terfenadine [Ligand Id: 2608] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL17157 (Antihistamine, Histafen, Histafen 120, NSC-665802, NSC-758627, RMI 9918, RMI-9918, Seldane, Terfenadine, Terfenor, Terfenor fte, Terfex, Terfinax 120, Terfinax 60, Triludan, Triludan fte)
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
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  • Transcriptional activator protein luxR in Aliivibrio fischeri [ChEMBL: CHEMBL5351] [UniProtKB: P12746]
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  • FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
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  • Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Human [ChEMBL: CHEMBL1940] [GtoPdb: 529] [UniProtKB: Q13936]
  • Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
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  • Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.73 pKi 1846 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin) B 5.48 pIC50 3335 nM IC50 DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 6.26 pKi 545 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) B 5.43 pIC50 3748 nM IC50 DrugMatrix in vitro pharmacology data
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
ChEMBL DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha) B 6.07 pKi 852 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Chemokine CCR5 radioligand binding (ligand: [125I] MIP-1alpha) B 5.96 pIC50 1103 nM IC50 DrugMatrix in vitro pharmacology data
CYP2J2/Cytochrome P450 2J2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3491] [GtoPdb: 1332] [UniProtKB: P51589]
GtoPdb Measuring CYP2J2-induced inhibition ebastine hydroxylation. - 5.09 pIC50 8100 nM IC50 Bioorg Med Chem Lett (2006) 16: 2777-80 [PMID:16495056]
ChEMBL Inhibition of human recombinant CYP2J2 expressed in baculovirus-infected Sf9 insect cells B 5.09 pIC50 8100 nM IC50 Bioorg Med Chem Lett (2006) 16: 2777-2780 [PMID:16495056]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.87 pKi 1337 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) B 5.57 pIC50 2673 nM IC50 DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.69 pKi 2056 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D2L radioligand binding (ligand: [3H] Spiperone) B 5.21 pIC50 6167 nM IC50 DrugMatrix in vitro pharmacology data
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 6.29 pKi 511 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) B 5.82 pIC50 1503 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 6.69 pKi 203 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) B 6.59 pIC50 255 nM IC50 DrugMatrix in vitro pharmacology data
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.45 pIC50 3566 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 [3H]astemizole binding to Potassium channel HERG B 6.49 pKi 320 nM Ki J Med Chem (2005) 48: 1725-1728 [PMID:15771419]
ChEMBL Binding affinity to human ERG assessed as inhibition constant B 7.11 pKi 78 nM Ki J Med Chem (2021) 64: 13373-13393 [PMID:34472337]
ChEMBL Inhibition of human ERG channel B 7.25 pKi 56 nM Ki J Med Chem (2015) 58: 2584-2608 [PMID:25494650]
ChEMBL Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay B 4.25 pIC50 56000 nM IC50 Bioorg Med Chem Lett (2006) 16: 5507-5512 [PMID:16931010]
ChEMBL Inhibition of human ERG expressed in HEK293 cells measured after 30 mins by FluxOR dye based FLIPR TETRA assay B 5.92 pIC50 1200 nM IC50 J Med Chem (2020) 63: 5734-5751 [PMID:32392053]
ChEMBL Inhibition of human ERG F656A mutant expressed in HEK293 cells by whole cell patch clamp method B 6.02 pIC50 960 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of human ERG Y652A mutant expressed in HEK293 cells by whole cell patch clamp method B 6.46 pIC50 350 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of human ERG in L929 cells by whole cell patch-clamp assay B 6.51 pIC50 312 nM IC50 Bioorg Med Chem Lett (2009) 19: 5043-5047 [PMID:19660947]
ChEMBL Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay B 6.51 pIC50 312 nM IC50 Bioorg Med Chem Lett (2009) 19: 5043-5047 [PMID:19660947]
ChEMBL Inhibition of human ERG B 6.67 pIC50 213.8 nM IC50 Eur J Med Chem (2011) 46: 618-630 [PMID:21185626]
ChEMBL Inhibition of human ERG channel B 6.67 pIC50 213 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL Inhibition of human ERG channel B 6.67 pIC50 213 nM IC50 J Med Chem (2009) 52: 4266-4276 [PMID:19534531]
