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 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]
