azithromycin [Ligand Id: 6510] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL529 (Anhydrous azithromycin, Aruzilina, Azasite, Aziromycin, Azithrocin, Azithromycin, Azithromycin anhydrous, Azithromycin (as dihydrate), Azithromycin dihydrate, Azithromycin hydrate, Azithromycin, unspecified, Azithromycin, unspecified form, Aziwin, Azyter, Clamelle, CP 62993, CP-62,993, CP-62993, Durasite, Hemomycin, Macrozit, NSC-758625, Sumamed, Sunamed, Trozocina, Xithrone, XZ 405, XZ 450, XZ-450, Zithromac, Zithromax, ZMax, Zythromax) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antimalarial activity after 48 hrs against Plasmodium falciparum GCO3 by [3H]hypoxanthine uptake | F | 4.65 | pIC50 | 22585 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 48 hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake | F | 4.8 | pIC50 | 15742 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7A infected in human A-positive erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 48 hrs by semi-automated microdilution technique | F | 4.94 | pIC50 | 11513 | nM | IC50 | Eur J Med Chem (2012) 49: 365-378 [PMID:22321992] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7A infected in type A rhesus-positive human erythrocytes assessed as [3H]hypoxanthine incorporation after 48 hrs by scintillation counting | F | 4.94 | pIC50 | 11513 | nM | IC50 | J Med Chem (2012) 55: 3216-3227 [PMID:22380766] |
| ChEMBL | Antiplasmodial activity after 48 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity | F | 5.04 | pIC50 | 9040 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 774-777 [PMID:18056275] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 after 48 hrs | F | 5.06 | pIC50 | 8700 | nM | IC50 | J Med Chem (2016) 59: 5587-5603 [PMID:26791529] |
| ChEMBL | Antimalarial activity as 2nd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs by flow cytometry | F | 5.06 | pIC50 | 8670 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 3485-3490 [PMID:17698630] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum FCR 3TC after 48 hrs | F | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (2016) 59: 5587-5603 [PMID:26791529] |
| ChEMBL | Antiplasmodial activity after 72 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity | F | 5.34 | pIC50 | 4570 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 774-777 [PMID:18056275] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum isolates assessed as parasite growth inhibition after 72 hrs by ELISA based histidine-rich protein 2 in vitro drug susceptibility assay | F | 5.37 | pIC50 | 4314.35 | nM | IC50 | Antimicrob Agents Chemother (2009) 53: 4040-4042 [PMID:19596882] |
| ChEMBL | Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake | F | 5.4 | pIC50 | 3971.7 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 48 hrs against Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake | F | 5.46 | pIC50 | 3464 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum W2 infected in human A-positive erythrocytes assessed as inhibition of [3H]-hypoxanthine incorporation after 48 hrs by semi-automated microdilution technique | F | 5.57 | pIC50 | 2680 | nM | IC50 | Eur J Med Chem (2012) 49: 365-378 [PMID:22321992] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 infected in type A rhesus-positive human erythrocytes assessed as [3H]hypoxanthine incorporation after 48 hrs by scintillation counting | F | 5.57 | pIC50 | 2680 | nM | IC50 | J Med Chem (2012) 55: 3216-3227 [PMID:22380766] |
| ChEMBL | Antimalarial activity against mefloquine-resistant Plasmodium falciparum TM91C235 assessed as [3H]hypoxanthine incorporation after 48 hrs | F | 5.58 | pIC50 | 2654 | nM | IC50 | J Med Chem (2012) 55: 1389-1401 [PMID:22148880] |
| ChEMBL | Antimalarial activity against chloroquine/pyrimethamine-resistant Plasmodium falciparum W2 after 48 hrs by [3H]hypoxanthine incorporation assay | F | 5.64 | pIC50 | 2294 | nM | IC50 | J Med Chem (2011) 54: 3595-3605 [PMID:21476508] |
| ChEMBL | Antimalarial activity against chloroquine-,pyrimethamine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by microtiter plate scintillation counting | F | 5.65 | pIC50 | 2241 | nM | IC50 | Bioorg Med Chem (2011) 19: 1692-1701 [PMID:21316974] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 after 48 hrs by [3H]hypoxanthine incorporation assay | F | 5.68 | pIC50 | 2112 | nM | IC50 | J Med Chem (2011) 54: 3595-3605 [PMID:21476508] |
| ChEMBL | Antimalarial activity against multidrug-resistant Plasmodium falciparum TM91C235 assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by microtiter plate scintillation counting | F | 5.69 | pIC50 | 2065 | nM | IC50 | Bioorg Med Chem (2011) 19: 1692-1701 [PMID:21316974] |
