GFB-8438 [Ligand Id: 12527] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4530872 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG stably expressed in HEK293 cells measured at holding potential of -90 mV by manual patch clamp assay | B | 5.06 | pIC50 | 8700 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| TRPC4/Short transient receptor potential channel 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295971] [GtoPdb: 489] [UniProtKB: Q9UBN4] | ||||||||
| ChEMBL | Inhibition of Englerin-activated human TRPC4 channel expressed in HEK293 cells by Q-patch clamp assay | B | 6.54 | pIC50 | 290 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| TRPC5/Short transient receptor potential channel 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | - | - | 6.5 | pIC50 | - | - | - | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| ChEMBL | Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as decrease in current amplitude treated for 3 mins measured between +80 mV and -80 mV by manual patch clamp assay | B | 6.55 | pIC50 | 280 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| ChEMBL | Inhibition of rosiglitazone-activated human TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay | B | 6.74 | pIC50 | 180 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| TRPC6/Short transient receptor potential channel 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210] | ||||||||
| ChEMBL | Inhibition of OAG-activated human TRPC6 channel expressed in HEK293 cells by Q-patch clamp assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| Nav1.5/Sodium channel protein type V alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] | ||||||||
| ChEMBL | Inhibition of human Nav1.5 stably expressed in CHO cells measured at holding potential of -80 mV by manual patch clamp assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
| Transient receptor potential cation channel subfamily C member 5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523409] [UniProtKB: Q8VD38] | ||||||||
| ChEMBL | Inhibition of rosiglitazone-activated rat TRPC5 channel expressed in HEK293 cells assessed as reduction in Ca2+ current measured at +80 mV with holding potential of -60 mV by Q-patch clamp assay | B | 6.74 | pIC50 | 180 | nM | IC50 | ACS Med Chem Lett (2019) 10: 1579-1585 [PMID:31749913] |
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]
