lovastatin [Ligand Id: 2739] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL503 (Mevinacor, Mevinolin, C10AA02, Mevinacor 10, Mevacor, Lovastatin, L-154803, Mevinacor 40, Simvastatin impurity, lovastatin-, MK-803, Altoprev)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • Acyl-CoA:cholesterol acyltransferase in Rabbit [ChEMBL: CHEMBL6141] [UniProtKB: Q95214]
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • Androgen receptor/Androgen Receptor in Rat [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
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  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
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  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
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  • histone deacetylase 6/Histone deacetylase 6 in Human [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
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  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Mouse [ChEMBL: CHEMBL2764] [GtoPdb: 639] [UniProtKB: Q01237]
  • hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639]
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  • integrin, beta 2 subunit (complement component 3 receptor 3 and 4 subunit)/integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)/Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2 in Human [ChEMBL: CHEMBL2096661] [GtoPdb: 24562451] [UniProtKB: P05107P05362P20701]
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  • integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)/Leukocyte adhesion glycoprotein LFA-1 alpha in Human [ChEMBL: CHEMBL1803] [GtoPdb: 2451] [UniProtKB: P20701]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
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  • Pregnane X receptor in Human [GtoPdb: 606] [UniProtKB: O75469]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method B 5.57 pKi 2700 nM Ki Med Chem Res (2005) 14: 297-308
Acyl-CoA:cholesterol acyltransferase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6141] [UniProtKB: Q95214]
ChEMBL Inhibition of ACAT in Albino rabbit intestinal mucosa B 4.77 pIC50 16800 nM IC50 Bioorg. Med. Chem. Lett. (2007) 17: 1946-1950 [PMID:17275297]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 4.81 pKi 15586 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX) B 4.57 pIC50 26720 nM IC50 DrugMatrix in vitro pharmacology data
Androgen receptor/Androgen Receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3072] [GtoPdb: 628] [UniProtKB: P15207]
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.7 pKi 20110 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone) B 4.52 pIC50 30164 nM IC50 DrugMatrix in vitro pharmacology data
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 5.3 pKi 5011.87 nM Ki Med Chem Res (2005) 14: 297-308
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 5.96 pKi 1100 nM Ki Med Chem Res (2005) 14: 297-308
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.1 pKi 8028 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5 pIC50 10104 nM IC50 DrugMatrix in vitro pharmacology data
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of recombinant HDAC1 (unknown origin) after 10 mins by fluorimetric analysis B 4.92 pIC50 11911 nM IC50 J. Med. Chem. (2013) 56: 3645-3655 [PMID:23570542]
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 4.92 pIC50 11911 nM IC50 US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015)
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 4.95 pIC50 11214 nM IC50 US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016)
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of recombinant HDAC2 (unknown origin) after 10 mins by fluorimetric analysis B 4.59 pIC50 25933 nM IC50 J. Med. Chem. (2013) 56: 3645-3655 [PMID:23570542]
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 4.59 pIC50 25933 nM IC50 US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015)
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 4.59 pIC50 25933 nM IC50 US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016)
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7]
ChEMBL Inhibition of recombinant HDAC6 (unknown origin) after 10 mins by fluorimetric analysis B 4.79 pIC50 16285 nM IC50 J. Med. Chem. (2013) 56: 3645-3655 [PMID:23570542]
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 4.79 pIC50 16285 nM IC50 US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015)
ChEMBL Fluorescent Activity Assay: The HDAC activity was performed using the HDAC fluorescent activity assay kit (BIOMOL, Plymouth Meeting, Pa., USA) according to the manufacturer's instructions. Briefly, recombinant proteins of HDAC1 or HDAC6 were incubated with test compounds, and HDAC reaction was initiated by addition of Fluor-de-Lys substrate. Samples were incubated for 10 min at room temperature, followed by adding developer to stop the reaction. Fluorescence was measured by fluorometric reader with excitation at 360 nm and emission at 460 nm. The HDAC activity was expressed as arbitrary fluorescence units (AFU). B 4.79 pIC50 16283 nM IC50 US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016)
