puromycin [Ligand Id: 13311] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL469912 (3123-L, 3123L, CL 13,900, CL-13900, GNF-PF-2016, P-638, Puromicina, Puromycin, Puromycine, TCMDC-123493)
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  • Puromycin-sensitive aminopeptidase in Human [ChEMBL: CHEMBL2264] [GtoPdb: 1575] [UniProtKB: P55786]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Aminopeptidase N in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1907] [GtoPdb: 1560] [UniProtKB: P15144]
ChEMBL Inhibition of recombinant human C-terminal His10-tagged APN (Lys69 to Lys967 residues) using Ala-AMC as substrate measured for 30 mins by fluorescence assay B 4.39 pIC50 41000 nM IC50 Eur J Med Chem (2017) 139: 325-336 [PMID:28803047]
Aminopeptidase N in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2590] [UniProtKB: P15145]
ChEMBL Inhibition of porcine aminopeptidase-N using Leu-pNA as substrate after 30 mins B 4 pIC50 >100000 nM IC50 Eur J Med Chem (2015) 106: 26-33 [PMID:26513642]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 infected HEK293 cells by DAPI-staining based assay F 6.39 pIC50 410 nM IC50 J Med Chem (2019) 62: 2485-2498 [PMID:30715882]
ChEMBL Antigametocytocidal activity against Plasmodium falciparum NF54-pfs16-GPF late (4 to 6) gametocyte assessed as viability after 72 hrs by MitoTracker Red CM-H2XRos/micro-plate confocal imaging system F 6.71 pIC50 194 nM IC50 Bioorg Med Chem Lett (2015) 25: 327-332 [PMID:25488841]
ChEMBL Antigametocytocidal activity against Plasmodium falciparum NF54-pfs16-GPF early (1 to 3) gametocyte assessed as viability after 72 hrs by MitoTracker Red CM-H2XRos/micro-plate confocal imaging system F 6.76 pIC50 175 nM IC50 Bioorg Med Chem Lett (2015) 25: 327-332 [PMID:25488841]
ChEMBL Antimalarial activity against synchronous ring stage of Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis F 6.83 pIC50 148.9 nM IC50 Eur J Med Chem (2021) 221: 113518-113518 [PMID:34058708]
ChEMBL Antimalarial activity against early (1 to 3) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 6.86 pIC50 137 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against synchronous ring stage of Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by Griffith assay based fluorescence analysis F 6.94 pIC50 114.4 nM IC50 Eur J Med Chem (2021) 221: 113518-113518 [PMID:34058708]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based confocal imaging analysis F 6.96 pIC50 110.8 nM IC50 J Med Chem (2019) 62: 622-640 [PMID:30537832]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 ring stage incubated for 72 hrs by DAPI-staining based imaging analysis F 6.96 pIC50 110 nM IC50 J Nat Prod (2020) 83: 3435-3444 [PMID:33105995]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by DAPI staining-based confocal imaging analysis F 6.97 pIC50 106.6 nM IC50 J Med Chem (2019) 62: 622-640 [PMID:30537832]
ChEMBL Antiplasmodial activity against ring stage drug-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth incubated for 72 hrs by DAPI staining based assay F 7.04 pIC50 91 nM IC50 J Nat Prod (2023) 86: 2171-2184 [PMID:37610242]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as reduction in parasite replication incubated for 62 hrs F 7.05 pIC50 89 nM IC50 J Nat Prod (2012) 75: 1206-1209 [PMID:22680914]
ChEMBL Antimalarial activity against multidrug resistant Plasmodium falciparum Dd2 assessed as parasite growth inhibition incubated for 72 hrs by DAPI staining method F 7.09 pIC50 81.4 nM IC50 J Nat Prod (2023) 86: 557-565 [PMID:36799121]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 incubated for 72 hrs by DAPI staining based analysis F 7.1 pIC50 80 nM IC50 J Nat Prod (2023) 86: 1317-1334 [PMID:37171174]
