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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]