ChEMBL ligand: CHEMBL744 (BHV-0223, Exservan, NSC-753433, NSC-759823, Rilutek, Riluzol, Riluzole, Riluzole zentiva, RP 54274, RP-54274, Teglutik, Tiglutik, Tiglutik kit)
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] There should be some charts here, you may need to enable JavaScript!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
Pteridine reductase 1 in Leishmania major [ChEMBL: CHEMBL6194] [UniProtKB: Q01782] There should be some charts here, you may need to enable JavaScript!
Nav1.2/Sodium channel protein type II alpha subunit in Human [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250] Nav1.2/Sodium channel protein type II alpha subunit in Rat [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775] There should be some charts here, you may need to enable JavaScript!
Nav1.4/Sodium channel protein type IV alpha subunit in Human [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499] There should be some charts here, you may need to enable JavaScript!
Nav1.7/Sodium channel protein type IX alpha subunit in Human [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858] There should be some charts here, you may need to enable JavaScript!
KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952] There should be some charts here, you may need to enable JavaScript!
KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604] There should be some charts here, you may need to enable JavaScript!
KCa2.3 in Human [GtoPdb: 383] [UniProtKB: Q9UGI6] There should be some charts here, you may need to enable JavaScript!
KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554] There should be some charts here, you may need to enable JavaScript!
TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] There should be some charts here, you may need to enable JavaScript!
Kv4.2 in Rat [GtoPdb: 553] [UniProtKB: Q63881] There should be some charts here, you may need to enable JavaScript!
Kv4.3 in Rat [GtoPdb: 554] [UniProtKB: Q62897] 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]
GtoPdb	Inhibition of currents via human Kv11.1 (hERG) channels expressed in HEK293 cells in whole-cell patch-clamp experiments.	-	4.3	pIC50	50000	nM	IC50	Mol Pharmacol (2009) 75: 281-95 [PMID:18955585]
ChEMBL	Displacement of Tracer Red from human ERG by fluorescence polarization assay	B	4.6	pIC50	>25000	nM	IC50	J Med Chem (2019) 62: 3989-4012 [PMID:30908048]
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.76	pKi	1718	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.76	pIC50	1733	nM	IC50	DrugMatrix in vitro pharmacology data
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	5.1	pIC50	7943.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
Pteridine reductase 1 in Leishmania major (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6194] [UniProtKB: Q01782]
ChEMBL	Inhibition of Leishmania major PTR1 by Lineweaver-Burk analysis	B	5.4	pKi	4000	nM	Ki	J Med Chem (2011) 54: 211-221 [PMID:21126022]
ChEMBL	Inhibition of Leishmania major pteridine reductase 1 using di-hydrobiopterine as substrate in presence of NADPH	B	4.03	pIC50	94100	nM	IC50	J Med Chem (2019) 62: 3989-4012 [PMID:30908048]
ChEMBL	Inhibition of Leishmania major PTR1	B	4.3	pIC50	50000	nM	IC50	J Med Chem (2011) 54: 211-221 [PMID:21126022]
Nav1.2/Sodium channel protein type II alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4187] [GtoPdb: 579] [UniProtKB: Q99250]
ChEMBL	Blockade of synaptosomal sodium channels, inhibition of [14C]guanidinium ion flux into CHO cells expressing Type II sodium channel	F	5.66	pIC50	2200	nM	IC50	Bioorg Med Chem Lett (1995) 5: 2259-2262
Nav1.2/Sodium channel protein type II alpha subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399] [GtoPdb: 579] [UniProtKB: P04775]
ChEMBL	Sodium channel block, determined by % block of [14C]guanidinium flux in CHO line expressing rat type IIA sodium channels derived from rat brain	F	5.33	pIC50	4730	nM	IC50	J Med Chem (1998) 41: 3298-3302 [PMID:9703475]
Nav1.4/Sodium channel protein type IV alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2072] [GtoPdb: 581] [UniProtKB: P35499]
ChEMBL	Inhibition of human Nav 1.4 expressed in HEK293T cells assessed as tonic block at 0.1 Hz by whole cell patch clamp assay	B	4.2	pIC50	63000	nM	IC50	ACS Med Chem Lett (2023) 14: 999-1008 [PMID:37465302]
ChEMBL	Inhibition of human Nav 1.4 expressed in HEK293T cells assessed as phasic block at 10 Hz by whole cell patch clamp assay	B	4.29	pIC50	51000	nM	IC50	ACS Med Chem Lett (2023) 14: 999-1008 [PMID:37465302]
Nav1.7/Sodium channel protein type IX alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4296] [GtoPdb: 584] [UniProtKB: Q15858]
ChEMBL	Inhibition of human Nav 1.7 expressed in HEK293T cells assessed as tonic block at 0.1 Hz by whole cell patch clamp assay	B	4.25	pIC50	56000	nM	IC50	ACS Med Chem Lett (2023) 14: 999-1008 [PMID:37465302]
ChEMBL	Inhibition of human Nav 1.7 expressed in HEK293T cells assessed as phasic block at 10 Hz by whole cell patch clamp assay	B	4.39	pIC50	41000	nM	IC50	ACS Med Chem Lett (2023) 14: 999-1008 [PMID:37465302]
KCa2.1 in Human [GtoPdb: 381] [UniProtKB: Q92952]
GtoPdb	-	-	4.68	pEC50	21000	nM	EC50	Mol Pharmacol (2009) 75: 281-95 [PMID:18955585]
KCa2.2 in Rat [GtoPdb: 382] [UniProtKB: P70604]
GtoPdb	-	-	4.89	pEC50	12800	nM	EC50	Mol Pharmacol (2009) 75: 281-95 [PMID:18955585]
KCa2.3 in Human [GtoPdb: 383] [UniProtKB: Q9UGI6]
GtoPdb	-	-	4.9	pEC50	12500	nM	EC50	Mol Pharmacol (2009) 75: 281-95 [PMID:18955585]
KCa3.1 in Human [GtoPdb: 384] [UniProtKB: O15554]
GtoPdb	-	-	5.7	pIC50	-	-	-	Mol Pharmacol (2009) 75: 281-95 [PMID:18955585]
TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
GtoPdb	-	-	5.04	pEC50	9200	nM	EC50	Br J Pharmacol (2014) 171: 158-70 [PMID:24117252]
Kv4.2 in Rat [GtoPdb: 553] [UniProtKB: Q63881]
GtoPdb	Inhibition of currents via rat Kv4.2 channels expressed in LTK cells in whole-cell patch-clamp experiments.	-	3.89	pIC50	130000	nM	IC50	Mol Pharmacol (2009) 75: 281-95 [PMID:18955585]
Kv4.3 in Rat [GtoPdb: 554] [UniProtKB: Q62897]
GtoPdb	-	-	3.9	pIC50	-	-	-	J Pharmacol Exp Ther (2006) 319: 323-31 [PMID:16815868]

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]