azithromycin [Ligand Id: 6510] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL529 (CP 62993, CP-62993, ZMax, Sumamed, XZ 450, XZ 405, XZ-450, Clamelle, Azasite, Zithromax, Azithromycin, Azithromycin Dihydrate, Azithromycin hydrate, Azyter, Sunamed)
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  • motilin receptor in Human [GtoPdb: 297] [UniProtKB: O43193]
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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 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 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 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]

ChEMBL data shown on this page come from version 26:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]