ChEMBL Antiplasmodial activity against drug-resistant Plasmodium falciparum Dd2 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 7.13 pIC50 74.7 nM IC50 J Nat Prod (2019) 82: 1019-1023 [PMID:30865443]
ChEMBL Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage forms assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 7.15 pIC50 70.2 nM IC50 J Nat Prod (2019) 82: 1019-1023 [PMID:30865443]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 ring stage incubated for 72 hrs by DAPI-staining based imaging analysis F 7.17 pIC50 68 nM IC50 J Nat Prod (2020) 83: 3435-3444 [PMID:33105995]
ChEMBL Antimalarial activity against asexual stage of Plasmodium falciparum 3D7 after 72 hrs by image-based HTS assay F 7.19 pIC50 64 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 incubated for 72 hours by DAPI-staining based confocal imaging analysis F 7.21 pIC50 62 nM IC50 Bioorg Med Chem Lett (2016) 26: 3326-3329 [PMID:27212070]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 measured after 72 hrs by DAPI staining based high throughput screening assay F 7.21 pIC50 62 nM IC50 Bioorg Med Chem Lett (2017) 27: 2602-2607 [PMID:28400231]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 measured after 72 hrs by DAPI staining based high throughput screening assay F 7.21 pIC50 61 nM IC50 Bioorg Med Chem Lett (2017) 27: 2602-2607 [PMID:28400231]
ChEMBL Antiplasmodial activity against 4-aminoquinoline/antifolates-resistant Plasmodium falciparum Dd2 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method F 7.21 pIC50 61 nM IC50 J Nat Prod (2018) 81: 1588-1597 [PMID:29969262]
ChEMBL Antiplasmodial activity against drug-sensitive Plasmodium falciparum 3D7 ring stage infected in human erythrocytes after 72 hrs by DAPI staining based method F 7.22 pIC50 60 nM IC50 J Nat Prod (2018) 81: 1588-1597 [PMID:29969262]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 incubated for 72 hours by DAPI-staining based confocal imaging analysis F 7.22 pIC50 60 nM IC50 Bioorg Med Chem Lett (2016) 26: 3326-3329 [PMID:27212070]
ChEMBL Antimalarial activity against Plasmodium falciparum 3D7 after 72 hrs by DAPI staining-based fluorescence microscopic analysis F 7.27 pIC50 53.2 nM IC50 Bioorg Med Chem Lett (2017) 27: 4091-4095 [PMID:28774427]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based confocal microplate imaging method F 7.28 pIC50 53 nM IC50 J Nat Prod (2017) 80: 3211-3217 [PMID:29236492]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by DAPI staining based fluorescence assay F 7.28 pIC50 53 nM IC50 J Nat Prod (2018) 81: 1079-1083 [PMID:29533611]
ChEMBL Antimalarial activity against late (4 to 5) gametocytic stage of Plasmodium falciparum after 72 hrs by image-based HTS assay F 7.34 pIC50 46 nM IC50 J Med Chem (2013) 56: 7727-7740 [PMID:23927763]
ChEMBL Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 7.34 pIC50 45.2 nM IC50 J Nat Prod (2015) 78: 2932-2939 [PMID:26651537]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 assessed as reduction in parasite growth incubated for 72 hrs by DAPI staining based fluorescence assay F 7.35 pIC50 45 nM IC50 J Nat Prod (2020) 83: 316-322 [PMID:32067457]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method F 7.35 pIC50 45 nM IC50 J Nat Prod (2017) 80: 114-125 [PMID:28001067]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based fluorescence assay F 7.36 pIC50 44 nM IC50 J Nat Prod (2018) 81: 1079-1083 [PMID:29533611]
ChEMBL Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by DAPI staining-based fluorescence microscopic analysis F 7.36 pIC50 43.8 nM IC50 Bioorg Med Chem Lett (2017) 27: 4091-4095 [PMID:28774427]
ChEMBL Antimalarial activity against chloroquine sensitive Plasmodium falciparum 3D7 assessed as parasite growth inhibition incubated for 72 hrs by DAPI staining method F 7.37 pIC50 42.9 nM IC50 J Nat Prod (2023) 86: 557-565 [PMID:36799121]
