nitroxoline [Ligand Id: 13964] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1454910 (A-82, Nitrohydroxyquinoline, Nitroxolina, Nitroxoline, NSC-74947) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bromodomain containing 4/Bromodomain-containing protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1163125] [GtoPdb: 1945] [UniProtKB: O60885] | ||||||||
| ChEMBL | Inhibition of BRD4 BD1 (unknown origin) using biotin labelled NeC: SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins by alpha screen assay | B | 6.01 | pIC50 | 980 | nM | IC50 | Eur J Med Chem (2019) 163: 281-294 [PMID:30529546] |
| ChEMBL | Inhibition of BRD4 in human MV4-11 cells using biotin labelled N-C:SGRG-K(Ac)-GG-K(Ac)-GLG-K(Ac)-GGA-K(Ac)-RHRKVGG-K as substrate preincubated for 15 mins followed by substrate addition measured after 5 mins by alpha screen assay | B | 6.01 | pIC50 | 980 | nM | IC50 | Eur J Med Chem (2019) 163: 281-294 [PMID:30529546] |
| Catechol-O-methyltransferase/Catechol O-methyltransferase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2372] [GtoPdb: 2472] [UniProtKB: P22734] | ||||||||
| ChEMBL | Inhibition of Sprague-Dawley rat liver COMT after 10 mins using 0.05 uCi [14CH3]-SAM as substrate | B | 4.7 | pIC50 | 19952.62 | nM | IC50 | J Med Chem (1976) 19: 558-560 [PMID:817025] |
| cathepsin B/Cathepsin B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4072] [GtoPdb: 2343] [UniProtKB: P07858] | ||||||||
| ChEMBL | Mixed inhibition of cathepsin B (unknown origin) endopeptidase activity assessed as inhibition constant for enzyme-substrate-inhibitor complex | B | 4.4 | pKi | 39500 | nM | Ki | J Med Chem (2013) 56: 521-533 [PMID:23252745] |
| ChEMBL | Mixed inhibition of recombinant human cathepsin B endopeptidase activity assessed as inhibitory constant for enzyme-substrate-inhibitor complex using Z-Arg-Arg-AMC as substrate in presence of pH 6 phosphate buffer by fluorescence assay | B | 4.4 | pKi | 39500 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 1239-1247 [PMID:29503024] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2013) 56: 8377-8388 [PMID:24088053] |
| Cystathionine γ-lyase/Cystathionine gamma-lyase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295745] [GtoPdb: 1444] [UniProtKB: P32929] | ||||||||
| ChEMBL | Inhibition of human CSE using H-Cys as the substrate by tandem well based HTS assay | B | 4.97 | pIC50 | 10700 | nM | IC50 | J Med Chem (2019) 62: 1677-1683 [PMID:30562026] |
| ChEMBL | Inhibition of human CSE using L-Cys as the substrate by tandem well based HTS assay | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2019) 62: 1677-1683 [PMID:30562026] |
| ChEMBL | Inhibition of human CSE using H-Cys as the substrate by LC/MS/MS-based assay | B | 5.22 | pIC50 | 6000 | nM | IC50 | J Med Chem (2019) 62: 1677-1683 [PMID:30562026] |
| Methionyl aminopeptidase 1/Methionine aminopeptidase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2474] [GtoPdb: 1572] [UniProtKB: P53582] | ||||||||
| ChEMBL | Inhibition of human methionine aminopeptidase 1 | B | 4.82 | pIC50 | >15000 | nM | IC50 | ACS Med Chem Lett (2013) 4: 699-703 [PMID:24376907] |
| Methionyl aminopeptidase 2/Methionine aminopeptidase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3922] [GtoPdb: 1573] [UniProtKB: P50579] | ||||||||
| ChEMBL | Inhibition of human methionine aminopeptidase 2 | B | 7.26 | pIC50 | 55 | nM | IC50 | ACS Med Chem Lett (2013) 4: 699-703 [PMID:24376907] |
| ChEMBL | Inhibition of recombinant human N-terminal His-tagged MetAP2 expressed in baculovirus infected BTI-TN-5B1-4 insect cells using Met-Pro-pNA as substrate preincubated for 20 mins followed by substrate addition and measured after 30 mins | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (2019) 62: 5025-5039 [PMID:30939017] |
ChEMBL data shown on this page come from version 35:
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]
