Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL96926 (Thapsigargin) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 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]