| ChEMBL | Antimalarial activity after 96 hrs against azithromycin-resistant Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake | F | 5.71 | pIC50 | 1938.7 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity as 2nd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by flow cytometry | F | 5.84 | pIC50 | 1460 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 3485-3490 [PMID:17698630] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 after 48 hrs by [3H]hypoxanthine incorporation assay | F | 5.98 | pIC50 | 1039 | nM | IC50 | J Med Chem (2011) 54: 3595-3605 [PMID:21476508] |
| ChEMBL | Antimalarial activity against chloroquine-sensitive Plasmodium falciparum D6 assessed as inhibition of [3H]hypoxanthine incorporation after 96 hrs by microtiter plate scintillation counting | F | 5.99 | pIC50 | 1015 | nM | IC50 | Bioorg Med Chem (2011) 19: 1692-1701 [PMID:21316974] |
| ChEMBL | Antiplasmodial activity after 96 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity | F | 6.03 | pIC50 | 940 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 774-777 [PMID:18056275] |
| ChEMBL | Antiplasmodial activity after 120 hrs against Plasmodium falciparum 3D7 as Malstat LDH activity | F | 6.39 | pIC50 | 410 | nM | IC50 | Antimicrob Agents Chemother (2008) 52: 774-777 [PMID:18056275] |
| ChEMBL | Antimalarial activity after 96hrs against Plasmodium falciparum 7G8 by [3H]hypoxanthine uptake | F | 6.64 | pIC50 | 228.1 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum 3BA6 CDY mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 6.71 | pIC50 | 194.2 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum 3BA6 by [3H]hypoxanthine uptake | F | 6.74 | pIC50 | 180.3 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum 3BA6 SND mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 6.8 | pIC50 | 157.9 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3BA6 SDD with CRT and MDR1 mutation after 96 hrs in [3H]hypoxanthine uptake | F | 6.81 | pIC50 | 154.7 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum 7G8 C1 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 6.85 | pIC50 | 141.8 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 T76K1 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 6.91 | pIC50 | 121.8 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum 7G8 T76K1 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 6.94 | pIC50 | 114.8 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 by [3H]hypoxanthine uptake | F | 6.99 | pIC50 | 103.4 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum Dd2 C1 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.02 | pIC50 | 95.7 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 C6 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.12 | pIC50 | 76.7 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 CDY mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.15 | pIC50 | 70.2 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 C4 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.18 | pIC50 | 66.7 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 SDD mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.2 | pIC50 | 63.3 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity against Plasmodium falciparum 3D7 after 96 hrs | F | 7.28 | pIC50 | 53 | nM | IC50 | J Med Chem (2016) 59: 5587-5603 [PMID:26791529] |
| ChEMBL | Antimalarial activity as 3rd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs dose then 48 hrs drug-free | F | 7.28 | pIC50 | 52.7 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 3485-3490 [PMID:17698630] |
| ChEMBL | Antimalarial activity after 96hrs against Plasmodium falciparum GCO3 C2 mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.32 | pIC50 | 48 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 SND mutant CRT/MDR1 by [3H]hypoxanthine uptake | F | 7.32 | pIC50 | 47.8 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity after 96 hrs against Plasmodium falciparum GCO3 by [3H]hypoxanthine uptake | F | 7.36 | pIC50 | 43.3 | nM | IC50 | J Biol Chem (2007) 282: 2494-2504 [PMID:17110371] |
| ChEMBL | Antimalarial activity as 3rd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs dose then 48 hrs drug-free | F | 7.51 | pIC50 | 31 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 3485-3490 [PMID:17698630] |
| motilin receptor in Human [GtoPdb: 297] [UniProtKB: O43193] | ||||||||
| GtoPdb | - | - | 5.5 | pEC50 | - | - | - | Br J Pharmacol (2013) 168: 1859-67 [PMID:23190027] |
| TAS2R4 in Human [GtoPdb: 661] [UniProtKB: Q9NYW5] | ||||||||
| GtoPdb | - | - | 4.13 | pEC50 | 74450 | nM | EC50 | FASEB J (2019) 33: 501-517 [PMID:30011231] |
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]
