tilarginine [Ligand Id: 11467] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL256147 (L-NMMA, Ng-methylarginine, Ng-monomethyl-l-arginine, .omega.-n-methylarginine, Omega-n-methylarginine, Omega-n-methylated arginine, Targinine, Tilarginine)
  • Neuronal NOS/Nitric-oxide synthase, brain in Human [ChEMBL: CHEMBL3568] [GtoPdb: 1251] [UniProtKB: P29475]
  • Neuronal NOS/Nitric-oxide synthase, brain in Mouse [ChEMBL: CHEMBL4719] [GtoPdb: 1251] [UniProtKB: Q9Z0J4]
  • Neuronal NOS/Nitric-oxide synthase, brain in Rat [ChEMBL: CHEMBL3048] [GtoPdb: 1251] [UniProtKB: P29476]
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  • Endothelial NOS/Nitric-oxide synthase, endothelial in Human [ChEMBL: CHEMBL4803] [GtoPdb: 1249] [UniProtKB: P29474]
  • Nitric-oxide synthase, endothelial in Bovine [ChEMBL: CHEMBL4802] [UniProtKB: P29473]
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  • Inducible NOS/Nitric oxide synthase, inducible in Human [ChEMBL: CHEMBL4481] [GtoPdb: 1250] [UniProtKB: P35228]
  • Inducible NOS/Nitric oxide synthase, inducible in Mouse [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Neuronal NOS/Nitric-oxide synthase, brain in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3568] [GtoPdb: 1251] [UniProtKB: P29475]
ChEMBL Inhibitory constant for the inhibition of human Neuronal nitric oxide synthase B 6.08 pKi 840 nM Ki Bioorg Med Chem Lett (1997) 7: 1763-1768
ChEMBL Inhibitory activity against human neuronal nitric oxide synthase (nNOS) isoenzyme. B 6.08 pKi 840 nM Ki J Med Chem (1998) 41: 2858-2871 [PMID:9667974]
GtoPdb - - 6.08 pKi 840 nM Ki Bioorganic and Medicinal Chemistry Letters (1997) 7: 1763-1768
ChEMBL Inhibition of cloned (from RNA) human Neuronal nitric oxide synthase B 5 pIC50 10000 nM IC50 J Med Chem (1998) 41: 3675-3683 [PMID:9733492]
ChEMBL Inhibition of human neuronal Nitric Oxide Synthase B 5.31 pIC50 4900 nM IC50 Bioorg Med Chem Lett (2000) 10: 597-600 [PMID:10741561]
ChEMBL Inhibitory activity against neuronal nitric oxide synthase B 5.57 pIC50 2700 nM IC50 Bioorg Med Chem Lett (2000) 10: 1975-1978 [PMID:10987430]
ChEMBL Inhibition of human recombinant nNOS assessed as conversion of [3H]L-arginine to [3H]L-citrulline preincubated for 15 mins measured after 45 mins by liquid scintillation counting B 6.02 pIC50 950 nM IC50 ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459]
ChEMBL Inhibition of human nNOS expressed in Sf9 cells assessed as reduction in conversion of [3H]L-arginine to [3H]L-citrulline preincubated for 15 mins by radiometric method B 6.02 pIC50 950 nM IC50 J Med Chem (2012) 55: 2882-2893 [PMID:22335555]
ChEMBL Inhibitory concentration against recombinant human (neuronal nitric oxide synthase) n-NOS B 6.05 pIC50 890 nM IC50 Bioorg Med Chem Lett (2003) 13: 1981-1984 [PMID:12781178]
Neuronal NOS/Nitric-oxide synthase, brain in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4719] [GtoPdb: 1251] [UniProtKB: Q9Z0J4]
ChEMBL Inhibition of neuronal nitric oxide synthase (nNOS) in mice B 5.37 pIC50 4300 nM IC50 Bioorg Med Chem Lett (2004) 14: 313-316 [PMID:14698148]
Neuronal NOS/Nitric-oxide synthase, brain in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3048] [GtoPdb: 1251] [UniProtKB: P29476]
ChEMBL Inhibition of rat nNOS B 6.7 pKi 200 nM Ki J Med Chem (2013) 56: 3121-3147 [PMID:23458846]
ChEMBL Compound was tested in vitro for inhibitory activity against nNOS (constitutive isoform found in neurons) B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (1996) 6: 999-1002
ChEMBL Inhibitory activity against isomeric form of Neuronal nitric oxide synthase measured by citrulline assay B 5.12 pIC50 7500 nM IC50 J Med Chem (1998) 41: 2636-2642 [PMID:9651169]
