ChEMBL ligand: CHEMBL291536 (SB-334867)
A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] There should be some charts here, you may need to enable JavaScript!
OX1 receptor/Orexin receptor 1 in Human [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613] OX1 receptor in Rat [GtoPdb: 321] [UniProtKB: P56718] There should be some charts here, you may need to enable JavaScript!
OX2 receptor/Orexin receptor 2 in Human [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614] 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!
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 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
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Binding affinity to adenosine 2A receptor (unknown origin)	B	6.17	pKi	670	nM	Ki	Bioorg Med Chem (2017) 25: 5203-5215 [PMID:28807572]
OX1 receptor/Orexin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613]
ChEMBL	Binding affinity to human OXIR	B	7.32	pKi	48	nM	Ki	ACS Med Chem Lett (2020) 11: 2002-2009 [PMID:33062185]
GtoPdb	-	-	7.4	pKi	-	-	-	Br J Pharmacol (2009) 156: 1326-41 [PMID:19751316]
ChEMBL	Displacement of N6,10-rhodamine green-tagged orexin-A from human OX1 receptor expressed in CHO cells measured after 30 mins by syto62 staining based laser scanning cytometry	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem Lett (2016) 26: 5809-5814 [PMID:27818110]
ChEMBL	Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method	B	7.8	pKi	15.85	nM	Ki	J Med Chem (2020) 63: 1528-1543 [PMID:31860301]
ChEMBL	Displacement of [125I]-orexin A from human OX1 receptor expressed in CHO cell membranes after 90 mins by scintillation counting	B	7.85	pKi	14	nM	Ki	J Med Chem (2016) 59: 8263-8275 [PMID:27546834]
GtoPdb	-	-	7.9	pKi	-	-	-	Br J Pharmacol (2004) 141: 340-6 [PMID:14691055]; Bioorg Med Chem Lett (2001) 11: 1907-10 [PMID:11459658]; Mol Pharmacol (2009) 76: 618-31 [PMID:19542319]; J Med Chem (2020) 63: 1528-1543 [PMID:31860301]; J Pharmacol Exp Ther (2015) 352: 590-601 [PMID:25583879]
ChEMBL	Antagonist activity at human OX1R expressed in CHOK1 cells by Syto62 probe based fluorescence assay	B	4.74	pIC50	18000	nM	IC50	Eur J Med Chem (2019) 181: 111569-111569 [PMID:31404862]
ChEMBL	Antagonist activity at OX1 receptor expressed in CHO cells assessed as inhibition of OXA-stimulated intracellular calcium mobilization after 30 mins by FLIPR assay	F	7.4	pIC50	40	nM	IC50	Bioorg Med Chem Lett (2012) 22: 3890-3894 [PMID:22617492]
OX1 receptor in Rat [GtoPdb: 321] [UniProtKB: P56718]
GtoPdb	-	-	6.84	pKi	144	nM	Ki	J Pharmacol Exp Ther (2015) 352: 590-601 [PMID:25583879]
OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614]
GtoPdb	-	-	5.2	pKi	-	-	-	Br J Pharmacol (2009) 156: 1326-41 [PMID:19751316]
ChEMBL	Binding affinity to human OX2R	B	5.42	pKi	3781	nM	Ki	ACS Med Chem Lett (2020) 11: 2002-2009 [PMID:33062185]
ChEMBL	Binding affinity to human OX2 receptor expressed in CHO cells by fluorescence assay	B	6.08	pKi	835	nM	Ki	Bioorg Med Chem Lett (2016) 26: 5809-5814 [PMID:27818110]
ChEMBL	Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX2 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method	B	6.2	pKi	630.96	nM	Ki	J Med Chem (2020) 63: 1528-1543 [PMID:31860301]
GtoPdb	-	-	6.3	pKi	-	-	-	Bioorg Med Chem Lett (2001) 11: 1907-10 [PMID:11459658]; Mol Pharmacol (2009) 76: 618-31 [PMID:19542319]; Br J Pharmacol (2014) 171: 351-63 [PMID:23692283]; J Pharmacol Exp Ther (2015) 352: 590-601 [PMID:25583879]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	Binding affinity against 5-hydroxytryptamine 2B receptor	B	5.4	pKi	3981.07	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1907-1910 [PMID:11459658]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	Binding affinity against 5-hydroxytryptamine 2C receptor	B	5.3	pKi	<5011.87	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1907-1910 [PMID:11459658]
ChEMBL	Binding affinity to 5HT2c receptor (unknown origin)	B	5.92	pKi	1200	nM	Ki	Bioorg Med Chem (2017) 25: 5203-5215 [PMID:28807572]

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]