vinorelbine [Ligand Id: 7105] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL553025 (Navelbin, NSC-760087, Vinorelbine, Vinorelbine Base)
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684]
ChEMBL DRUGMATRIX: CYP450, 3A4 enzyme inhibition (substrate: 7-Benzyloxy-4-(trifluoromethyl)-coumarin) B 6 pIC50 1000 nM IC50 DrugMatrix in vitro pharmacology data
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 6.27 pKi 535.55 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.79 pIC50 1606.2 nM IC50 DrugMatrix in vitro pharmacology data
tubulin beta class I/tubulin alpha 4a/tubulin beta 4B class IVb/tubulin beta 3 class III/tubulin beta 8 class VIII/tubulin alpha 1a/Tubulin in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095182] [GtoPdb: 264026392641275227532638] [UniProtKB: P04350P07437P0DPH7P68363P68366P68371Q13509Q13885Q3ZCM7Q6PEY2Q71U36Q9BQE3Q9BUF5Q9BVA1Q9H4B7]
ChEMBL Inhibition of brain tubulin (unknown origin) polymerization measured up to 15 to 30 mins B 5.7 pIC50 2000 nM IC50 J Med Chem (2015) 58: 6678-6696 [PMID:26226379]
ChEMBL Inhibition of tubulin (unknown origin) polymerization B 6.15 pIC50 700 nM IC50 Bioorg Med Chem Lett (2015) 25: 1771-1773 [PMID:25804719]

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]