ChEMBL ligand: CHEMBL464859 (5'-N-Ethylcarboxamidoadenosine, NECA)
Adenosine A1 receptor in Chicken [ChEMBL: CHEMBL2114] [UniProtKB: P49892] A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190] A1 receptor/Adenosine A1 receptor in Mouse [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612] A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] 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] A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614] A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] 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] A3 receptor/Adenosine A3 receptor in Mouse [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] There should be some charts here, you may need to enable JavaScript!
heat shock protein 90 beta family member 1/Endoplasmin in Human [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625] Endoplasmin in Pig [ChEMBL: CHEMBL3425397] [UniProtKB: Q29092] There should be some charts here, you may need to enable JavaScript!
oxoglutarate receptor/G protein-coupled receptor 80 in Rat [ChEMBL: CHEMBL2325] [GtoPdb: 162] [UniProtKB: Q6Y1R5] There should be some charts here, you may need to enable JavaScript!
Heat shock protein 90 beta in Dog [ChEMBL: CHEMBL4748] [UniProtKB: P41148] There should be some charts here, you may need to enable JavaScript!
heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] There should be some charts here, you may need to enable JavaScript!
Transmembrane domain-containing protein TMIGD3 in Human [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9] 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
Adenosine A1 receptor in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2114] [UniProtKB: P49892]
ChEMBL	Displacement of [125I]ABA from adenosine A1 receptor of chick cerebellar membrane	B	7.77	pIC50	17	nM	IC50	J Med Chem (1987) 30: 954-956 [PMID:3572985]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL	Binding affinity to A1R E172 5.30A mutant (unknown origin) by saturation NanoBRET binding assay	B	5.38	pKd	4168.69	nM	Kd	J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor in CHO cells	B	6.24	pKd	575.44	nM	Kd	J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL	Binding affinity to A1R S267 7.32A mutant (unknown origin) in by saturation NanoBRET binding assay	B	6.31	pKd	489.78	nM	Kd	J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL	Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay	B	6.63	pKd	234.42	nM	Kd	J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL	Binding affinity to wild type A1R (unknown origin) by saturation NanoBRET binding assay	B	6.67	pKd	213.8	nM	Kd	J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL	Binding affinity to A1R H251 6.52A mutant (unknown origin) by saturation NanoBRET binding assay	B	8.04	pKd	9.12	nM	Kd	J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL	Dissociation constant against Adenosine A1 receptor	B	8.07	pKd	8.6	nM	Kd	J Med Chem (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay	B	5.3	pKi	5011.87	nM	Ki	J Med Chem (2021) 64: 6670-6695 [PMID:33724031]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 2 hrs by scintillation counting analysis relative to control	B	5.95	pKi	1122.02	nM	Ki	Medchemcomm (2012) 3: 333-338
ChEMBL	Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay	B	6.61	pKi	245.47	nM	Ki	J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL	Displacement of CA200645 from NLuc human A1 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay	B	6.69	pKi	204.17	nM	Ki	ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146]
ChEMBL	Affinity for Adenosine A1 receptor by displacement of [3H]DPCPX from human cerebral cortex	B	6.7	pKi	>200	nM	Ki	Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602]
ChEMBL	Binding affinity to wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay	B	7.08	pKi	83.18	nM	Ki	J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL	Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells	B	7.74	pKi	18.3	nM	Ki	J Med Chem (2007) 50: 374-380 [PMID:17228880]
ChEMBL	Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells	B	7.74	pKi	18.2	nM	Ki	J Med Chem (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL	Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells	B	7.74	pKi	18.2	nM	Ki	Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548]
