dopamine [Ligand Id: 940] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL59 (Carbilev, Parcopa, Sinemet, Dopamine, Intropin, NSC-173182)
  • 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!
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Rat [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
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]
  • Beta-2 adrenergic receptor in Dog [ChEMBL: CHEMBL2289] [UniProtKB: P54833]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • Dopamine D2 receptor in Bovine [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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]
  • D3 receptor/Dopamine D3 receptor in Rat [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • D4 receptor/Dopamine D4 receptor in Rat [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729]
There should be some charts here, you may need to enable JavaScript!
  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2]
There should be some charts here, you may need to enable JavaScript!
  • MT1 receptor/Melatonin receptor 1A in Human [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039]
There should be some charts here, you may need to enable JavaScript!
  • MT2 receptor/Melatonin receptor 1B in Human [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286]
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-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
  • Organic cation transporter 3/Solute carrier family 22 member 3 in Rat [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446]
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!
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
ChEMBL Compound was tested for its binding affinity against Alpha-2 adrenergic receptor B 6.01 pKi 977.24 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 2371-2376
β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090]
ChEMBL Binding of [3H]dihydroalprenolol to beta-1 adrenergic receptor of rat cerebral cortical membranes B 5 pKi 10000 nM Ki J. Med. Chem. (2000) 43: 1611-1619 [PMID:10780918]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Binding affinity to human adrenergic beta2 receptor B 4.19 pKd 64560 nM Kd Eur. J. Med. Chem. (2009) 44: 2840-2846 [PMID:19168263]
ChEMBL Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells B 4.21 pKi 61000 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833]
ChEMBL Binding of [3H]dihydroalprenolol to beta-2 adrenergic receptor of rat cerebral cortical membranes B 4.3 pKi 50000 nM Ki J. Med. Chem. (2000) 43: 1611-1619 [PMID:10780918]
cyclic AMP phosphoprotein in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2170] [UniProtKB: Q712U5]
ChEMBL Effective concentration that gives maximal stimulation of cyclic AMP production over the concentration range tested. F 5.46 pEC50 3500 nM EC50 J. Med. Chem. (1984) 27: 28-35 [PMID:6317860]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Equilibrium dissociation constant against recombinant Dopamine receptor D1A expressed in COS7 cells B 5.6 pKd 2500 nM Kd J. Med. Chem. (1996) 39: 850-859 [PMID:8632409]
ChEMBL Affinity towards Dopamine receptor D1 B 4.74 pKi 18200 nM Ki J. Med. Chem. (1998) 41: 4385-4399 [PMID:9784114]
ChEMBL Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells B 4.92 pKi 12000 nM Ki Eur. J. Med. Chem. (2012) 55: 255-261 [PMID:22846798]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by scintillation counting analysis B 4.92 pKi 12000 nM Ki Bioorg. Med. Chem. (2013) 21: 4143-4150 [PMID:23727194]
ChEMBL Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells B 5.35 pKi 4470 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
GtoPdb - - 5.6 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762];
J Biol Chem (1994) 269: 27925-31 [PMID:7525564]
ChEMBL Displacement of [3H]-SCH23390 from human dopamine D1 receptor expressed in LTK cell membranes after 30 mins by liquid scintillation counting B 6.61 pKi 243 nM Ki J Med Chem (2018) 61: 11384-11397 [PMID:30431269]
ChEMBL Binding affinity to displace [3H]- SCH 23390 against Dopamine receptor D1 B 6.72 pKi 192 nM Ki J. Med. Chem. (1990) 33: 2197-2204 [PMID:1973733]
ChEMBL Binding affinity against cloned human Dopamine receptor D1 using [125I]-SCH 23982 as radioligand transfected in HEK cells B 6.89 pKi 130 nM Ki J. Med. Chem. (1995) 38: 3445-3447 [PMID:7658429]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor expressed in Ltk deficient fibroblast cells by liquid scintillation counting B 6.91 pKi 124 nM Ki Bioorg. Med. Chem. (2009) 17: 4756-4762 [PMID:19454369]
