ChEMBL ligand: CHEMBL787 (Brondilat, MK-476, Montelukast, Singulair)
A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] There should be some charts here, you may need to enable JavaScript!
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] There should be some charts here, you may need to enable JavaScript!
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] 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] 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] There should be some charts here, you may need to enable JavaScript!
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271] Cysteinyl leukotriene receptor 1 in Guinea pig [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5] There should be some charts here, you may need to enable JavaScript!
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75] There should be some charts here, you may need to enable JavaScript!
δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] There should be some charts here, you may need to enable JavaScript!
D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] There should be some charts here, you may need to enable JavaScript!
DAT/Dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] There should be some charts here, you may need to enable JavaScript!
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] There should be some charts here, you may need to enable JavaScript!
Leukotriene C4 synthase in Human [ChEMBL: CHEMBL1743183] [GtoPdb: 1391] [UniProtKB: Q16873] There should be some charts here, you may need to enable JavaScript!
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] There should be some charts here, you may need to enable JavaScript!
M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] There should be some charts here, you may need to enable JavaScript!
M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] There should be some charts here, you may need to enable JavaScript!
NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] There should be some charts here, you may need to enable JavaScript!
NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] 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] There should be some charts here, you may need to enable JavaScript!
CYP5A1/Thromboxane-A synthase in Human [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557] There should be some charts here, you may need to enable JavaScript!
FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] There should be some charts here, you may need to enable JavaScript!
GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304] GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65] 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
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)	B	6.61	pKi	245	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA)	B	6.36	pIC50	434	nM	IC50	DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	5.83	pKi	1470	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	5.41	pIC50	3919	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	6.12	pKi	767	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	5.28	pIC50	5279	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]
ChEMBL	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	B	5.62	pKi	2398	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177)	B	5.46	pIC50	3488	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	5.49	pKi	3200	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol)	B	5.37	pIC50	4300	nM	IC50	DrugMatrix in vitro pharmacology data
CysLT1 receptor/Cysteinyl leukotriene receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1798] [GtoPdb: 269] [UniProtKB: Q9Y271]
GtoPdb	against [3H]LTD4 in human lung parenchyma	-	8.55	pKi	-	-	-	Biochem Pharmacol (2002) 63: 1537-46 [PMID:11996896]
ChEMBL	DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)	B	8.94	pKi	1.14	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Antagonist activity at human CysLT1	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (2015) 58: 6093-6113 [PMID:26200813]
GtoPdb	against [3H]LTD4 in COS-7 or HEK-293 cells	-	8.64	pIC50	2.3	nM	IC50	Nature (1999) 399: 789-93 [PMID:10391245]; Mol Pharmacol (1999) 56: 657-63 [PMID:10462554]
GtoPdb	-	-	8.64	pIC50	2.3	nM	IC50	Mol Pharmacol (1999) 56: 657-63 [PMID:10462554]
ChEMBL	DRUGMATRIX: Cysteinyl leukotriene receptor 1 radioligand binding (ligand: [3H]LTD4)	B	8.64	pIC50	2.29	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	In vitro inhibition of [3H]-LTD4 binding to LTD4 receptor of DMSO differentiated human U937 cell membranes	B	9.11	pIC50	0.78	nM	IC50	Bioorg Med Chem Lett (1998) 8: 453-458 [PMID:9871597]