ChEMBL	Displacement of [3H]-CCPA from CHO cells expressing human recombinant Adenosine A1 receptor	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	7.85	pKi	14	nM	Ki	J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	7.85	pKi	14	nM	Ki	J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL	Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells	B	7.85	pKi	14	nM	Ki	J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	7.85	pKi	14	nM	Ki	J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL	Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane	B	7.85	pKi	14	nM	Ki	J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins	B	7.85	pKi	14	nM	Ki	Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL	Binding affinity to human recombinant adenosine A1 receptor	B	7.85	pKi	14	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Displacement of [3H]CCPA from human recombinant adenosine A1 receptor	B	7.87	pKi	13.6	nM	Ki	ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL	Displacement of [3H]CCPA from human recombinant adenosine A1 receptor	B	7.87	pKi	13.6	nM	Ki	Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL	Binding affinity for human adenosine A1 receptor	B	7.87	pKi	13.6	nM	Ki	J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL	Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]DPCPX; Range = 9.6-15 nM	B	7.92	pKi	12	nM	Ki	J Med Chem (2004) 47: 3707-3709 [PMID:15239649]
ChEMBL	In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement.	B	7.92	pKi	12	nM	Ki	J Med Chem (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL	Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method	B	8.06	pKi	8.62	nM	Ki	J Med Chem (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane	B	8.11	pKi	7.8	nM	Ki	J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL	Binding affinity to human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay	B	8.17	pKi	6.8	nM	Ki	J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL	Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer	B	8.17	pKi	6.8	nM	Ki	J Med Chem (2012) 55: 8075-8090 [PMID:22921089]
ChEMBL	Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method	B	8.17	pKi	6.8	nM	Ki	J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL	Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells	B	8.17	pKi	6.8	nM	Ki	J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
GtoPdb	-	-	8.2	pKi	-	-	-	J Biol Chem (1994) 269: 32077-84 [PMID:7798201]; J Biol Chem (1999) 274: 3617-21 [PMID:9920910]; J Biol Chem (1994) 269: 2373-6 [PMID:8300561]; Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
ChEMBL	Inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells	B	8.3	pKi	5	nM	Ki	J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL	Displacement of [3H]-CCPA from human A1 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay	B	8.34	pKi	4.6	nM	Ki	Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
ChEMBL	Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method	B	8.34	pKi	4.6	nM	Ki	J Med Chem (2017) 60: 5772-5790 [PMID:28590753]
ChEMBL	Displacement of [3H]N6-R-phenylisopropyladenosine from human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay	B	8.52	pKi	3	nM	Ki	J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL	Displacement of 3[H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 mins by Liquid scintillation analysis	B	8.52	pKi	3	nM	Ki	J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL	Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells	B	8.98	pKi	1.04	nM	Ki	Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL	Antagonist activity at wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins	F	8.95	pIC50	1.12	nM	IC50	J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL	Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gi-mediated inhibition of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry	F	9.1	pIC50	0.79	nM	IC50	Medchemcomm (2012) 3: 333-338
ChEMBL	Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis	F	9.68	pIC50	0.21	nM	IC50	J Med Chem (2016) 59: 947-964 [PMID:26756468]
ChEMBL	Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gs-mediated activation of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry	F	5.83	pEC50	1479.11	nM	EC50	Medchemcomm (2012) 3: 333-338
ChEMBL	Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase reporter gene assay	B	6	pEC50	1000	nM	EC50	J Med Chem (2016) 59: 947-964 [PMID:26756468]
ChEMBL	Binding against human adenosine A1 receptor	B	7.23	pEC50	59	nM	EC50	Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL	Agonist activity at Homo sapiens (human) adenosine A1 receptor expressed in CHO cells	B	7.5	pEC50	31.62	nM	EC50	Med Chem Res (2004) 13: 88-98
