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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) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 |