MK-8153 [Ligand Id: 12780] 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: CHEMBL3913475 |
|---|
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!
|
|
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 |
|---|---|---|---|---|---|---|---|---|
| Kir1.1/ATP-sensitive inward rectifier potassium channel 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293292] [GtoPdb: 429] [UniProtKB: P48048] | ||||||||
| ChEMBL | Thallium Flux Assay: The ROMK channel functional thallium flux assay is performed in 384 wells, using the FLIPR-Tetra instrument. HEK-hKir1.1 cells are seeded in Poly-D-Lysine microplates and kept in a 37° C.-10% CO2 incubator overnight. On the day of the experiment, the growth media is replaced with the FluxOR reagent loading buffer and incubated, protected from light, at ambient temperature (23-25° C.) for 90 min. The loading buffer is replaced with assay buffer+/-test compound followed by 30 min incubation at ambient temperature, where the Thallium/Potassium stimulant is added to the microplate.Step Protocol 1. Seed HEK-hKir1.1 cells (50 uA at 20,000 cells/well) in 384-well PDL coated Microplates 2. Allow cells to adhere overnight in humidified 37° C./10% CO2 incubator 3. Completely remove cell growth media from microplate and replace with 25 ul loading buffer 4. Incubate Microplate at room temperature, protected form light, for 90 min. | B | 7.7 | pIC50 | 20 | nM | IC50 | US-9206198-B2. Inhibitors of the renal outer medullary potassium channel (2015) |
| ChEMBL | Electrophysiology Assay: Block of Kir1.1 (ROMK1) currents was examined by whole cell voltage clamp (Hamill et. al. Pfluegers Archives 391:85-100 (1981)) using the IonWorks Quattro automated electrophysiology platform (Molecular Devices, Sunnyvale, Calif.). Chinese hamster ovary cells stably expressing Kir1.1 channels were maintained in T-75 flasks in cell culture media in a humidified 10% CO2 incubator at 37° C. Prior to an experiment, Kir1.1 expression was induced by overnight incubation with 1 mM sodium butyrate. On the day of the experiment, cells were dissociated with 2.5 mL of Versene (Invitrogen 15040-066) for approximately 6 min at 37° C. and suspended in 10 mL of bath solution containing (in mM): 150 NaCl, 10 KCl, 2.7 CaCl2, 0.5 MgCl2, 5 HEPES, pH 7.4. After centrifugation, the cell pellet was resuspended in approximately 4.0 mL of bath solution and placed in the IonWorks instrument. The intracellular solution consisted of (in mM): 80 K gluconate, 40 KCl, 20 KF, 3.2 MgCl2, 3 EGTA, 5 Hepes, pH 7.4. | B | 8 | pIC50 | 10 | nM | IC50 | US-9206198-B2. Inhibitors of the renal outer medullary potassium channel (2015) |
| GtoPdb | hKir1.1 electrophysiology | - | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| ChEMBL | Inhibition of human ROMK expressed in CHO cells by whole cell voltage clamp electrophysiology assay | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| Kir1.1/ATP-sensitive inward rectifier potassium channel 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146350] [GtoPdb: 429] [UniProtKB: P35560] | ||||||||
| ChEMBL | Inhibition of rat Kir1.1 expressed in HEK293 cells by electrophysiology assay | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| Kir4.1/ATP-sensitive inward rectifier potassium channel 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146348] [GtoPdb: 438] [UniProtKB: P78508] | ||||||||
| ChEMBL | Inhibition of Kir4.1 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| CYP2C8/Cytochrome P450 2C8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3721] [GtoPdb: 1325] [UniProtKB: P10632] | ||||||||
| ChEMBL | Inhibition of CYP2C8 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| CYP2C9/Cytochrome P450 2C9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3397] [GtoPdb: 1326] [UniProtKB: P11712] | ||||||||
| ChEMBL | Inhibition of CYP2C9 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
| ChEMBL | Inhibition of CYP2D6 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| CYP3A4/Cytochrome P450 3A4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] | ||||||||
| ChEMBL | Inhibition of CYP3A4 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| Kir7.1/Inward rectifier potassium channel 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146349] [GtoPdb: 443] [UniProtKB: O60928] | ||||||||
| ChEMBL | Inhibition of Kir7.1 (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of Nav1.5 (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936] | ||||||||
| ChEMBL | Inhibition of Cav1.2 (unknown origin) | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
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]
