Nω-hydroxy-nor-L-arginine [Ligand Id: 5091] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1234777
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Arginase I/Arginase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075097] [GtoPdb: 1244] [UniProtKB: P05089]
ChEMBL Binding affinity to human Arg1 at pH 8.5 B 6.29 pKd 517 nM Kd Bioorg Med Chem (2020) 28: 115658-115658 [PMID:32828425]
ChEMBL Inhibition of human Arginase I assessed as dissociation constant by ITC analysis B 7.3 pKd 50 nM Kd Bioorg Med Chem Lett (2023) 84: 129193-129193 [PMID:36822300]
ChEMBL Binding affinity to arginase 1 (unknown origin) B 7.33 pKd 47 nM Kd Bioorg Med Chem Lett (2018) 28: 319-329 [PMID:29326017]
ChEMBL Inhibition of recombinant human liver ARGI using L-arginine as substrate incubated for 60 mins by spectroscopic analysis B 5.22 pIC50 6000 nM IC50 RSC Med Chem (2020) 11: 559-568 [PMID:33479657]
ChEMBL Inhibition of human ARG1 B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2018) 157: 582-598 [PMID:30125720]
ChEMBL Inhibition of human arginase 1 measured after 60 mins by calorimetric assay B 5.77 pIC50 1700 nM IC50 Bioorg Med Chem (2022) 72: 116970-116970 [PMID:36063653]
ChEMBL Inhibition of human recombinant arginase 1 expressed in Escherichia coli BL21 (DE3) assessed as reduction in urea production using L-arginine as substrate in presence of MnSO4 incubated for 60 mins by o-phthaldialdehyde/N-(1-naphthyl)ethylene-diamine dihydrochloride reagent based colorimetric assay B 5.87 pIC50 1360 nM IC50 J Med Chem (2019) 62: 8164-8177 [PMID:31408339]
ChEMBL Binding affinity to human ARG1 assessed as dissociation constant B 6.29 pIC50 517 nM IC50 Eur J Med Chem (2021) 218: 113356-113356 [PMID:33773287]
ChEMBL Inhibition of recombinant human ARG1 expressed in Escherichia coli using L-arginine hydrochloride as substrate incubated for 1 hr by colorimetric assay B 6.35 pIC50 450 nM IC50 Eur J Med Chem (2021) 218: 113356-113356 [PMID:33773287]
Arginase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075060] [UniProtKB: Q2KJ64]
ChEMBL Inhibition of recombinant bovine liver ARGI using L-arginine as substrate incubated for 60 mins by spectroscopic analysis B 5.57 pIC50 2700 nM IC50 RSC Med Chem (2020) 11: 559-568 [PMID:33479657]
Arginase I/Arginase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3232699] [GtoPdb: 1244] [UniProtKB: P07824]
ChEMBL Inhibition of Sprague-Dawley rat liver arginase 1 assessed as inhibition constant B 6.3 pKi 500 nM Ki Bioorg Med Chem (2022) 72: 116970-116970 [PMID:36063653]
ChEMBL Inhibition of Sprague-Dawley rat liver arginase 1 B 4.3 pIC50 50000 nM IC50 Bioorg Med Chem (2022) 72: 116970-116970 [PMID:36063653]
ChEMBL Inhibition of rat liver arginase B 5.7 pIC50 2000 nM IC50 Eur J Med Chem (2014) 76: 132-144 [PMID:24583353]
ChEMBL Inhibition of rat Arg1 at pH 7.4 B 6.1 pIC50 800 nM IC50 Bioorg Med Chem (2020) 28: 115658-115658 [PMID:32828425]
ChEMBL Inhibition of rat ARG1 B 6.1 pIC50 800 nM IC50 Eur J Med Chem (2021) 218: 113356-113356 [PMID:33773287]
Arginase II/Arginase-2, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795148] [GtoPdb: 1245] [UniProtKB: P78540]
ChEMBL Inhibition of arginase 2 (unknown origin) B 7.29 pKi 51 nM Ki Bioorg Med Chem Lett (2018) 28: 319-329 [PMID:29326017]
ChEMBL Inhibition of human Arg2 at pH 7.5 B 7.29 pKi 51 nM Ki Bioorg Med Chem (2020) 28: 115658-115658 [PMID:32828425]
ChEMBL Binding affinity to human ARG2 assessed as inhibition constant B 7.29 pIC50 51 nM IC50 Eur J Med Chem (2021) 218: 113356-113356 [PMID:33773287]

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]