MK-7145 [Ligand Id: 10382] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3696475 (Mk-7145) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
| ChEMBL | Inhibition of ACES (unknown origin) | B | 5 | pIC50 | 9940 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| Kir1.1/ATP-sensitive inward rectifier potassium channel 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293292] [GtoPdb: 429] [UniProtKB: P48048] | ||||||||
| ChEMBL | Inhibition of ROMK (unknown origin) after 30 mins by 86Rb+ efflux assay | B | 7.17 | pIC50 | 68 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| ChEMBL | Inhibition of ROMK (unknown origin) expressed in CHO cells after 6 mins by electrophysiological assay | B | 8.05 | pIC50 | 9 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| ChEMBL | Inhibition of human ROMK expressed in CHO cells by whole cell voltage clamp electrophysiology assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2021) 64: 7691-7701 [PMID:34038119] |
| GtoPdb | Measured using a Tl+ flux assay. | - | 8.22 | pIC50 | 6 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| ChEMBL | Inhibition of ROMK (unknown origin) after 30 mins by Tl+ influx assay | B | 8.22 | pIC50 | 6 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| Kir1.1/ATP-sensitive inward rectifier potassium channel 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146350] [GtoPdb: 429] [UniProtKB: P35560] | ||||||||
| ChEMBL | Electrophysiology Assay: Block of Kir 1.1 (ROMKl) 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, CA). Chinese hamster ovary cells stably expressing Kirl.l channels were maintained in T-75 flasks in cell culture media in a humidified 10% CO2 incubator at 37 0C. Prior to an experiment, Kirl .l 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 0C and suspended in 10 ml of bath solution containing (in roM): 150 NaCl, 10 KCl, 2.7 CaCl2, 0.5 MgCl2, 5 HEPES5 pH 7.4. After centrifugation, the cell pellet was resuspended in approximately 4.0 ml of bath solution and placed in the Ion Works instrument. The intracellular solution consisted of (in mM): 80 K gluconate, 40 KCl, 20 KF5 3.2 MgCl2, 3 EGTA, 5 Hepes, pH 7.4. | B | 8.05 | pIC50 | 9 | nM | IC50 | US-9018211-B2. Inhibitors of the renal outer medullary potassium channel (2015) |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Displacement of [35S]MK-499 from human ERG | B | 4.64 | pIC50 | 23000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| ChEMBL | Inhibition of human ERG after 6 mins by electrophysiological assay | B | 4.66 | pIC50 | 22000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| GtoPdb | In a hERG electrophysiology assay. | - | 4.66 | pIC50 | 22000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Inhibition of [3H]-serotonin uptake at human SERT transfected in HEK293 cells | B | 5.62 | pIC50 | 2400 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| ChEMBL | Inhibition of human SERT | B | 6.92 | pIC50 | 120 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| 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 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| SST1 receptor/Somatostatin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1917] [GtoPdb: 355] [UniProtKB: P30872] | ||||||||
| ChEMBL | Inhibition of somatostatin receptor subtype 1 (unknown origin) | B | 5.58 | pIC50 | 2630 | nM | IC50 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
| 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 | ACS Med Chem Lett (2016) 7: 697-701 [PMID:27437080] |
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]
