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]
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
CYP2J2/Cytochrome P450 2J2 in Human [ChEMBL: CHEMBL3491] [GtoPdb: 1332] [UniProtKB: P51589]
D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] Histamine H1 receptor in Guinea pig [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
Neurokinin 1 receptor in Guinea pig [ChEMBL: CHEMBL3942] [UniProtKB: P30547]
NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
ABCB1/P-glycoprotein 1 in Human [ChEMBL: CHEMBL4302] [GtoPdb: 768] [UniProtKB: P08183] P-glycoprotein 1 in Mouse [ChEMBL: CHEMBL3467] [UniProtKB: P06795]
ABCB1/P-glycoprotein 3 in Mouse [ChEMBL: CHEMBL2573] [GtoPdb: 768] [UniProtKB: P21447]
Plasmodium falciparum [ChEMBL: CHEMBL364]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
Nav1.5/Sodium channel protein type V alpha subunit in Human [ChEMBL: CHEMBL1980] [GtoPdb: 582] [UniProtKB: Q14524]
Transcriptional activator protein luxR in Aliivibrio fischeri [ChEMBL: CHEMBL5351] [UniProtKB: P12746]
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241]
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig [ChEMBL: CHEMBL2366456] [UniProtKB: O35505]
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]
Kv10.1 in Human [GtoPdb: 570] [UniProtKB: O95259]

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 35:

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]