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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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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]