ChEMBL ligand: CHEMBL4530872
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
TRPC4/Short transient receptor potential channel 4 in Human [ChEMBL: CHEMBL4295971] [GtoPdb: 489] [UniProtKB: Q9UBN4] There should be some charts here, you may need to enable JavaScript!
TRPC5/Short transient receptor potential channel 5 in Human [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62] There should be some charts here, you may need to enable JavaScript!
TRPC6/Short transient receptor potential channel 6 in Human [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210] There should be some charts here, you may need to enable JavaScript!
Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524] There should be some charts here, you may need to enable JavaScript!
Transient receptor potential cation channel subfamily C member 5 in Rat [ChEMBL: CHEMBL4523409] [UniProtKB: Q8VD38] 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
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 TRPC5 channel (unknown origin) expressed in HEK293 cells assessed as inhibition of EA-evoked Ca2+ entry by measuring reduction in intracellular Ca2+ level by Fluo-4 dye based FLIPR assay	B	6.68	pIC50	211	nM	IC50	Bioorg Med Chem Lett (2022) 61: 128612-128612 [PMID:35143983]
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]
ChEMBL	Inhibition of human TRPC5 channel expressed in HEK293 cells assessed as inhibition of EA-evoked channel current measured at +80 mV by whole-cell voltage clamp assay	B	7.3	pIC50	50.11	nM	IC50	Bioorg Med Chem Lett (2022) 61: 128612-128612 [PMID:35143983]
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 34:

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]