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

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
LigandPNGBDBM50523585(CHEMBL4577468)
Affinity DataIC50:  2.5nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50239250(CHEMBL4086080)
Affinity DataIC50:  26nMAssay Description:Inhibition of microsomal CYP2C8 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50384467(CHEMBL2036213)
Affinity DataIC50:  43nMAssay Description:Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM155255(US10098888, Compound 105 | US11642348, Compound 10...)
Affinity DataIC50:  47.4nMAssay 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))
Celgene

Curated by ChEMBL
LigandPNGBDBM50123453(CHEMBL3623290)
Affinity DataIC50: >50nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50384475(CHEMBL2036225)
Affinity DataIC50:  50nMAssay Description:Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50384472(CHEMBL2036220)
Affinity DataIC50:  54nMAssay Description:Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50533229(CHEMBL4446613)
Affinity DataIC50:  79nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50384473(CHEMBL2036222)
Affinity DataIC50:  79nMAssay Description:Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50533229(CHEMBL4446613)
Affinity DataIC50:  79nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50384464(CHEMBL2036210)
Affinity DataIC50:  86nMAssay Description:Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50463725(CHEMBL4242598)
Affinity DataIC50:  100nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50533234(CHEMBL4437930)
Affinity DataIC50:  100nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM155253(US10098888, Compound 1 | US9006242, 1)
Affinity DataIC50: >100nMAssay 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))
Celgene

Curated by ChEMBL
LigandPNGBDBM50090462(CHEMBL3581693)
Affinity DataIC50: <100nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50533234(CHEMBL4437930)
Affinity DataIC50:  100nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM155254(US10098888, Compound 2 | US9006242, 2)
Affinity DataIC50: >100nMAssay 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))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
LigandPNGBDBM50052024(CHEMBL787 | montelukast)
Affinity DataIC50:  130nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate incubated for 5 to 45 mins in presence of NADPH by LC/MS analysisMore data for this Ligand-Target Pair
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50175303(CHEMBL3810042)
Affinity DataIC50:  180nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50265673(CHEMBL4068611)
Affinity DataIC50:  210nMAssay Description:Inhibition of CYP2C8 (unknown origin)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50253810(CHEMBL459505 | N-(4-(2-ethyl-1-(1H-1,2,4-triazol-1...)
Affinity DataIC50:  220nMAssay Description:Compounds were assessed for inhibition (IC50, n=2) of CYP2C8, CYP2C9 and CYP3A4 in pooled human liver microsomes using selective probe substrates at ...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
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))
Celgene

Curated by ChEMBL
LigandPNGBDBM50384474(CHEMBL2036223)
Affinity DataIC50:  220nMAssay Description:Inhibition of human recombinant CYP2C8 incubated for 15 mins prior to substrate addition measured after 30 mins by spectrophotometryMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50380508(CHEMBL2018923)
Affinity DataIC50:  250nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using paclitaxel as substrate preincubated for 5 mins by LC-MS/MS analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM50366401(CHEMBL4169721)
Affinity DataIC50:  260nMAssay Description:Inhibition of CYP2C8 in human liver microsomes using amodiaquine as substrate preincubated for 5 mins followed by addition of NADPH-regenerating syst...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetCytochrome P450 2C8(Homo sapiens (Human))
Celgene

Curated by ChEMBL
LigandPNGBDBM253985(US9481673, 27)
Affinity DataIC50:  300nMAssay Description:The final incubation volume contains TRIS buffer (0.1 M), MgCl2 (5 mM), a certain concentration of human liver microsomes dependent on the P450 isoen...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
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