ChEMBL Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on beta-arrestin2 recruitment by PRESTO-Tango beta-arrestin2 recruitment assay B 5.85 pEC50 1400 nM EC50 ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001]
ChEMBL Agonist activity at human dopamine D1 receptor expressed in HEK293T cells assessed as induction of cAMP levels after 30 mins by HTRF assay F 6.63 pEC50 232 nM EC50 J Med Chem (2018) 61: 11384-11397 [PMID:30431269]
ChEMBL Activity at human dopamine D1 receptor expressed in HEK293 cells assessed as stimulation of cAMP production F 6.92 pEC50 120 nM EC50 J. Med. Chem. (2006) 49: 6848-6857 [PMID:17154515]
ChEMBL Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D1 B 7 pEC50 100 nM EC50 J. Med. Chem. (1995) 38: 3445-3447 [PMID:7658429]
ChEMBL Agonist activity at wild type human D1R expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay B 7.36 pEC50 44 nM EC50 ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001]
ChEMBL Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as cAMP production after 20 mins B 7.41 pEC50 39 nM EC50 Bioorg. Med. Chem. (2014) 22: 381-392 [PMID:24296012]
ChEMBL Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production F 7.46 pEC50 35 nM EC50 Bioorg. Med. Chem. (2008) 16: 3438-3444 [PMID:18313303]
ChEMBL Agonist activity at human D1 receptor assessed as cAMP accumulation F 7.7 pEC50 20 nM EC50 Bioorg. Med. Chem. (2010) 18: 6763-6770 [PMID:20709559]
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Binding affinity against Dopamine receptor D1 like from bovine retina membranes measured using [3H]SCH-23390 radioligand B 5.37 pKi 4300 nM Ki J. Med. Chem. (1998) 41: 4933-4938 [PMID:9836610]
ChEMBL Binding affinity for dopamine D1-like receptor labelled with [3H]SCH-23390 in retina B 5.37 pKi 4300 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 223-226 [PMID:11206464]
ChEMBL Binding Affinity was determined for its ability to displace the radioligand [3H]-SCH- 23390 from Bovine dopamine receptor D1 B 5.8 pKi 1600 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding Affinity was tested on low Affinity Site of Bovine Dopamine D1 Receptor. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site. B 6.19 pKi 650 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor in bovine striatum B 6.36 pKi 440 nM Ki Bioorg. Med. Chem. (2013) 21: 1680-1684 [PMID:23428965]
ChEMBL Binding Affinity was tested on relative proportion of High Affinity Site of Bovine dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 at the binding site. B 7.44 pKi 36 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding Affinity was tested on High Affinity Site of Bovine Dopamine receptor D1. Tested for ability to displace the radioligand [3H]-SCH- 23390 B 8.15 pKi 7 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL In vitro binding affinity towards Dopamine D1 receptor using [3H]-SCH- 23390 as radioligand B 6.7 pIC50 200 nM IC50 Bioorg. Med. Chem. Lett. (1991) 1: 403-406
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Affinity for Dopamine receptor D1 binding sites was evaluated in a test involving displacement of [3H]- fenoldopam in rat striatum B 6.82 pKd 0.15 uM K Bind J. Med. Chem. (1986) 29: 1615-1627 [PMID:2875183]
ChEMBL In vitro affinity against Dopamine receptor D1 using [3H]SCH-23390 radioligand in rat striatal homogenate. B 5.36 pKi 4400 nM Ki J. Med. Chem. (1986) 29: 1889-1895 [PMID:3761308]
ChEMBL Binding affinity at Dopamine receptor D1 in rat neostriatum by [3H]-SCH- 23390 displacement. B 6 pKi >1000 nM Ki J. Med. Chem. (1996) 39: 4238-4246 [PMID:8863801]
ChEMBL Binding Affinity was determined against Dopamine receptor D1 in rat striatal membranes using [3H]- SCH 23390 radioligand. B 6.38 pKi 416.87 nM Ki J. Med. Chem. (2000) 43: 599-608 [PMID:10691686]
ChEMBL Binding affinity against Dopamine receptor D1 in rat striatal membranes using [3H]SCH-23390 B 6.51 pKi 309.03 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 2371-2376
ChEMBL Displacement of [3H]fenoldopam from Dopamine receptor D1 of rat striatum membranes B 6.82 pKi 150 nM Ki J. Med. Chem. (1986) 29: 1904-1912 [PMID:3761310]
ChEMBL Inhibitory activity against [3H]-SCH- 23390 in Rat Striatal membrane B 5.43 pIC50 3700 nM IC50 J. Med. Chem. (1992) 35: 4408-4414 [PMID:1360027]
ChEMBL Compound was evaluated for the inhibition of [3H]-SCH- 23390 binding to Dopamine receptor D1 of rat striatal membranes B 5.52 pIC50 3000 nM IC50 J. Med. Chem. (1990) 33: 2408-2412 [PMID:1975274]