ChEMBL Ability to inhibit the conversion of [3H]-L-Arg to [3H]L-citrulline catalyzed by n-NOS from rat cerebellum F 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2001) 11: 1027-1030 [PMID:11327581]
ChEMBL Inhibition of conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by neuronal NOS (n NOS) from rat cerebellum F 7 pIC50 100 nM IC50 Bioorg Med Chem Lett (2001) 11: 1023-1026 [PMID:11327580]
Endothelial NOS/Nitric-oxide synthase, endothelial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4803] [GtoPdb: 1249] [UniProtKB: P29474]
ChEMBL Inhibitory constant for the inhibition of human Endothelial nitric oxide synthase B 6.4 pKi 400 nM Ki Bioorg Med Chem Lett (1997) 7: 1763-1768
ChEMBL Inhibitory activity against human endothelial nitric oxide synthase (eNOS) isoenzyme. B 6.4 pKi 400 nM Ki J Med Chem (1998) 41: 2858-2871 [PMID:9667974]
GtoPdb - - 6.4 pKi 400 nM Ki Bioorganic and Medicinal Chemistry Letters (1997) 7: 1763-1768
ChEMBL Inhibitory activity against endothelial nitric oxide synthase (eNOS) B 5.06 pIC50 8700 nM IC50 Bioorg Med Chem Lett (2000) 10: 1975-1978 [PMID:10987430]
ChEMBL The compound was evaluated for the inhibitory potencies using human Endothelial nitric oxide synthase B 5.22 pIC50 6000 nM IC50 J Med Chem (1996) 39: 5110-5118 [PMID:8978842]
ChEMBL Inhibition of cloned (from RNA) human endothelial constitutive Endothelial nitric oxide synthase (heNOS) B 5.23 pIC50 5900 nM IC50 J Med Chem (1998) 41: 3675-3683 [PMID:9733492]
ChEMBL Inhibition of human endothelial Nitric Oxide Synthase B 5.46 pIC50 3500 nM IC50 Bioorg Med Chem Lett (2000) 10: 597-600 [PMID:10741561]
ChEMBL Inhibition of human eNOS expressed in Sf9 cells assessed as reduction in conversion of [3H]L-arginine to [3H]L-citrulline preincubated for 15 mins by radiometric method B 6.19 pIC50 650 nM IC50 J Med Chem (2012) 55: 2882-2893 [PMID:22335555]
ChEMBL Inhibition of human recombinant eNOS assessed as conversion of [3H]L-arginine to [3H]L-citrulline preincubated for 15 mins measured after 45 mins by liquid scintillation counting B 6.19 pIC50 650 nM IC50 ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459]
ChEMBL Inhibitory concentration against recombinant human Endothelial nitric oxide synthase B 6.27 pIC50 540 nM IC50 Bioorg Med Chem Lett (2003) 13: 1981-1984 [PMID:12781178]
ChEMBL Ability to inhibit the conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by e-NOS from HUVEC cells F 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2001) 11: 1027-1030 [PMID:11327581]
ChEMBL Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by endothelial NOS (e NOS) from HUVEC cells F 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2001) 11: 1023-1026 [PMID:11327580]
Nitric-oxide synthase, endothelial in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4802] [UniProtKB: P29473]
ChEMBL Inhibitory activity of conversion of radiolabeled arginine to citrulline by isomeric form of nitric oxide synthase Endothelial nitric oxide synthase from cultured bovine aortic endothelial cells B 5.15 pIC50 7000 nM IC50 J Med Chem (1998) 41: 2636-2642 [PMID:9651169]
Inducible NOS/Nitric oxide synthase, inducible in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4481] [GtoPdb: 1250] [UniProtKB: P35228]
ChEMBL Inhibitory constant for the inhibition of human Inducible nitric oxide synthase B 6.07 pKi 860 nM Ki Bioorg Med Chem Lett (1997) 7: 1763-1768
ChEMBL Inhibitory activity against human inducible nitric oxide synthase (iNOS) isoenzyme. B 6.07 pKi 860 nM Ki J Med Chem (1998) 41: 2858-2871 [PMID:9667974]
