propafenone [Ligand Id: 2561] 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: CHEMBL631 (Propafenone, Rythmol, GNF-Pf-4594)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
  • This target only has 1 pki data point
  • 5.6
1 CHEMBL631_lig_chart_1 Alpha-1a adrenergic receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
  • This target only has 1 pki data point
  • 5.85
2 CHEMBL631_lig_chart_2 Alpha-1b adrenergic receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • 6.69
3 CHEMBL631_lig_chart_3 Beta-1 adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • 7.44
4 CHEMBL631_lig_chart_4 Beta-2 adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
  • This target only has 1 pki data point
  • 6.5
5 CHEMBL631_lig_chart_5 Beta-3 adrenergic receptor Human
There should be some charts here, you may need to enable JavaScript!
  • CYP1A2/Cytochrome P450 1A2 in Human [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
  • This target only has 0 pki data point
  • 0
6 CHEMBL631_lig_chart_6 Cytochrome P450 1A2 Human
There should be some charts here, you may need to enable JavaScript!
  • CYP2D6/Cytochrome P450 2D6 in Human [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
  • This target only has 0 pki data point
  • 0
7 CHEMBL631_lig_chart_7 Cytochrome P450 2D6 Human
There should be some charts here, you may need to enable JavaScript!
  • DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
  • This target only has 1 pki data point
  • 5.83
8 CHEMBL631_lig_chart_8 Dopamine transporter Human
There should be some charts here, you may need to enable JavaScript!
  • Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
  • This target only has 0 pki data point
  • 0
9 CHEMBL631_lig_chart_9 HERG Human
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
  • This target only has 1 pki data point
  • 5.52
10 CHEMBL631_lig_chart_10 Norepinephrine transporter Human
There should be some charts here, you may need to enable JavaScript!
  • ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
  • This target only has 1 pki data point
  • 5.38
11 CHEMBL631_lig_chart_11 P-glycoprotein 1 Human
There should be some charts here, you may need to enable JavaScript!
  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
12 CHEMBL631_lig_chart_12 Plasmodium falciparum Plasmodium falciparum
There should be some charts here, you may need to enable JavaScript!
  • Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 [ChEMBL: CHEMBL612856]
  • This target only has 0 pki data point
  • 0
13 CHEMBL631_lig_chart_13 Plasmodium falciparum (isolate K1 / Thailand) Plasmodium falciparum K1
There should be some charts here, you may need to enable JavaScript!
  • K2P2.1/Potassium channel subfamily K member 2 in Human [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
  • This target only has 0 pki data point
  • 0
14 CHEMBL631_lig_chart_14 Potassium channel subfamily K member 2 Human
There should be some charts here, you may need to enable JavaScript!
  • K2P3.1/Potassium channel subfamily K member 3 in Human [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
  • This target only has 0 pki data point
  • 0
15 CHEMBL631_lig_chart_15 Potassium channel subfamily K member 3 Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • This target only has 1 pki data point
  • 6.03
16 CHEMBL631_lig_chart_16 Serotonin 1a (5-HT1a) receptor Rat
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
  • 6.73
17 CHEMBL631_lig_chart_17 Serotonin 2a (5-HT2a) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
  • 7.24
18 CHEMBL631_lig_chart_18 Serotonin 2b (5-HT2b) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
  • 6.7
19 CHEMBL631_lig_chart_19 Serotonin 2c (5-HT2c) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • This target only has 1 pki data point
  • 6.06
20 CHEMBL631_lig_chart_20 Serotonin 6 (5-HT6) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • This target only has 1 pki data point
  • 5.96
21 CHEMBL631_lig_chart_21 Sigma opioid receptor Human
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]
  • This target only has 0 pki data point
  • 0
22 CHEMBL631_lig_chart_22 Sodium channel protein type V alpha subunit Human
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 1/Solute carrier family 22 member 1 in Human [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
  • This target only has 0 pki data point
  • 0
23 CHEMBL631_lig_chart_23 Solute carrier family 22 member 1 Human
There should be some charts here, you may need to enable JavaScript!
