vinblastine [Ligand Id: 6851] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL159 ([3H]-Vinblastine, NSC-47842, Velban, Vinblastine)
  • Arachidonate 15-lipoxygenase in Rabbit [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
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  • ABCC2/Canalicular multispecific organic anion transporter 1 in Human [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
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  • ABCC1/Multidrug resistance-associated protein 1 in Human [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530]
ChEMBL DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) B 5.3 pIC50 5037 nM IC50 DrugMatrix in vitro pharmacology data
Beta tubulin in Leishmania donovani (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3186] [UniProtKB: Q25270]
ChEMBL Inhibition of tubulin polymerization interacting at the colchicine binding site. F 6 pIC50 1000 nM IC50 Bioorg Med Chem Lett (2005) 15: 1051-1054 [PMID:15686910]
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL TP_TRANSPORTER: increase in dihydrofluorescein intracellular accumulation (dihydrofluorescein: 1 uM) in SK-E2 cells (expressing BSEP) F 4.21 pIC50 62000 nM IC50 Pharm Res (2003) 20: 537-544 [PMID:12739759]
ABCC2/Canalicular multispecific organic anion transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
ChEMBL TP_TRANSPORTER: inhibition of calcein-AM efflux in MRP2-expressing MDCK cells F 4.68 pIC50 21000 nM IC50 Drug Metab Dispos (2005) 33: 537-546 [PMID:15616150]
Monoamine oxidase B in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2756] [UniProtKB: P56560]
ChEMBL Inhibitory activity against Monoamine oxidase B isolated from beef liver mitochondria was determined B 4.11 pKi 77000 nM Ki J Med Chem (1990) 33: 1845-1848 [PMID:2362262]
ChEMBL Inhibition of bovine liver MAOB B 4.11 pKi 77000 nM Ki J Nat Prod (1992) 55: 269-284 [PMID:1593278]
ABCC1/Multidrug resistance-associated protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3004] [GtoPdb: 779] [UniProtKB: P33527]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.05 uM) in membrane vesicle from MRP1-expressing HeLa cells F 4.52 pIC50 30000 nM IC50 J Biol Chem (1996) 271: 9683-9689 [PMID:8621644]
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: binding in membrane vesicle from CEM/VLB100 cells F 5.52 pKd 3000 nM Kd J Pharmacol Exp Ther (1999) 290: 854-862 [PMID:10411602]
ChEMBL TP_TRANSPORTER: inhibition of Taxol transepithelial transport (basal to apical) in Caco-2 cells F 4.44 pKi 36500 nM Ki Pharm Res (2001) 18: 171-176 [PMID:11405287]
ChEMBL TP_TRANSPORTER: transepithelial transport of digoxin (basal to apical) in Caco-2 cells F 4.82 pKi 15000 nM Ki Pharm Res (2003) 20: 161-168 [PMID:12636153]
ChEMBL TP_TRANSPORTER: inhibition of ATPase activity (Verapamil) in membranes from CEM/VLB100 cells F 5.68 pKi 2100 nM Ki Biochem Pharmacol (1998) 56: 719-727 [PMID:9751076]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 5.89 pKi 1300 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL High affinity constant at binding site of human P-Glycoprotein (P-gp) in two-affinity model B 7 pKi 100 nM Ki J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Concentration required for 50% inhibition at binding site of human P-Glycoprotein (P-gp) in one-affinity model B 4.47 pIC50 34000 nM IC50 J Med Chem (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 4.53 pIC50 29500 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells F 4.54 pIC50 29000 nM IC50 Drug Metab Dispos (2005) 33: 537-546 [PMID:15616150]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 4.7 pIC50 19900 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 4.75 pIC50 17700 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL Inhibition of P-glycoprotein expressed in A2780/ADR cells by calcein AM assay B 4.98 pIC50 10471.29 nM IC50 Bioorg Med Chem (2007) 15: 7470-7479 [PMID:17890094]
ChEMBL Inhibition of P-glycoprotein by Hoechst assay B 5 pIC50 10000 nM IC50 Bioorg Med Chem (2007) 15: 7470-7479 [PMID:17890094]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 5.7 pIC50 2000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-CEM cells F 4.47 pEC50 34000 nM EC50 Anticancer Drugs (1996) 7: 568-578 [PMID:8862725]
ChEMBL TP_TRANSPORTER: increase in Calcein-AM intracellular accumulation (Calcein-AM: 0.25 uM) in MDR-P388 cells F 4.84 pEC50 14600 nM EC50 Anticancer Drugs (1996) 7: 568-578 [PMID:8862725]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.1 pIC50 8000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 5.1 pIC50 8000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.3 pIC50 >50000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay F 8.7 pIC50 2 nM IC50 Antimicrob Agents Chemother (2010) 54: 3597-3604 [PMID:20547797]
Plasmodium yoelii yoelii (target type: ORGANISM) [ChEMBL: CHEMBL612328]
ChEMBL Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs F 5.1 pIC50 7950 nM IC50 Antimicrob Agents Chemother (2008) 52: 1215-1220 [PMID:18212104]
ChEMBL Antimalarial activity against liver stages of Plasmodium yoelii yoelii F 5.1 pIC50 7950 nM IC50 J Med Chem (2012) 55: 995-1012 [PMID:22122518]
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2) B 5.73 pIC50 1870 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: 2640, 2639, 2641, 2752, 2753, 2638] [UniProtKB: P04350, P07437, P0DPH7, P68363, P68366, P68371, Q13509, Q13885, Q3ZCM7, Q6PEY2, Q71U36, Q9BQE3, Q9BUF5, Q9BVA1, Q9H4B7]
ChEMBL Inhibition of tubulin (unknown origin) polymerization B 5.68 pIC50 2100 nM IC50 Bioorg Med Chem Lett (2015) 25: 1771-1773 [PMID:25804719]
ChEMBL Inhibition of tubulin polymerization B 6.52 pIC50 300 nM IC50 J Med Chem (2004) 47: 6299-6310 [PMID:15566300]
ChEMBL The compound tested for the inhibition of tubulin polymerization. F 7.15 pIC50 70 nM IC50 J Med Chem (1991) 34: 1998-2003 [PMID:2066973]
GtoPdb - - 9 pIC50 1 nM IC50
ChEMBL Inhibition of tubulin polymerization B 6.7 pEC50 200 nM EC50 J Med Chem (2005) 48: 7096-7098 [PMID:16279766]
Tubulin beta chain in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3394] [UniProtKB: Q6B856]
ChEMBL Binding constant at colchicine site of bovine brain tubulin B 4 pKi >100000 nM Ki Bioorg Med Chem Lett (2002) 12: 465-469 [PMID:11814821]

ChEMBL data shown on this page come from version 32:

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]