GtoPdb - - 6.07 pKi 860 nM Ki Bioorganic and Medicinal Chemistry Letters (1997) 7: 1763-1768
ChEMBL The compound was evaluated for the inhibitory potencies using human Inducible nitric oxide synthase (hiNOS) B 4.57 pIC50 27000 nM IC50 J Med Chem (1996) 39: 5110-5118 [PMID:8978842]
ChEMBL Inhibition of cloned (from RNA) human inducible nitric oxide synthase (hiNOS) B 4.85 pIC50 14000 nM IC50 J Med Chem (1998) 41: 3675-3683 [PMID:9733492]
ChEMBL Inhibitory activity against inducible nitric oxide synthase (iNOS) B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (2000) 10: 1975-1978 [PMID:10987430]
ChEMBL Inhibition of human inducible nitric oxide synthase B 5.18 pIC50 6600 nM IC50 Bioorg Med Chem Lett (2000) 10: 597-600 [PMID:10741561]
ChEMBL Inhibition of iNOS B 5.47 pIC50 3400 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Inhibition of human recombinant iNOS expressed in Sf9 cells assessed as reduction in conversion of [3H]L-arginine to [3H]L-citrulline preincubated for 15 mins by radiometric method B 5.74 pIC50 1800 nM IC50 J Med Chem (2012) 55: 2882-2893 [PMID:22335555]
ChEMBL Inhibitory concentration against human Inducible nitric oxide synthase B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2003) 13: 1981-1984 [PMID:12781178]
ChEMBL Ability to inhibit conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by inducible NOS (i NOS) from human DLD-1 cells F 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2001) 11: 1023-1026 [PMID:11327580]
ChEMBL Ability to inhibit the conversion of [3H]L-Arg to [3H]L-citrulline catalyzed by i-NOS from human DLD-1 cells F 6.52 pIC50 300 nM IC50 Bioorg Med Chem Lett (2001) 11: 1027-1030 [PMID:11327581]
ChEMBL Inhibition of human recombinant iNOS assessed as conversion of [3H]L-arginine to [3H]L-citrulline preincubated for 15 mins measured after 45 mins by liquid scintillation counting B 8.74 pIC50 1.8 nM IC50 ACS Med Chem Lett (2012) 3: 227-231 [PMID:24900459]
Inducible NOS/Nitric oxide synthase, inducible in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3464] [GtoPdb: 1250] [UniProtKB: P29477]
ChEMBL Compound was tested in vitro for inhibitory activity against inducible nitric oxide synthase B 4.6 pIC50 25000 nM IC50 Bioorg Med Chem Lett (1996) 6: 999-1002
ChEMBL Inhibition of radiolabeled arginine conversion to citrulline by isomeric form of Inducible nitric oxide synthase from mouse RAW 264.7 cells B 4.6 pIC50 25000 nM IC50 J Med Chem (1998) 41: 2636-2642 [PMID:9651169]
ChEMBL Inhibition of iNOS-mediated nitric oxide production in LPS-stimulated mouse RAW 264.7 cells pretreated 15 mins before LPS challenge measured after 20 hrs relative to control B 4.66 pIC50 22100 nM IC50 Bioorg Med Chem (2011) 19: 6182-6195 [PMID:21978950]
ChEMBL Inhibition of LPS-induced iNOS activity in mouse RAW 264.7 cells assessed as inhibition of NO production pretreated with compound for 30 mins before LPS challenge after 24 hrs by Griess reagent method B 4.71 pIC50 19700 nM IC50 Bioorg Med Chem (2012) 20: 7030-7039 [PMID:23142320]
ChEMBL Inhibition of inducible nitric oxide synthase (iNOS) in mice B 4.72 pIC50 19000 nM IC50 Bioorg Med Chem Lett (2004) 14: 313-316 [PMID:14698148]
ChEMBL Inhibition of iNOS in ddY mouse peritoneal exudate cells after 20 hrs B 4.89 pIC50 13000 nM IC50 J Nat Prod (2004) 67: 1119-1124 [PMID:15270564]
ChEMBL Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS activity incubated for 30 mins prior to LPS challenge measured after 24 hrs by Griess assay B 5.64 pIC50 2300 nM IC50 Bioorg Med Chem (2015) 23: 3248-3259 [PMID:25975638]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]