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, Terfenadina, 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 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]