vinblastine [Ligand Id: 6851] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL159 ([3H]-Vinblastine, NSC-47842, Velban, Vinblastine) |
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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 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]