ChEMBL Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum B 6.1 pIC50 800 nM IC50 J. Med. Chem. (1990) 33: 1756-1764 [PMID:1971308]
ChEMBL Effective concentration was determined for the adenylate cyclase activity in rat striatal tissue as a measure of Dopamine receptor D1 functional activity F 5.3 pEC50 5000 nM EC50 J. Med. Chem. (1996) 39: 285-296 [PMID:8568818]
ChEMBL Dopamine receptor D1 agonist efficacy was measured with stimulation of dopamine-sensitive rat adenylate cyclase in caudate membranes F 5.46 pEC50 3500 nM EC50 J. Med. Chem. (1987) 30: 1166-1176 [PMID:2955118]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D2S B 4.82 pKi 15000 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding Affinity was determined in the presence of 100 micro M Gpp(NH)p for decoupling of the ternary complex of Compound to Dopamine receptor D2L B 4.82 pKi 15000 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Affinity towards Dopamine receptor D2 B 5.1 pKi 7940 nM Ki J. Med. Chem. (1998) 41: 4385-4399 [PMID:9784114]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 5.43 pKi 3690 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Displacement of [3H]-NPA from dopamine D2L receptor (unknown origin) expressed in CHO cell membranes B 5.47 pKi 3420 nM KiL J. Med. Chem. (2013) 56: 9199-9221 [PMID:24138311]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor at low affinity state expressed in HEK293 cells B 5.68 pKi 2100 nM Ki J. Med. Chem. (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL Displacement of [3H]raclopride from human dopamine D2L receptor expressed in HEK293 cells by scintillation counting analysis B 5.68 pKi 2100 nM Ki Bioorg. Med. Chem. (2013) 21: 4143-4150 [PMID:23727194]
ChEMBL Displacement of [3H]raclopride from human D2L receptor expressed in HEK293 cells B 5.68 pKi 2100 nM Ki Eur. J. Med. Chem. (2012) 55: 255-261 [PMID:22846798]
ChEMBL Binding Affinity was tested on low Affinity Site of Dopamine receptor D2L B 5.72 pKi 1900 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding Affinity of Compound of Dopamine receptor D2S B 5.96 pKi 1100 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Displacement of [3H]raclopride from human dopamine D2A receptors expressed in LtK cells B 6.12 pKi 759 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2167-2172 [PMID:10465538]
ChEMBL Inhibition of [3H]raclopride binding to Dopamine receptor D2 B 6.24 pKi 572 nM Ki J. Med. Chem. (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL Displacement of [3H]spiperone from human D2long receptor expressed in CHO cells B 6.35 pKi 450 nM Ki J. Med. Chem. (2008) 51: 6829-6838 [PMID:18834111]
ChEMBL Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells B 6.37 pKi 422 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Displacement of [3H]spiperone from human D2short receptor expressed in CHO cells B 6.44 pKi 360 nM Ki J. Med. Chem. (2008) 51: 6829-6838 [PMID:18834111]
ChEMBL Binding affinity against cloned human Dopamine receptor D2 using [3H]spiperone as radioligand transfected in HEK cells B 6.59 pKi 260 nM Ki J. Med. Chem. (1995) 38: 3445-3447 [PMID:7658429]
ChEMBL Displacement of [3H]spiperone from human dopamine D2long receptor expressed in CHO cells B 6.72 pKi 190 nM Ki Bioorg. Med. Chem. (2013) 21: 1680-1684 [PMID:23428965]
ChEMBL Displacement of [3H]spiperone from human dopamine D2short receptor expressed in CHO cells B 6.96 pKi 110 nM Ki Bioorg. Med. Chem. (2013) 21: 1680-1684 [PMID:23428965]
GtoPdb - - 7.2 pKi - - - J Pharmacol Exp Ther (1994) 268: 417-26 [PMID:8301582];
Neuroreport (1995) 6: 329-332 [PMID:7756621];
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]
ChEMBL Displacement of [3H]-NPA from dopamine D2L receptor (unknown origin) expressed in CHO cell membranes B 7.24 pKi 58 nM KiH J. Med. Chem. (2013) 56: 9199-9221 [PMID:24138311]
ChEMBL Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells B 7.32 pKi 48 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2L B 7.38 pKi 42 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D2S B 7.47 pKi 34 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding affinity on High Affinity Site of Dopamine receptor D2L B 7.7 pKi 20 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Binding Affinity on High Affinity Site of Dopamine receptor D2S B 7.77 pKi 17 nM Ki J. Med. Chem. (2000) 43: 756-762 [PMID:10691700]
