thapsigargin [Ligand Id: 5351] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL96926 (Thapsigargin)
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  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
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  • SERCA1/Sarcoplasmic/endoplasmic reticulum calcium ATPase 1 in Human [ChEMBL: CHEMBL3136] [GtoPdb: 840] [UniProtKB: O14983]
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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 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]