SAR296968 [Ligand Id: 13934] activity data from GtoPdb and ChEMBL
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: CHEMBL3662001 |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| Sodium/calcium exchanger 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4076] [GtoPdb: 945] [UniProtKB: P32418] | ||||||||
| ChEMBL | Forward Mode Assay: The assay is based on the monitoring of intracellular Ca2+concentrations using the PBX Calcium Assay Kit from BD (Becton, Dickinson and Company) with calcium indicator dye 51-9000177BKa (BD, 640177), CHO cells expressing NCX1 were loaded with the dye, and after a preincubation period with the test compound, lonomycin (Calbiochem, 407950) was added. Ionomycin is an ionophor for Ca2+ions mediating an increase of intracellular Ca2+ions. Consequently, intracellular Ca2+ions are exchanged against extracellular Na+ions (Ca2+efflux, forward mode). The decrease of intracellular Ca2+ions was detected by measuring the fluorescence of the calcium indicator dye at a wavelength of 520 nm by a FLIPR device.Briefly, similarly as for the reverse mode, for the forward mode transport assay 18000 cells per well were seeded into a 96 well microplate (Corning COSTAR 3904) and incubated overnight in culture medium (cf. above). A total volume of 100 ul medium per well was used. | B | 6.7 | pIC50 | 200 | nM | IC50 | US-8912224-B2. Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals (2014) |
| ChEMBL | Reverse Mode Assay: The assay is based on the monitoring of intracellular Ca2+concentrations using the calcium-sensitive dye Fluo-4. CHO cells expressing NCX1 were loaded with the dye by means of the acetoxymethyl ester Fluo-4 AM (Invitrogen, F14202), which is cleaved intracellularly by esterase activity to yield the charged species of free Fluo-4. After an preincubation period with the test compound, Gramicidine (Sigma, G5002) was added. Gramicidine is an ionophor for Na+ions mediating an increase of intracellular Na+ions. Consequently, intracellular Na+ions are exchanged against extracellular Ca2+ions (Ca2+influx, reverse mode). The intracellular elevation of Ca2+ ions was detected by measuring the fluorescence of Fluo-4 at a wavelength of 520 nm by a FLIPR device.Briefly, for the reverse mode transport assay 18000 cells per well were seeded into a 96 well microplate (Corning COSTAR 3904) and incubated overnight in culture medium (1x Nut Mix F12 (Ham) (Gibco, 21765-029); 10% (v/v) fetal calf serum. | B | 7 | pIC50 | 100 | nM | IC50 | US-8912224-B2. Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals (2014) |
| GtoPdb | - | - | 7.13 | pIC50 | 74 | nM | IC50 | J Pharmacol Exp Ther (2021) 377: 293-304 [PMID:33602875] |
| Sodium/calcium exchanger 2 in Human [GtoPdb: 946] [UniProtKB: Q9UPR5] | ||||||||
| GtoPdb | - | - | 7.64 | pIC50 | 23 | nM | IC50 | J Pharmacol Exp Ther (2021) 377: 293-304 [PMID:33602875] |
| Sodium/calcium exchanger 3 in Human [GtoPdb: 947] [UniProtKB: P57103] | ||||||||
| GtoPdb | - | - | 6.89 | pIC50 | 129 | nM | IC50 | J Pharmacol Exp Ther (2021) 377: 293-304 [PMID:33602875] |
ChEMBL data shown on this page come from version 35:
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]
