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, Tilarginina, 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]
  • Inducible NOS/Nitric oxide synthase, inducible in Rat [ChEMBL: CHEMBL3051] [GtoPdb: 1250] [UniProtKB: Q06518]
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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 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 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 Concentration required to inhibit neuronal nitric oxide synthase B 6.05 pIC50 890 nM IC50 Bioorg Med Chem Lett (2002) 12: 2561-2564 [PMID:12182860]
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]
ChEMBL Inhibitory activity against human neuronal nitric oxide synthase B 7.05 pIC50 90 nM IC50 J Med Chem (2003) 46: 913-916 [PMID:12620067]
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 Compound was tested for binding affinity against neuronal nitric oxide synthase(nNOS) B 5 pKi 10000 nM Ki J Med Chem (1997) 40: 3869-3870 [PMID:9397167]
ChEMBL Inhibition of rat nNOS transfected in HEK293 cells assessed as inhibition constant in presence of NADPH by spectrophotometric analysis B 6.3 pKi 500 nM Ki Bioorg Med Chem (2022) 72: 116970-116970 [PMID:36063653]
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 In vitro inhibition of endothelial nitric oxide synthase. B 6.27 pIC50 540 nM IC50 Bioorg Med Chem Lett (2002) 12: 2561-2564 [PMID:12182860]
ChEMBL Inhibitory activity against human endothelial nitric oxide synthase B 6.48 pIC50 330 nM IC50 J Med Chem (2003) 46: 913-916 [PMID:12620067]
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 Compound was tested for binding affinity against Endothelial nitric oxide synthase B 5.23 pKi 5900 nM Ki J Med Chem (1997) 40: 3869-3870 [PMID:9397167]
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 iNOS (unknown origin) B 5.18 pIC50 6600 nM IC50 Eur J Med Chem (2023) 248: 115112-115112 [PMID:36641860]
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 In vitro inhibition of inducible nitric oxide synthase. B 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2002) 12: 2561-2564 [PMID:12182860]
ChEMBL Inhibitory activity of compound against human inducible nitric oxide synthase B 6.47 pIC50 340 nM IC50 J Med Chem (2003) 46: 913-916 [PMID:12620067]
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 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 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 for binding affinity against recombinant inducible nitric oxide synthase (iNOS) from mouse B 4.85 pKi 14000 nM Ki J Med Chem (1997) 40: 3869-3870 [PMID:9397167]
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 Tested for inhibition of mouse inducible nitric oxide synthase B 5.08 pIC50 8300 nM IC50 J Med Chem (1994) 37: 3886-3888 [PMID:7525961]
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]
Inducible NOS/Nitric oxide synthase, inducible in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3051] [GtoPdb: 1250] [UniProtKB: Q06518]
ChEMBL Tested for inhibition of rat brain inducible nitric oxide synthase B 4.74 pIC50 18000 nM IC50 J Med Chem (1994) 37: 3886-3888 [PMID:7525961]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]