ChEMBL	Compound were tested for inhibitory activity against Cysteinyl leukotriene D4 receptor	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (1996) 39: 2629-2654 [PMID:8709092]
ChEMBL	Antagonist activity at CysLT1 receptor in human dU937 cells assessed as inhibition of LTD4-induced increase of calcium level treated 30 mins before LTD4 challenge	F	7.14	pEC50	72	nM	EC50	Bioorg Med Chem (2010) 18: 5519-5527 [PMID:20621485]
Cysteinyl leukotriene receptor 1 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5645] [UniProtKB: Q2NNR5]
ChEMBL	In vitro binding affinity towards Cysteinyl leukotriene D4 receptor by using [3H]LTD4 binding assay in guinea pig lung membranes	B	8.68	pKi	2.1	nM	Ki	J Med Chem (2000) 43: 392-400 [PMID:10669566]
ChEMBL	Binding affinity towards Cysteinyl leukotriene D4 receptor (cysLT1) was measured by the displacement of [3H]LTD4 radioligand	B	9.3	pKi	0.5	nM	Ki	J Med Chem (1998) 41: 1439-1445 [PMID:9554877]
ChEMBL	Concentration required for inhibition of binding of [3H]LTD4 to guinea pig lung membranes	B	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem Lett (1995) 5: 283-288
ChEMBL	Displacement of [3H]LTD4 from LTD4 receptor in guinea pig lung membrane	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (2016) 59: 8712-8756 [PMID:27299736]
CysLT2 receptor/Cysteinyl leukotriene receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4330] [GtoPdb: 270] [UniProtKB: Q9NS75]
ChEMBL	Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2015) 58: 6093-6113 [PMID:26200813]
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL	DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)	B	5.77	pKi	1690	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Opiate delta1 (OP1, DOP) radioligand binding (ligand: [3H] Naltrindole)	B	5.32	pIC50	4795	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	5.58	pKi	2631	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	5.11	pIC50	7747	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	5.68	pKi	2067	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.58	pIC50	2601	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	5.5	pIC50	3197	nM	IC50	DrugMatrix in vitro pharmacology data
Leukotriene C4 synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743183] [GtoPdb: 1391] [UniProtKB: Q16873]
ChEMBL	Inhibition of recombinant human N-terminal His6-tagged LTC4S expressed in in Pichia pastoris X33 assessed as inhibition of EXC4 formation using EXA4 as substrate preincubated for 10 mins followed by substrate addition and measured after 1 min by EIA	B	5.3	pIC50	<5000	nM	IC50	J Med Chem (2019) 62: 7769-7787 [PMID:31415176]
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539]
ChEMBL	DRUGMATRIX: Protein Serine/Threonine Kinase, p38alpha enzyme inhibition (substrate: Myelin Basic Protein)	B	6.07	pIC50	856	nM	IC50	DrugMatrix in vitro pharmacology data
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	5.71	pKi	1938	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	5.09	pIC50	8045	nM	IC50	DrugMatrix in vitro pharmacology data
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	5.85	pKi	1404	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)	B	5.18	pIC50	6626	nM	IC50	DrugMatrix in vitro pharmacology data
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	5.89	pKi	1274	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Tachykinin NK2 radioligand binding (ligand: [3H] SR-48968)	B	5.42	pIC50	3822	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	5.57	pKi	2667	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55)	B	5.57	pIC50	2689	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	5.4	pKi	3981	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	5.2	pIC50	6256	nM	IC50	DrugMatrix in vitro pharmacology data
CYP5A1/Thromboxane-A synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1835] [GtoPdb: 1353] [UniProtKB: P24557]
ChEMBL	DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)	B	5.82	pIC50	1525	nM	IC50	DrugMatrix in vitro pharmacology data
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	5.33	pIC50	4702	nM	IC50	DrugMatrix in vitro pharmacology data
GPR17/Uracil nucleotide/cysteinyl leukotriene receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075162] [GtoPdb: 88] [UniProtKB: Q13304]
ChEMBL	Displacement of [3H]PSB-12150 from human GPR17 expressed in CHO-K1 cell membranes after 60 mins by heterologous competition binding assay	B	5.18	pKi	6540	nM	Ki	ACS Med Chem Lett (2014) 5: 326-330 [PMID:24900835]
GPR17 in Mouse [GtoPdb: 88] [UniProtKB: Q6NS65]
GtoPdb	-	-	7.21	pIC50	61	nM	IC50	PLoS ONE (2008) 3: e3579 [PMID:18974869]

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]