ChEMBL K+ channel blocking activity in human embryonic kidney cells expressing HERG Kv11.1 F 6.69 pIC50 204 nM IC50 J Med Chem (2002) 45: 3844-3853 [PMID:12190308]
ChEMBL Inhibitory concentration against potassium channel HERG B 6.7 pIC50 199.53 nM IC50 Bioorg Med Chem Lett (2005) 15: 2886-2890 [PMID:15911273]
ChEMBL Inhibition of human Potassium channel HERG expressed in mammalian cells B 6.7 pIC50 199.53 nM IC50 Bioorg Med Chem Lett (2003) 13: 2773-2775 [PMID:12873512]
ChEMBL Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique B 6.7 pIC50 199.53 nM IC50 Bioorg Med Chem (2008) 16: 6252-6260 [PMID:18448342]
ChEMBL Displacement of [3H]astemizole from human ERG expressed in HEK293 cells by scintillation counting method B 6.89 pIC50 130 nM IC50 J Med Chem (2014) 57: 8540-8562 [PMID:25238555]
ChEMBL Inhibition of partially open human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) F 6.89 pIC50 128.82 nM IC50 Bioorg Med Chem Lett (2005) 15: 1737-1741 [PMID:15745831]
ChEMBL Inhibition of human ERG in MCF7 cells B 6.89 pIC50 128.82 nM IC50 Eur J Med Chem (2009) 44: 1926-1932 [PMID:19110341]
ChEMBL Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual patch clamp assay B 7.07 pIC50 86 nM IC50 J Med Chem (2019) 62: 1484-1501 [PMID:30624934]
ChEMBL Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 B 7.25 pIC50 56 nM IC50 Bioorg Med Chem Lett (2003) 13: 1829-1835 [PMID:12729675]
ChEMBL Inhibitory activity against Potassium channel HERG B 7.25 pIC50 56 nM IC50 J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis B 7.25 pIC50 56 nM IC50 Bioorg Med Chem Lett (2012) 22: 3781-3785 [PMID:22542010]
GtoPdb - - 7.3 pIC50 56 nM IC50 FEBS Lett (1997) 417: 28-32 [PMID:9395068]
ChEMBL Inhibitory concentration against IKr potassium channel B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2004) 14: 4771-4777 [PMID:15324906]
ChEMBL Inhibition of human ERG S624A mutant expressed in HEK293 cells by whole cell patch clamp method B 7.52 pIC50 30 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of wild-type human ERG expressed in HEK293 cells by whole cell patch clamp method B 7.52 pIC50 30 nM IC50 J Med Chem (2009) 52: 1630-1638 [PMID:19260734]
ChEMBL Inhibition of human ERG expressed in HEK293 cells by patch clamp method B 7.66 pIC50 22 nM IC50 J Med Chem (2017) 60: 4424-4443 [PMID:28481112]
ChEMBL Inhibition of hERG K channel F 8.05 pIC50 8.9 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Binding affinity towards histamine H1 receptor B 7.24 pKi 58 nM Ki J Med Chem (2003) 46: 2017-2022 [PMID:12747773]
ChEMBL Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHO cell by Betaplate scintillation counting B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2009) 19: 5043-5047 [PMID:19660947]
GtoPdb - - 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2009) 19: 5043-7 [PMID:19660947]
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 8.59 pKi 2.59 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL Antagonism of the human histamine H1 receptor F 6.25 pIC50 563 nM IC50 Bioorg Med Chem Lett (1997) 7: 2819-2824
ChEMBL DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine) B 7.66 pIC50 22 nM IC50 DrugMatrix in vitro pharmacology data
ChEMBL Inhibition of histamine H1 receptor (unknown origin) B 9 pIC50 1 nM IC50 J Med Chem (2015) 58: 2584-2608 [PMID:25494650]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Inhibition of specific binding of [3H]mepyramine to Histamine 1 receptors in guinea-pig B 6.52 pKd 302 nM Kd Bioorg Med Chem Lett (1991) 1: 387-390
ChEMBL Dissociation constant was determined against H1 receptor of guinea pig lung membranes using radioligand binding assays. B 7.45 pKd 35.48 nM Kd J Med Chem (1995) 38: 2472-2477 [PMID:7608912]
ChEMBL Inhibitory activity against Tritiated [3H]- mepyramine binding to histamine H1 receptor in guinea pig cerebral cortex B 6.53 pIC50 295 nM IC50 J Med Chem (1989) 32: 105-118 [PMID:2562852]
ChEMBL Compound is evaluated for in vitro receptor binding affinity against H1 receptor B 7.03 pIC50 94 nM IC50 J Med Chem (1995) 38: 4026-4032 [PMID:7562938]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Compound is evaluated for in vitro receptor binding affinity against Muscarinic acetylcholine receptor M1 B 5.54 pIC50 2900 nM IC50 J Med Chem (1995) 38: 4026-4032 [PMID:7562938]
