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: CHEMBL122413 (SB-366791) |
---|
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!
|
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 |
---|---|---|---|---|---|---|---|---|
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
ChEMBL | Inhibition of rat brain FAAH assessed as hydrolysis of [14C]AEA to [14C]Ethanolamine incubated for 30 mins by scintillation counting method | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1401-1405 [PMID:26850005] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | 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 | pIC50 | 10000 | 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 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
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 W2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
TRPM1/Transient receptor potential cation channel subfamily M member 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879460] [GtoPdb: 493] [UniProtKB: Q2TV84] | ||||||||
ChEMBL | Inhibition of mouse TRPM1 expressed in HEK293T cells assessed as blocked of capsaicin-activated current at 10 uM by whole cell patch clamp electrophysiology relative to control | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2021) 64: 3976-3996 [PMID:33784097] |
TRPM8/Transient receptor potential cation channel subfamily M member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075319] [GtoPdb: 500] [UniProtKB: Q7Z2W7] | ||||||||
ChEMBL | Inhibition of human TRPM8 expressed in HEK293T cells assessed as blocked of menthol-activated current by whole cell patch clamp electrophysiology relative to control | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 3976-3996 [PMID:33784097] |
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
ChEMBL | Antagonist activity at recombinant human TRPV1 channel expressed in CHO cells assessed as inhibition of capsiacin-induced Ca2+ flux by Fluo-3 dye based FLIPR assay | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1401-1405 [PMID:26850005] |
ChEMBL | Antagonist activity at recombinant human TRPV1 channel expressed in HEK293 cells assessed as inhibition of capsiacin-induced Ca2+ flux preincubated for 5 mins followed by capsiacin challenge by Fluo-4-AM dye based spectrofluorimetry | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1401-1405 [PMID:26850005] |
GtoPdb | - | - | 8.24 | pIC50 | 5.7 | nM | IC50 | Neuropharmacology (2004) 46: 133-49 [PMID:14654105] |
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]