ChEMBL Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D2 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis B 7.8 pKi 16 nM Ki J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL Displacement of [3H]7-OH-DPAT from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 8.06 pKi 8.73 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Displacement of [3H]-NPA from dopamine D2L receptor (unknown origin) expressed in CHO cell membranes B 8.1 pKi 8 nM Ki J. Med. Chem. (2013) 56: 9199-9221 [PMID:24138311]
ChEMBL Displacement of [3H]spiperone from human dopamine D2 receptor at high affinity state expressed in HEK293 cells B 8.54 pKi 2.9 nM Ki J. Med. Chem. (2010) 53: 2510-2520 [PMID:20155917]
ChEMBL Displacement of [3H]quinpirole from Dopamine receptor D2 B 8.72 pKi 1.89 nM Ki J. Med. Chem. (1996) 39: 4421-4429 [PMID:8893836]
ChEMBL Displacement of [3H]quinpirole from human dopamine D2A receptors expressed in LtK cells B 8.72 pKi 1.89 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2167-2172 [PMID:10465538]
ChEMBL Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay F 6.33 pEC50 470 nM EC50 J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Agonist activity at human dopamine D2 short receptor transiently expressed in HEK293 cells co-expressing Galphai2 after 30 mins by [35S]GTPgammaS binding assay F 6.33 pEC50 467.74 nM EC50 J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay B 6.41 pEC50 390 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at human D2 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay B 6.42 pEC50 376 nM EC50 Bioorg Med Chem (2016) 24: 5088-5102 [PMID:27591013]
ChEMBL Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTP gammaS binding assay F 6.62 pEC50 240 nM EC50 ACS Med. Chem. Lett. (2012) 3: 991-996 [PMID:23275802]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis F 6.64 pEC50 227 nM EC50 Bioorg. Med. Chem. (2013) 21: 3164-3174 [PMID:23623679]
ChEMBL Agonist activity at human cloned dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 6.64 pEC50 227 nM EC50 J. Med. Chem. (2012) 55: 5826-5840 [PMID:22642365]
ChEMBL Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-1 recruitment after 15 mins by BRET assay B 6.65 pEC50 226 nM EC50 J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 6.66 pEC50 218 nM EC50 J. Med. Chem. (2014) 57: 1557-1572 [PMID:24471976]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 6.68 pEC50 209 nM EC50 J. Med. Chem. (2010) 53: 2114-2125 [PMID:20146482]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 6.68 pEC50 209 nM EC50 Bioorg. Med. Chem. (2010) 18: 5661-5674 [PMID:20605099]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgamma binding F 6.68 pEC50 209 nM EC50 J. Med. Chem. (2010) 53: 1023-1037 [PMID:20038106]
ChEMBL Agonist activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 6.68 pEC50 209 nM EC50 J. Med. Chem. (2008) 51: 3005-3019 [PMID:18410082]
ChEMBL Agonist activity at human cloned dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 6.68 pEC50 209 nM EC50 J. Med. Chem. (2008) 51: 101-117 [PMID:18072730]
ChEMBL Activity at human dopamine D2L receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding F 6.68 pEC50 209 nM EC50 Bioorg. Med. Chem. (2009) 17: 3923-3933 [PMID:19427222]
ChEMBL Agonist activity at human D2S receptor expressed in HEK293T cell membranes coexpressing Galphao1 assessed as induction of nucleotide exchange preincubated for 30 mins followed by addition of [35S]GTPgammaS measured after 30 mins by [35S]GTPgammaS binding assay B 6.7 pEC50 200 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at human D2 receptor expressed in CHO cells by [35S]GTPgammaS binding assay B 6.74 pEC50 183 nM EC50 J. Med. Chem. (2015) 58: 9179-9195 [PMID:26555041]
ChEMBL Adenylate cyclase assay carried out in LTK cells transfected with human Dopamine receptor D2 B 6.77 pEC50 170 nM EC50 J. Med. Chem. (1995) 38: 3445-3447 [PMID:7658429]
ChEMBL Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of renilla luciferase 2-tagged beta-arrestin-2 recruitment after 15 mins by BRET assay B 6.79 pEC50 163 nM EC50 J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Partial agonist activity at human D2SR expressed in HEK293T cells co-expressing (EA)beta-arrestin2 and GRK2 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay B 6.8 pEC50 160 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at ARMS2-PK2 tagged D2S receptor (unknown origin) expressed in HEK293 cells assessed as induction of EA-tagged beta-arrestin-2 recruitment incubated for 5 hrs measured after 60 mins by PathHunter assay B 6.81 pEC50 156