E+3nMAssay Description:Inhibition of CYP2C8 in human liver microsomes preincubated for 30 mins followed by substrate addition measured after 2 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM58922(MLS001304727 | MONTELUKAST Na | SMR000469188 | cid...)
Affinity DataKi:  1.10E+4nMAssay Description:Inhibition of recombinant human CYP2C8 expressed in microsomes isolated from baculovirus infected insect cell after 3 minsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM81939(CAS_52-53-9 | NSC_62969 | VERAPAMIL)
Affinity DataKi:  1.75E+4nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50397663(CHEMBL2181817)
Affinity DataKi:  2.00E+4nMAssay Description:Inhibition constants with Met (L-methionine) substrate site of M-2 (kidney form) variant of rat Methionine adenosyltransferaseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50397663(CHEMBL2181817)
Affinity DataKi:  2.00E+4nMAssay Description:Time dependent inhibition of CYP2C8 in human liver microsomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50088489(CHEMBL3527324)
Affinity DataKi:  3.17E+4nMAssay Description:Inhibition of recombinant CYP2C8 (unknown origin) treated with AMG 853More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM112777(NORTRIPTYLINE | US8629135, SW-02)
Affinity DataKi:  4.99E+4nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM18957((2-{4-[(2-butyl-1-benzofuran-3-yl)carbonyl]-2,6-di...)
Affinity DataKi:  5.12E+4nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using human liver microsomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50397663(CHEMBL2181817)
Affinity DataKi:  5.20E+4nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate preincubated for 2 to 40 mins followed by NADPH-generating system additi...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50105417(CHEMBL1089 | Nardil | PHENELZINE | Phenethyl-hydra...)
Affinity DataKi:  5.43E+4nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using human liver microsomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50336507(4-pyridinecarbohydrazide(Isoniazid) | CHEMBL64 | D...)
Affinity DataKi:  1.70E+5nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using human liver microsomesMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM30130(CHEMBL1201082 | CHEMBL41 | Fluoxetin | Fluoxetine ...)
Affinity DataKi:  2.94E+5nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50336507(4-pyridinecarbohydrazide(Isoniazid) | CHEMBL64 | D...)
Affinity DataKi:  3.74E+5nMAssay Description:Mechanism based inhibition of human cytochrome P450 2C8 measured by paclitaxel hydroxylation using a recombinant systemMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50393342(CHEMBL2152252)
Affinity DataIC50:  2.33E+3nMAssay Description:Inhibition of human CYP2C8 using paclitaxel as substrate after 45 mins by LC/MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50417554(ANIDULAFUNGIN)
Affinity DataIC50:  1.20E+4nMAssay Description:Inhibition of human CYP2C8 using amodiaquine as a substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50417554(ANIDULAFUNGIN)
Affinity DataIC50: >1.75E+4nMAssay Description:Inhibition of human CYP2C8 using rosiglitazone as a substrateMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50438845(CHEMBL2413882)
Affinity DataIC50:  120nMAssay Description:Inhibition of CYP2C8 in human liver microsomes assessed as paclitaxel 6alpha-hydroxylation after 20 mins by LC-MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50438846(CHEMBL2413881)
Affinity DataIC50:  220nMAssay Description:Inhibition of CYP2C8 in human liver microsomes assessed as paclitaxel 6alpha-hydroxylation after 20 mins by LC-MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50437205(CHEMBL2402572)
Affinity DataIC50:  2.10E+4nMAssay Description:Inhibition of human CYP2C8More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM7460(2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chrome...)
Affinity DataIC50:  3.50E+3nMAssay Description:The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest); The IC50s of the compounds w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM189322(US9173935, SC12)
Affinity DataIC50: >1.00E+5nMAssay Description:The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest); The IC50s of the compounds w...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM190404(US9180183, SC12)
Affinity DataIC50: >1.00E+5nMT: 2°CAssay Description:The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest); The IC50s of the compounds w...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM7460(2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-chrome...)
Affinity DataIC50:  3.50E+3nMT: 2°CAssay Description:The interaction of SC12 with cytochrome P450 enzymes was tested using Fluorescent High Throughput P450 assays (Gentest); The IC50s of the compounds w...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM50120423(CHEMBL3617971 | US9290459, 1A | US9670166, 1A)
Affinity DataIC50: >5.00E+4nMT: 2°CAssay Description:The inhibition of cytochrome P450 2C8-isoenzyme catalysed deethylation of Amodiaquine by the test compound is assayed at 37° C. with human liver ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211757(US9290459, 10A | US9290459, 47.21 | US9670166, 10A)
Affinity DataIC50: >5.00E+4nMT: 2°CAssay Description:The inhibition of cytochrome P450 2C8-isoenzyme catalysed deethylation of Amodiaquine by the test compound is assayed at 37° C. with human liver ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211754(US9290459, 9A | US9670166, 9A)
Affinity DataIC50: >5.00E+4nMT: 2°CAssay Description:The inhibition of cytochrome P450 2C8-isoenzyme catalysed deethylation of Amodiaquine by the test compound is assayed at 37° C. with human liver ...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Epizyme

US Patent
LigandPNGBDBM211750(US9290459, 7.2A | US9670166, 7.2A)
Affinity DataIC50: >5.00E+4nMT: 2°CAssay Description:The inhibition of cytochrome P450 2C8-isoenzyme catalysed deethylation of Amodiaquine by the test compound is assayed at 37° C. with human liver ...More data for this Ligand-Target Pair
Ligand InfoKEGGPC cidPC sid
In DepthDetails US Patent
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