ChEMBL	Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay	B	7.52	pEC50	30	nM	EC50	Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL	Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay	F	7.99	pEC50	10.2	nM	EC50	ACS Med Chem Lett (2011) 2: 626-631 [PMID:21858244]
ChEMBL	Agonist activity at human A1A adenosine receptor expressed in CHOKI cells assessed as induction of beta-arrestin2 recruitment after 60 mins	B	8.3	pEC50	5.03	nM	EC50	J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL	Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of calcium mobilization by calcium mobilization assay	F	8.31	pEC50	4.9	nM	EC50	J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL	Antagonist activity at human wild type A1R expressed in CHO-K1 cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay	F	8.74	pEC50	1.82	nM	EC50	ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146]
ChEMBL	Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay	F	8.79	pEC50	1.62	nM	EC50	J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
ChEMBL	Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation incubated for 30 mins by LANCE cAMP assay	F	8.86	pEC50	1.38	nM	EC50	J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL	Agonist activity at human adenosine A1 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay	F	8.9	pEC50	1.26	nM	EC50	Medchemcomm (2014) 5: 192-196
ChEMBL	Agonist activity at human adenosine A1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay	F	8.96	pEC50	1.1	nM	EC50	J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL	Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay	F	9.12	pEC50	0.76	nM	EC50	J Med Chem (2018) 61: 2087-2103 [PMID:29446948]
ChEMBL	Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of ERK1/2 phosphorylation incubated for 5 mins	B	9.3	pEC50	0.5	nM	EC50	J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
ChEMBL	Activity at human adenosine A1 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells	F	9.44	pEC50	0.36	nM	EC50	J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL	Agonist activity at adenosine A1 receptor assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation in CHO cells	F	9.44	pEC50	0.36	nM	EC50	J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL	Agonist activity at human A1A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay	F	9.92	pEC50	0.12	nM	EC50	J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL	Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes.	B	7.85	pKi	14	nM	Ki	J Med Chem (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes	B	7.85	pKi	14	nM	Ki	J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL	Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes	B	7.85	pKi	14	nM	Ki	J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL	Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes	B	7.85	pKi	14	nM	Ki	J Med Chem (2005) 48: 1550-1562 [PMID:15743197]
A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
ChEMBL	Displacement of [3H]N6-R-phenylisopropyladenosine from mouse A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay	B	9.35	pKi	0.45	nM	Ki	J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay	B	6.53	pKd	295.12	nM	Kd	J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL	Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine	B	5.9	pKi	1257	nM	Ki	J Med Chem (1990) 33: 1919-1924 [PMID:2362269]
ChEMBL	Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX	B	6.19	pKi	650	nM	Ki	J Med Chem (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL	Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the presence of 1 mM of GTP	B	6.28	pKi	530	nM	Ki	J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL	Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay	B	6.38	pKi	416.87	nM	Ki	J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL	Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand.	B	7.2	pKi	63	nM	Ki	J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL	Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the absence of GTP	B	7.2	pKi	63	nM	Ki	J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL	Displacement of [3H]N6-R-phenylisopropyladenosine from rat A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay	B	7.2	pKi	63	nM	Ki	J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL	Displacement of 3[H]R-PIA from rat A1 adenosine receptor expressed in CHO cells after 60 min by Liquid scintillation analysis	B	7.2	pKi	63	nM	Ki	J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL	Ability to displace [3H]DPCPX from Adenosine A1 receptor in rat cortical membrane	B	7.2	pKi	63	nM	Ki	J Med Chem (2002) 45: 420-429 [PMID:11784146]
