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 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]