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL402] [GtoPdb: 639] [UniProtKB: P04035]
GtoPdb Inhibition of HMG-CoA reductase - 9.22 pKi 0.6 nM Ki Proc. Natl. Acad. Sci. U.S.A. (1980) 77: 3957-61 [PMID:6933445]
ChEMBL Inhibition of human HMGCoA reductase B 9.22 pKi 0.6 nM Ki J. Nat. Prod. (1989) 52: 153-161
ChEMBL Inhibition of HMG-CoA reductase using HMG-CoA as substrate by spectrophotometry in presence of NADPH B 4.7 pIC50 20100 nM IC50 Eur. J. Med. Chem. (2011) 46: 5206-5211 [PMID:21872367]
ChEMBL Inhibition of HMG-CoA reductase in human A549 cells after 5 mins by spectrophotometric analysis B 4.7 pIC50 19800 nM IC50 J. Med. Chem. (2013) 56: 3645-3655 [PMID:23570542]
GtoPdb in vitro inhibition of HMG-CoA reductase - 7.3 pIC50 50 nM IC50 J. Med. Chem. (1990) 33: 61-70 [PMID:2153213]
ChEMBL Inhibition of the incorporation of sodium [14C]acetate into cholesterol in HEP G2 cells. F 7.3 pIC50 50 nM IC50 J. Med. Chem. (1991) 34: 2962-2983 [PMID:1656041]
ChEMBL Inhibition of cellular HMG-CoA reductase in cultures of human HEP G2 cells, determined by decreased incorporation of sodium [14C]acetate into cholesterol. B 7.3 pIC50 50 nM IC50 J. Med. Chem. (1990) 33: 52-60 [PMID:2296036]
ChEMBL Compound was evaluated for inhibitory activity against HMG-CoA reductase in HepG2 cells B 7.41 pIC50 39 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1085-1088
ChEMBL Concentration required to inhibit HMG-CoA reductase by 50% was determined in Hep G2 cell line F 7.43 pIC50 37 nM IC50 J. Med. Chem. (1992) 35: 3388-3393 [PMID:1527791]
ChEMBL Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negative control. HMGR activity under defined assay conditions, containing NADPH and HMG-CoA substrate in a final volume of 0.2 mL of 100 mM potassium phosphatate buffer (120 mM KCI, 1 mM EDTA, 5 mM DTT, pH 7.4), were initiated in the presence or absence (control) of test compounds dissolved in dimethylsulfoxide (DMSO). The rates of NADPH consumption were monitored every 20 seconds, for up to 10 minutes, by spectrophotometer at 37° C. and 340 nm. B 7.53 pIC50 29.5 nM IC50 US-9115116-B2. Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase (2015)
ChEMBL Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negative control. HMGR activity under defined assay conditions, containing NADPH and HMG-CoA substrate in a final volume of 0.2 mL of 100 mM potassium phosphatate buffer (120 mM KCl, 1 mM EDTA, 5 mM DTT, pH 7.4), were initiated in the presence or absence (control) of test compounds dissolved in dimethylsulfoxide (DMSO). The rates of NADPH consumption were monitored every 20 seconds, for up to 10 minutes, by spectrophotometer at 37° C. and 340 nm. B 7.53 pIC50 29.5 nM IC50 US-9353061-B2. 3,5,N-trihydroxy-alkanamide and derivatives: method for making same and use thereof (2016)
ChEMBL Inhibition of recombinant HMG-CoA reductase (unknown origin) after 10 mins by spectrophotometric analysis B 7.53 pIC50 29.5 nM IC50 J. Med. Chem. (2013) 56: 3645-3655 [PMID:23570542]
GtoPdb in vitro inhition of HMG-CoA reductase - 7.69 pIC50 20 nM IC50 J. Med. Chem. (1992) 35: 2095-103 [PMID:1597859]
ChEMBL Tested in vitro for the inhibition of HMG-CoA reductase from partially purified microsomal preparations. B 7.7 pIC50 20 nM IC50 J. Med. Chem. (1992) 35: 2095-2103 [PMID:1597859]
ChEMBL DRUGMATRIX: HMG-CoA Reductase enzyme inhibition (substrate: [14C]HMG-CoA) B 7.7 pIC50 20 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of HMG-CoA reductase (unknown origin) using [14C]-HMG-CoA as substrate after 5 mins in presence of NADPH B 8.66 pIC50 2.2 nM IC50 J Med Chem (2018) 61: 2166-2210 [PMID:28850227]
ChEMBL Inhibition of human HMGCoA reductase B 8.7 pIC50 2 nM IC50 J. Nat. Prod. (1989) 52: 153-161
ChEMBL Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line) B 10.3 pIC50 0.05 nM IC50 J. Med. Chem. (1990) 33: 61-70 [PMID:2153213]
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2764] [GtoPdb: 639] [UniProtKB: Q01237]
ChEMBL In vitro inhibitory activity against isolated enzyme HMG-CoA reductase B 7.57 pIC50 27 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1085-1088
GtoPdb In vitro inhibition of HMG-CoA reductase - 7.57 pIC50 27 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 223-228
hydroxymethylglutaryl-CoA reductase/HMG-CoA reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3247] [GtoPdb: 639] [UniProtKB: P51639]
ChEMBL Tested in vitro for the HMG-CoA reductase inhibitory activity in a microsomal preparation B 6.28 pIC50 530 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 549-554