ChEMBL	Binding affinity towards adenosine A1 receptor in rat brain cortex	B	7.88	pKi	13.3	nM	Ki	J Med Chem (2001) 44: 531-539 [PMID:11170643]
ChEMBL	Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand	B	7.88	pKi	13.3	nM	Ki	J Med Chem (1992) 35: 241-252 [PMID:1732541]
ChEMBL	Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX	B	7.96	pKi	11	nM	Ki	J Med Chem (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL	Displacement of [3H]CHA from Adenosine A1 receptor of rat brain	B	7.98	pKi	10.4	nM	Ki	J Med Chem (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL	Displacement of [3H]CHA from Adenosine A1 receptor of rat brain	B	7.98	pKi	10.4	nM	Ki	J Med Chem (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL	Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand.	B	7.98	pKi	10.4	nM	Ki	J Med Chem (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL	Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand	B	7.98	pKi	10.4	nM	Ki	J Med Chem (1994) 37: 1720-1726 [PMID:8201607]
ChEMBL	Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor	B	7.99	pKi	10.3	nM	Ki	J Med Chem (1992) 35: 4143-4149 [PMID:1433217]
ChEMBL	Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand.	B	8.08	pKi	8.3	nM	Ki	J Med Chem (1992) 35: 2881-2890 [PMID:1495019]
ChEMBL	Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes	B	8.09	pKi	8.2	nM	Ki	J Med Chem (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL	Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA	B	8.09	pKi	8.2	nM	Ki	J Med Chem (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL	Binding activity against Adenosine A1 receptor from rat brain membranes using [3H]8-cyclopentyl-1,3-dipropylxanthine (DPCPX)	B	8.11	pKi	7.7	nM	Ki	J Med Chem (2001) 44: 208-214 [PMID:11170630]
ChEMBL	Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement.	B	8.2	pKi	6.3	nM	Ki	J Med Chem (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL	Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand	B	8.2	pKi	6.3	nM	Ki	J Med Chem (1992) 35: 407-422 [PMID:1738138]
ChEMBL	Inhibition of [3H]- DPCPX binding to Adenosine A1 receptor ofrat brain membranes	B	8.2	pKi	6.3	nM	Ki	J Med Chem (1998) 41: 2676-2678 [PMID:9667957]
ChEMBL	Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]R-PIA.	B	8.2	pKi	6.3	nM	Ki	J Med Chem (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL	Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine	B	8.2	pKi	6.3	nM	Ki	J Med Chem (1988) 31: 271-273 [PMID:3336027]
ChEMBL	Binding affinity for A1-adenosine receptor by the displacement of specific [3H]-PIA binding in rat brain was determined	B	8.2	pKi	6.3	nM	Ki	J Med Chem (1994) 37: 636-646 [PMID:8126704]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain	B	8.2	pKi	6.24	nM	Ki	J Med Chem (1985) 28: 1383-1384 [PMID:2995663]
GtoPdb	-	-	8.29	pKi	5.1	nM	Ki	Curr Pharm Des (1996) 2: 501-530
ChEMBL	Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis	B	8.29	pKi	5.1	nM	Ki	Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL	Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex	B	8.29	pKi	5.1	nM	Ki	ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL	Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor	B	4.05	pIC50	90000	nM	IC50	J Med Chem (1988) 31: 752-756 [PMID:3351851]
ChEMBL	Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor	B	4.28	pIC50	52000	nM	IC50	J Med Chem (1988) 31: 752-756 [PMID:3351851]
ChEMBL	Binding affinity towards adenosine A1 receptor of rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding	B	5.61	pIC50	2460	nM	IC50	J Med Chem (1988) 31: 745-751 [PMID:3351850]
ChEMBL	Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor	B	6.7	pIC50	200	nM	IC50	J Med Chem (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL	Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor	B	7.8	pIC50	16	nM	IC50	J Med Chem (1991) 34: 2570-2579 [PMID:1875349]
ChEMBL	Potency against rat brain adenosine A1 receptor	B	7.99	pIC50	10.2	nM	IC50	J Med Chem (1986) 29: 1683-1689 [PMID:3018244]
ChEMBL	Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand.	B	8	pIC50	10	nM	IC50	J Med Chem (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL	Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding	B	8.62	pIC50	2.4	nM	IC50	J Med Chem (1988) 31: 745-751 [PMID:3351850]
ChEMBL	Functional activity against adenosine A1 receptor from rat atria.	F	4.26	pEC50	54800	nM	EC50	J Med Chem (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL	[S]GTP gamma-S binding against adenosine A1 receptor in rat brain	B	7.06	pEC50	87.2	nM	EC50	Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL	Activity at Adenosine A1 receptor of rat atria