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 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]