GtoPdb in vitro inhition of HMG-CoA reductase - 6.3 pIC50 530 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 549-554
ChEMBL Inhibitory activity against partially purified rat liver HMG-CoA reductase in vitro; 0.23-0.71 B 6.4 pIC50 400 nM IC50 J. Med. Chem. (1993) 36: 3674-3685 [PMID:8246237]
GtoPdb in vitro inhition of HMG-CoA reductase - 6.8 pIC50 160 nM IC50 Bioorg. Med. Chem. Lett. (1997) 7: 549-554
ChEMBL In vitro inhibitory activity was measured against rat liver HMG-CoA reductase using [2-14C]-acetate incorporation B 7.49 pIC50 32 nM IC50 J. Med. Chem. (1990) 33: 2982-2999 [PMID:2231596]
ChEMBL Compound was evaluated for inhibitory activity against HMG-CoA reductase from rat hepatocyte B 7.49 pIC50 32 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 1085-1088
GtoPdb in vitro inhition of HMG-CoA reductase - 7.55 pIC50 27 nM IC50 J. Med. Chem. (1991) 34: 367-73 [PMID:1992138]
ChEMBL Compound was evaluated for the inhibition of HMG-CoA reductase (COR) in rats. B 7.55 pIC50 28 nM IC50 J. Med. Chem. (1991) 34: 367-373 [PMID:1992138]
ChEMBL In vitro inhibitory activity was measured against rat liver HMG-CoA reductase B 7.57 pIC50 27 nM IC50 J. Med. Chem. (1990) 33: 2982-2999 [PMID:2231596]
ChEMBL Inhibition of microsomal rat liver HMG-CoA reductase B 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 223-228
GtoPdb in vitro inhibition of HMG-CoA reductase - 7.96 pIC50 11 nM IC50 Bioorg. Med. Chem. Lett. (1992) 2: 223-228
ChEMBL In vitro inhibition of HMG-CoA reductase in solubilized rat liver. B 8.1 pIC50 8 nM IC50 J. Med. Chem. (1991) 34: 2962-2983 [PMID:1656041]
ChEMBL In vitro inhibition of HMG-CoA reductase of rat liver B 8.1 pIC50 8 nM IC50 J. Med. Chem. (1990) 33: 61-70 [PMID:2153213]
ChEMBL In vitro inhibition of rat liver HMG-CoA reductase B 8.1 pIC50 8 nM IC50 J. Med. Chem. (1990) 33: 52-60 [PMID:2296036]
GtoPdb in vitro inhibition of HMG-CoA reductase - 8.1 pIC50 8 nM IC50 J. Med. Chem. (1991) 34: 2962-83 [PMID:1656041]
GtoPdb in vitro inhibition of HMG-CoA reductase - 8.1 pIC50 8 nM IC50 J. Med. Chem. (1990) 33: 61-70 [PMID:2153213]
ChEMBL Tested for inhibition of rat liver microsomal HMG-CoA reductase B 8.15 pIC50 7 nM IC50 J. Med. Chem. (1994) 37: 3240-3246 [PMID:7932551]
GtoPdb in vitro inhition of HMG-CoA reductase - 8.52 pIC50 3 nM IC50 J. Med. Chem. (1993) 36: 3658-62 [PMID:8246234]
ChEMBL Inhibition of rat liver microsomal HMG-CoA reductase B 8.52 pIC50 3 nM IC50 J. Med. Chem. (1993) 36: 3658-3662 [PMID:8246234]
integrin, beta 2 subunit (complement component 3 receptor 3 and 4 subunit)/integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)/Intercellular adhesion molecule (ICAM-1), Integrin alpha-L/beta-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2096661] [GtoPdb: 24562451] [UniProtKB: P05107P05362P20701]
ChEMBL In vitro inhibition of recombinant ICAM-1 binding to purified immobilized LFA-1 using cell-free assay F 5.42 pIC50 3780 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 2483-2487 [PMID:15109637]
integrin, alpha L subunit (antigen CD11A (p180), lymphocyte function-associated antigen 1; alpha polypeptide)/Leukocyte adhesion glycoprotein LFA-1 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1803] [GtoPdb: 2451] [UniProtKB: P20701]
ChEMBL Binding affinity to I-domain of human integrin alphaL (amino acid residues 128 to 307) plus initial methionine expressed in Escherichia coli by NMR spectroscopy B 4.89 pKd 12900 nM Kd J. Med. Chem. (2013) 56: 735-747 [PMID:23339734]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.03 pKi 9408 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 4.55 pIC50 28224 nM IC50 DrugMatrix in vitro pharmacology data
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.06 pKi 8680 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.06 pIC50 8753 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 transport in 3T3-G185 cells F 4.17 pIC50 67000 nM IC50 Pharm. Res. (2001) 18: 800-806 [PMID:11474784]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 4.49 pIC50 32700 nM IC50 Biochem. Biophys. Res. Commun. (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin transport in 3T3-G185 cells F 4.59 pIC50 26000 nM IC50 Pharm. Res. (2001) 18: 800-806 [PMID:11474784]
ChEMBL TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells F 5 pIC50 10000 nM IC50 Drug Metab. Dispos. (2005) 33: 537-546 [PMID:15616150]
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
ChEMBL TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells F 4.55 pIC50 28000 nM IC50 Drug Metab. Dispos. (2005) 33: 537-546 [PMID:15616150]
Pregnane X receptor in Human [GtoPdb: 606] [UniProtKB: O75469]
GtoPdb - - 6 pEC50 1000 nM EC50 J. Clin. Invest. (1998) 102: 1016-23 [PMID:9727070]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]