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ChEMBL ligand: CHEMBL96926 (Thapsigargin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone2 bearing P-type ATPase4 T418N and P990R mutations after 72 hrs by SYBR green based fluorescence assay | F | 5.96 | pIC50 | 1109 | nM | IC50 | Science (2010) 329: 1175-1180 [PMID:20813948] |
ChEMBL | Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone3 bearing P-type ATPase4 D1247Y mutations after 72 hrs by SYBR green based fluorescence assay | F | 5.98 | pIC50 | 1049 | nM | IC50 | Science (2010) 329: 1175-1180 [PMID:20813948] |
ChEMBL | Antimalarial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green based fluorescence assay | F | 6.04 | pIC50 | 905 | nM | IC50 | Science (2010) 329: 1175-1180 [PMID:20813948] |
ChEMBL | Antimalarial activity against NITD609-resistant Plasmodium falciparum Dd2 Clone1 bearing P-type ATPase4 I398F and P990R mutations after 72 hrs by SYBR green based fluorescence assay | F | 6.09 | pIC50 | 813 | nM | IC50 | Science (2010) 329: 1175-1180 [PMID:20813948] |
Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4693] [UniProtKB: P04191] | ||||||||
ChEMBL | Binding affinity to SERCA1a in sarcoplasmic reticulum vesicles of rabbit skeletal muscle after 2.5 to 6 mins by spectrophotometric analysis | B | 9.7 | pKd | 0.2 | nM | Kd | J Med Chem (2013) 56: 3609-3619 [PMID:23574308] |
ChEMBL | Binding affinity to rabbit skeletal muscle SERCA1a preincubated for 5 mins followed by Mg-ATP addition measured over 6 mins by spectrophotometric analysis | B | 9.7 | pKd | 0.2 | nM | Kd | J Nat Prod (2015) 78: 1262-1270 [PMID:25993619] |
ChEMBL | Inhibition of rabbit skeletal muscle SERCA1 assessed as reduction in calcium uptake preincubated for 10 mins followed by ATP addition and measured after 4 mins by scintillation liquid method | B | 8.41 | pIC50 | 3.9 | nM | IC50 | J Med Chem (2020) 63: 15410-15448 [PMID:33289552] |
ChEMBL | Inhibition of rabbit sarcoplasmic reticulum calcium ATPase by ATP regeneration assay | B | 9.7 | pIC50 | 0.2 | nM | IC50 | Bioorg Med Chem (2010) 18: 5634-5646 [PMID:20615710] |
SERCA1/Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3136] [GtoPdb: 840] [UniProtKB: O14983] | ||||||||
ChEMBL | Inhibition of SERCA1a (unknown origin) ATPase activity | B | 10 | pKi | 0.1 | nM | Ki | Bioorg Med Chem Lett (2018) 28: 298-301 [PMID:29292225] |
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]