ChEMBL ligand: CHEMBL240624 (MK-3814, Preladenant, Sch-420814, SCH 420814, SCH-420814)
A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] There should be some charts here, you may need to enable JavaScript!
A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] There should be some charts here, you may need to enable JavaScript!
A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] There should be some charts here, you may need to enable JavaScript!
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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL	Inhibition of human recombinant adenosine A1 receptor	B	5.83	pKi	1474	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb	-	-	6	pKi	>1000	nM	Ki	Recent Pat CNS Drug Discov (2007) 2: 1-21 [PMID:18221214]
ChEMBL	Binding affinity to human adenosine A1 receptor	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1376-1380 [PMID:17236762]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells by liquid scintillation counting	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5241-5244 [PMID:20659802]
ChEMBL	Inhibition of human recombinant adenosine A1 receptor	B	6	pKi	>996	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells after 90 mins by liquid scintillation counting analysis	B	6.53	pKi	295	nM	Ki	J Med Chem (2013) 56: 4580-4596 [PMID:23631427]
ChEMBL	Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting analysis	B	6.53	pKi	295	nM	Ki	J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membranes after 90 mins by liquid scintillation counting analysis	B	7.16	pKi	68.7	nM	Ki	J Med Chem (2013) 56: 4580-4596 [PMID:23631427]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method	B	9.5	pKd	0.32	nM	Kd	J Med Chem (2011) 54: 4312-4323 [PMID:21661720]
ChEMBL	Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in buculovirus system by liquid scintillation counting	B	8.3	pKi	5	nM	Ki	Bioorg Med Chem Lett (2010) 20: 5241-5244 [PMID:20659802]
ChEMBL	Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in high five cells after 30 mins by scintillation counting	B	8.3	pKi	5	nM	Ki	J Med Chem (2011) 54: 751-764 [PMID:21210664]
ChEMBL	Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method	B	8.8	pKi	1.58	nM	Ki	J Med Chem (2011) 54: 4312-4323 [PMID:21661720]
ChEMBL	Binding affinity to human adenosine A2A receptor	B	8.96	pKi	1.1	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1376-1380 [PMID:17236762]
ChEMBL	Inhibition of human recombinant adenosine receptor A2a	F	8.96	pKi	1.1	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Antagonist activity at human adenosine A2A receptor	B	8.96	pKi	1.1	nM	Ki	Medchemcomm (2019) 10: 1094-1108 [PMID:31391881]
ChEMBL	Displacement of [3H]SCH58261 from human adenosine 2A receptor expressed in HEK293 cell membranes incubated for 1.5 hrs by radioligand competition binding assay	B	8.96	pKi	1.1	nM	Ki	J Med Chem (2020) 63: 12196-12212 [PMID:32667814]
ChEMBL	Displacement of [3H]-ZM241385 from human adenosine A2A receptor expressed in HEK293 cells	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2014) 24: 152-155 [PMID:24332624]
GtoPdb	-	-	9.05	pKi	0.9	nM	Ki	Recent Pat CNS Drug Discov (2007) 2: 1-21 [PMID:18221214]
ChEMBL	Displacement of [3H]MSX2 from human recombinant adenosine A2A receptor expressed in CHO cells after 30 mins by liquid scintillation counting analysis	B	9.05	pKi	0.88	nM	Ki	J Med Chem (2013) 56: 4580-4596 [PMID:23631427]
ChEMBL	Displacement of [3H]MSX-2 from human recombinant adenosine A2A receptor expressed in CHO cells by liquid scintillation counting analysis	B	9.06	pKi	0.88	nM	Ki	J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
ChEMBL	Inhibition of human recombinant adenosine receptor A2a	F	9.22	pKi	0.6	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Antagonist activity at adenosine A2A receptor (unknown origin)	F	9.3	pKi	0.5	nM	Ki	Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776]
ChEMBL	Antagonist activity at adenosine A2A receptor (unknown origin)	F	9.3	pKi	0.5	nM	Ki	Eur J Med Chem (2018) 144: 151-163 [PMID:29268131]
ChEMBL	Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membrane incubated for 1 hr by microplate beta scintillation counting based radioligand inhibition assay	B	9.3	pKi	0.5	nM	Ki	Eur J Med Chem (2022) 241: 114620-114620 [PMID:35933788]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL	Binding affinity to rat adenosine A2A receptor	B	8.6	pKi	2.5	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1376-1380 [PMID:17236762]
ChEMBL	Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatal membranes after 30 mins by liquid scintillation counting analysis	B	9.18	pKi	0.66	nM	Ki	J Med Chem (2013) 56: 4580-4596 [PMID:23631427]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL	Binding affinity to human adenosine A2B receptor	B	5.77	pKi	>1700	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1376-1380 [PMID:17236762]
ChEMBL	Inhibition of human recombinant adenosine receptor A2b	B	5.77	pKi	>1700	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb	-	-	6	pKi	>1000	nM	Ki	Recent Pat CNS Drug Discov (2007) 2: 1-21 [PMID:18221214]
ChEMBL	Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis	B	6	pKi	>1000	nM	Ki	J Med Chem (2013) 56: 4580-4596 [PMID:23631427]
ChEMBL	Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells by liquid scintillation counting analysis	B	6	pKi	>1000	nM	Ki	J Med Chem (2021) 64: 8246-8262 [PMID:34107215]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb	-	-	6	pKi	>1000	nM	Ki	Recent Pat CNS Drug Discov (2007) 2: 1-21 [PMID:18221214]
ChEMBL	Binding affinity to human adenosine A3 receptor	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem Lett (2007) 17: 1376-1380 [PMID:17236762]
ChEMBL	Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by liquid scintillation counting analysis	B	6	pKi	>1000	nM	Ki	J Med Chem (2013) 56: 4580-4596 [PMID:23631427]
ChEMBL	Inhibition of human recombinant adenosine A3 receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting analysis	B	6	pKi	>1000	nM	Ki	J Med Chem (2021) 64: 8246-8262 [PMID:34107215]

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]