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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) |
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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 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]