  • ABCC9/Kir6.2/Sulfonylurea receptor 2, Kir6.2 in Human [ChEMBL: CHEMBL2095198] [GtoPdb: 2746442] [UniProtKB: O60706Q14654]
  • This target only has 0 pki data point
  • 0
24 CHEMBL631_lig_chart_24 Sulfonylurea receptor 2, Kir6.2 Human
There should be some charts here, you may need to enable JavaScript!
  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
  • This target only has 0 pki data point
  • 0
25 CHEMBL631_lig_chart_25 Voltage-dependent L-type calcium channel subunit alpha-1C Guinea pig
There should be some charts here, you may need to enable JavaScript!
  • Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
  • This target only has 0 pki data point
  • 0
26 CHEMBL631_lig_chart_26 Kv1.5 Human
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
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140]
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.6 pKi 2488 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin) B 5.21 pIC50 6147 nM IC50 DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.85 pKi 1416 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.59 pIC50 2558 nM IC50 DrugMatrix in vitro pharmacology data
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.69 pKi 205 nM Ki DrugMatrix in vitro pharmacology data
GtoPdb - - 6.7 pKi 205 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) B 6.45 pIC50 354 nM IC50 DrugMatrix in vitro pharmacology data
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
GtoPdb - - 7.44 pKi 36 nM Ki National Toxicology Program: Dept of Health and Human Services.. DrugMatrix
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.44 pKi 36 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) B 7.28 pIC50 52 nM IC50 DrugMatrix in vitro pharmacology data
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 6.5 pKi 318 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) B 6.37 pIC50 424 nM IC50 DrugMatrix in vitro pharmacology data
CYP1A2/Cytochrome P450 1A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3356] [GtoPdb: 1319] [UniProtKB: P05177]
ChEMBL DRUGMATRIX: CYP450, 1A2 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.48 pIC50 3292 nM IC50 DrugMatrix in vitro pharmacology data
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635]
ChEMBL DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) B 5.34 pIC50 4603.4 nM IC50 DrugMatrix in vitro pharmacology data
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.83 pKi 1484 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.73 pIC50 1868 nM IC50 DrugMatrix in vitro pharmacology data
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Inhibition of human cloned ERG channel expressed in chinese hamster CHO cells after 5 mins by patch clamp assay B 5.54 pIC50 2880 nM IC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
ChEMBL Inhibitory concentration against IKr potassium channel B 6.1 pIC50 800 nM IC50 Bioorg. Med. Chem. Lett. (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of hERG K channel F 6.36 pIC50 440 nM IC50 Cardiovasc. Res. (2011) 91: 53-61 [PMID:21300721]
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 5.52 pKi 2991 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.52 pIC50 3016 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model B 5.38 pKi 4200 nM Ki J. Med. Chem. (2002) 45: 5671-5686 [PMID:12477351]
ChEMBL Inhibition of P-glycoprotein-mediated daunorubicin efflux from human CCRF-CEM/VCR1000 cells after 240 secs by FACS flow cytometric analysis B 6.48 pIC50 331.13 nM IC50 J. Med. Chem. (2012) 55: 3261-3273 [PMID:22452412]
ChEMBL SUPPLEMENTARY: Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay. Same assay as CHEMBL914418 B 6.48 pEC50 331.13 nM EC50 Structure-activity data for a series of P-glycoprotein inhibitors (Supplementary Data to CHEMBL1142990)
ChEMBL Inhibition of P-glycoprotein expressed in MDR CCRF vcr1000 cells by daunorubicin efflux assay B 6.48 pEC50 329 nM EC50 J. Med. Chem. (2007) 50: 1698-1702 [PMID:17352460]
ChEMBL Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000. F 6.49 pEC50 320 nM EC50 J. Med. Chem. (1998) 41: 4001-4011 [PMID:9767638]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antimalarial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by spectrophotometry F 5.57 pEC50 2690 nM EC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