Neurokinin 1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
ChEMBL Antagonism of the guinea pig tachykinin NK1 receptor F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (1997) 7: 2819-2824
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 6.05 pKi 892 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968) B 5.57 pIC50 2677 nM IC50 DrugMatrix in vitro pharmacology data
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 5.72 pKi 1912 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) B 5.71 pIC50 1928 nM IC50 DrugMatrix in vitro pharmacology data
ABCB1/P-glycoprotein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183]
ChEMBL TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells F 5.57 pIC50 2700 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells F 5.6 pIC50 2500 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells F 5.74 pIC50 1800 nM IC50 Biochem Biophys Res Commun (2001) 289: 580-585 [PMID:11716514]
ChEMBL Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.85 pIC50 1400 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells F 5.85 pIC50 1400 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCEC F 5.96 pIC50 1100 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
P-glycoprotein 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 5.7 pIC50 2000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells F 5.7 pIC50 2000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ABCB1/P-glycoprotein 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
ChEMBL Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay F 4.64 pIC50 23000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
ChEMBL TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells F 4.64 pIC50 23000 nM IC50 J Med Chem (2003) 46: 1716-1725 [PMID:12699389]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5.2 pIC50 6309.57 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5.3 pIC50 5011.87 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay F 5.5 pIC50 3162.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.6 pIC50 2511.89 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.7 pIC50 1995.26 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
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 7.14 pKi 73 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin) B 6.59 pIC50 255 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 7.52 pKi 30 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 7.32 pIC50 48 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 6.19 pKi 645 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) B 5.91 pIC50 1231 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 6.22 pKi 606 nM Ki DrugMatrix in vitro pharmacology data
ChEMBL DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 radioligand binding (ligand: [3H] Lysergic acid diethylamide) B 5.88 pIC50 1306 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 sodium current measured using whole-cell patch clamp experiments in HEK-293 cells stably transfected with hNaV1.5 cDNA F 6.01 pIC50 971 nM IC50 Cardiovasc Res (2011) 91: 53-61 [PMID:21300721]
Transcriptional activator protein luxR in Aliivibrio fischeri (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5351] [UniProtKB: P12746]
ChEMBL Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity B 4.04 pIC50 92000 nM IC50 Bioorg Med Chem Lett (2010) 20: 4355-4358 [PMID:20615699]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
ChEMBL DRUGMATRIX: Protein Tyrosine Kinase, Fyn enzyme inhibition (substrate: Poly(Glu:Tyr)) B 5.21 pIC50 6123 nM IC50 DrugMatrix in vitro pharmacology data
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 6.43 pIC50 375 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 6.43 pIC50 375 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes F 6.6 pIC50 250 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
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 L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit F 5.88 pIC50 1320 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002]
ChEMBL Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes F 6.85 pIC50 142 nM IC50 J Appl Toxicol (2012) 32: 858-866 [PMID:22761000]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]
GtoPdb - - 7.8 pIC50 - - - Mol Pharmacol (2004) 65: 1120-9 [PMID:15102940]

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]