ChEMBL Antimalarial activity against Plasmodium falciparum W2 assessed as inhibition of parasite growth F 7.38 pIC50 42 nM IC50 Bioorg Med Chem (2015) 23: 5120-5130 [PMID:25913864]
ChEMBL Antiplasmodial activity against choloroquine-sensitive ring stage of Plasmodium falciparum 3D7 assessed as inhibition of parasite growth measured after 72 hrs by DAPI staining based analysis F 7.48 pIC50 33 nM IC50 J Nat Prod (2024) 87: 849-854 [PMID:38416027]
ChEMBL Antimalarial activity against chloroquine-resistant Plasmodium falciparum Dd2 after 72 hrs by DAPI staining based confocal microplate imaging method F 7.49 pIC50 32 nM IC50 J Nat Prod (2017) 80: 3211-3217 [PMID:29236492]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 infected in human RBC after 72 hrs by DAPI staining based confocal microscopic method F 7.64 pIC50 23 nM IC50 J Nat Prod (2017) 80: 114-125 [PMID:28001067]
ChEMBL Antimalarial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as reduction in parasite rowth incubated for 72 hrs by DAPI staining based fluorescence assay F 7.64 pIC50 23 nM IC50 J Nat Prod (2020) 83: 316-322 [PMID:32067457]
ChEMBL Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth after 72 hrs by DAPI staining-based confocal microscopic analysis F 7.64 pIC50 22.7 nM IC50 J Nat Prod (2015) 78: 2932-2939 [PMID:26651537]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay F 6.21 pEC50 611 nM EC50 Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay F 6.48 pEC50 328 nM EC50 Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783]
Plasmodium vivax (target type: ORGANISM) [ChEMBL: CHEMBL613013]
ChEMBL Antimalarial activity against liver stage Plasmodium vivax schizont infected in human hepatocytes preincubated for 5 to 10 days followed by compound addition and measured after 12 days post infection by immunofluorescence staining based assay F 5.64 pEC50 2290.87 nM EC50 J Nat Prod (2024) 87: 315-321 [PMID:38262446]
ChEMBL Antimalarial activity against liver stage Plasmodium vivax schizont infected in human hepatocytes preincubated for 5 to 10 days followed by compound addition and measured after 12 days post infection by immunofluorescence staining based assay F 5.64 pEC50 2290 nM EC50 J Nat Prod (2024) 87: 315-321 [PMID:38262446]
ChEMBL Antimalarial activity against liver stage Plasmodium vivax hypnozoite infected in human hepatocytes preincubated for 5 to 10 days followed by compound addition and measured after 12 days post infection by immunofluorescence staining based assay F 6.11 pEC50 776.25 nM EC50 J Nat Prod (2024) 87: 315-321 [PMID:38262446]
ChEMBL Antimalarial activity against liver stage Plasmodium vivax hypnozoite infected in human hepatocytes preincubated for 5 to 10 days followed by compound addition and measured after 12 days post infection by immunofluorescence staining based assay F 6.11 pEC50 776 nM EC50 J Nat Prod (2024) 87: 315-321 [PMID:38262446]
Puromycin-sensitive aminopeptidase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2264] [GtoPdb: 1575] [UniProtKB: P55786]
ChEMBL Inhibition of recombinant human N-terminal His6-MBP-tagged PSA expressed in Escherichia coli BL21 STAR (DE3) using 4-Ala-MNA as substrate measured for 30 mins by thefluorescence assay B 5.01 pIC50 9700 nM IC50 Eur J Med Chem (2017) 139: 325-336 [PMID:28803047]
GtoPdb - - 5.61 pIC50 2450 nM IC50 Eur J Med Chem (2015) 106: 26-33 [PMID:26513642]
ChEMBL Inhibition of recombinant human puromycin sensitive aminopeptidase using Leu-pNA as substrate after 30 mins B 5.61 pIC50 2450 nM IC50 Eur J Med Chem (2015) 106: 26-33 [PMID:26513642]

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]