ChEMBL Antimalarial activity against erythrocytic stage of chloroquine-sensitive Plasmodium falciparum 3D7 after 72 hrs by FACS method F 6 pEC50 1000 nM EC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay F 6.6 pEC50 252.1 nM EC50 Proc. Natl. Acad. Sci. U.S.A. (2008) 105: 9059-9064 [PMID:18579783]
ChEMBL NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay F 6.93 pEC50 116.5 nM EC50 Proc. Natl. Acad. Sci. U.S.A. (2008) 105: 9059-9064 [PMID:18579783]
Plasmodium falciparum (isolate K1 / Thailand) in Plasmodium falciparum K1 (target type: ORGANISM) [ChEMBL: CHEMBL612856]
ChEMBL Antimalarial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by spectrophotometry F 6.04 pEC50 920 nM EC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
ChEMBL Antimalarial activity against erythrocytic stage of chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by FACS method F 6.7 pEC50 200 nM EC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
K2P2.1/Potassium channel subfamily K member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321615] [GtoPdb: 514] [UniProtKB: O95069]
ChEMBL Inhibition of of human TREK1 expressed in CHO cells assessed as reduction in channel currents B 5.12 pIC50 7600 nM IC50 J. Med. Chem. (2016) 59: 5149-5157 [PMID:26588045]
K2P3.1/Potassium channel subfamily K member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321613] [GtoPdb: 515] [UniProtKB: O14649]
ChEMBL Inhibition of of TASK1 (unknown origin) expressed in CHO cells assessed as reduction in channel currents B 5.29 pIC50 5100 nM IC50 J. Med. Chem. (2016) 59: 5149-5157 [PMID:26588045]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 6.03 pKi 935 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT) B 5.79 pIC50 1637 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.73 pKi 187 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.18 pIC50 654 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.24 pKi 58 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.04 pIC50 92 nM IC50 DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.7 pKi 201 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 6.42 pIC50 384 nM IC50 DrugMatrix in vitro pharmacology data
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 6.06 pKi 865 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.73 pIC50 1863 nM IC50 DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.96 pKi 1097 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) B 5.58 pIC50 2610 nM IC50 DrugMatrix in vitro pharmacology data
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 cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as phasic inhibition after 5 mins by patch clamp assay B 5.3 pIC50 >5000 nM IC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
ChEMBL Inhibition of human cloned Nav1.5 channel expressed in chinese hamster CHO cells assessed as tonic inhibition after 5 mins by patch clamp assay B 5.48 pIC50 3300 nM IC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
ChEMBL Inhibition of sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA F 5.92 pIC50 1190 nM IC50 Cardiovasc. Res. (2011) 91: 53-61 [PMID:21300721]
Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245]
ChEMBL Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay B 4.81 pIC50 15540 nM IC50 J Med Chem (2017) 60: 2685-2696 [PMID:28230985]
ChEMBL Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy B 4.95 pIC50 11100 nM IC50 J. Med. Chem. (2008) 51: 5932-5942 [PMID:18788725]
ABCC9/Kir6.2/Sulfonylurea receptor 2, Kir6.2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095198] [GtoPdb: 2746442] [UniProtKB: O60706Q14654]
ChEMBL Inhibition of human kir6.2/SUR2A ion channel coexpressed in human HEK293 cells after 5 mins by patch clamp assay B 5.66 pIC50 2200 nM IC50 J. Med. Chem. (2011) 54: 7477-7485 [PMID:21955244]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
ChEMBL Inhibition of calcium current (ICaL) measured using whole-cell patch clamp experiments in isolated guinea pig ventricular myocytes F 5.74 pIC50 1800 nM IC50 Cardiovasc. Res. (2011) 91: 53-61 [PMID:21300721]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 5.74 pIC50 1800 nM IC50 Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000]
Kv1.5 in Human [GtoPdb: 542] [UniProtKB: P22460]
GtoPdb - - 4.4 pIC50 - - - Br J Pharmacol (1998) 125: 969-78 [PMID:9846634]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]