dopamine [Ligand Id: 940] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL59 (A-dopamine, Dobutamine a, Dopamina, Dopamine, Intropin, Medopa, NSC-173182, Oxytyramine) |
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| 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 |
| synuclein alpha/Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [GtoPdb: 3285] [UniProtKB: P37840] | ||||||||
| ChEMBL | Inhibition of human alpha-synuclein filament formation expressed in Escherichia coli BL21(DE3) cells incubated for 72 hrs by thioflavin S based fluorescence assay | B | 5.15 | pIC50 | 7100 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| ChEMBL | Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 6 days by thioflavin S based fluorescence assay | B | 6.28 | pIC50 | 530 | nM | IC50 | Eur J Med Chem (2019) 167: 10-36 [PMID:30743095] |
| 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 | F | 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 | F | 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] |
| ChEMBL | Agonist activity at human dopamine D1 receptor expressed in HEK-T cells assessed as cAMP production incubated for 15 mins by luciferase based Glosensor assay | F | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| 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 D2 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay | F | 5.46 | pEC50 | 3460 | nM | EC50 | J Med Chem (2023) 66: 12141-12162 [PMID:37646374] |
| 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 | F | 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 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 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 | 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 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 | Agonist activity at human D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by Perkin elmer analysis | B | 6.7 | pEC50 | 200.41 | nM | EC50 | Bioorg Med Chem (2023) 78: 117131-117131 [PMID:36571976] |
| 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 | F | 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 | F | 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 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 7.18 | pEC50 | 66.25 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Partial agonist activity at D2LR-Nluc in HEK293T cells assessed as mGsi-Venus recruitment using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 7.18 | pEC50 | 66.07 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay | F | 7.19 | pEC50 | 65 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human D2 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis | F | 7.24 | pEC50 | 57.1 | nM | EC50 | J Med Chem (2023) 66: 12141-12162 [PMID:37646374] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production | F | 7.37 | pEC50 | 43 | nM | EC50 | Bioorg Med Chem (2008) 16: 3438-3444 [PMID:18313303] |
| ChEMBL | Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production incubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay | F | 7.4 | pEC50 | 40 | nM | EC50 | Eur J Med Chem (2019) 180: 673-689 [PMID:31357129] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as increase of forskolin-induced cAMP production after 20 mins | F | 7.44 | pEC50 | 36 | nM | EC50 | Bioorg Med Chem (2014) 22: 381-392 [PMID:24296012] |
| ChEMBL | Agonist activity at dopamine D2 receptor long isoform (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 min by calcium 4-dye based FLIPR assay | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2018) 61: 10017-10039 [PMID:30383372] |
| ChEMBL | Agonist activity at human D2 receptor expressed in CHO-K1 cells by calcium 4 dye based FLIPR assay | F | 7.74 | pEC50 | 18.2 | nM | EC50 | Eur J Med Chem (2020) 207: 112709-112709 [PMID:32877805] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D2 using FLIPR assay | B | 7.74 | pEC50 | 18 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at human D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 7.74 | pEC50 | 18 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | Agonist activity at ferret D2 receptor in HEK293 cells coexpressing Galphaqo5 by FLIPR | F | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | Agonist activity at recombinant human D2 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | B | 8.11 | pEC50 | 7.7 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at dopamine D2 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay | B | 8.17 | pEC50 | 6.7 | nM | EC50 | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
| ChEMBL | Agonist activity at human D2 receptor transfected in HEK293T cells by BRET based G0 activation assay | B | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai3 after 10 mins by BRET assay | B | 8.35 | pEC50 | 4.5 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay | B | 8.4 | pEC50 | 3.98 | nM | EC50 | US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004) |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai2 after 10 mins by BRET assay | B | 8.41 | pEC50 | 3.9 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged Galphai1 after 10 mins by BRET assay | B | 8.55 | pEC50 | 2.8 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells assessed as increase in calcium flux incubated for 60 mins at 37 degC followed by 15 mins incubation under room temperature measured after 20 secs for 100 secs by calcium-4 dye based FLIPR assay | F | 9 | pEC50 | 0.99 | nM | EC50 | Bioorg Med Chem (2019) 27: 2100-2111 [PMID:30981605] |
| ChEMBL | Agonist activity at D2R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay | F | 9.1 | pEC50 | 0.8 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoB after 10 mins by BRET assay | B | 9.11 | pEC50 | 0.78 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| ChEMBL | Agonist activity at D2 receptor (unknown origin) expressed in CHOK1 cells co-expressing G-alpha 15 by fluo-4 dye based FLIPR assay | B | 9.16 | pEC50 | 0.69 | nM | EC50 | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| ChEMBL | Agonist activity at N-terminal flag-tagged D2S receptor (unknown origin) expressed in HEK293 cells coexpressing renilla luciferase 2-tagged GalphaoA after 10 mins by BRET assay | B | 9.17 | pEC50 | 0.67 | nM | EC50 | J Med Chem (2017) 60: 2908-2929 [PMID:28248104] |
| Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288] | ||||||||
| ChEMBL | Affinity for Dopamine receptor D2 was evaluated from the ability to displace [3H]spiroperidol from homogenized bovine pituitary | B | 5.63 | pKd | 2.35 | uM | K Bind | J Med Chem (1986) 29: 1615-1627 [PMID:2875183] |
| ChEMBL | Low binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol | B | 5.47 | pKi | 3380 | nM | Ki | J Med Chem (1989) 32: 961-968 [PMID:2565402] |
| ChEMBL | Compound was tested for inhibition of [3H]spiroperidol binding against Dopamine receptor D2 | B | 5.63 | pKi | 2350 | nM | Ki | J Med Chem (1986) 29: 1904-1912 [PMID:3761310] |
| ChEMBL | Binding Affinity was determined for its ability to displace the radioligand [3H]spiperone from low Affinity Site of Bovine dopamine receptor D2. | B | 5.8 | pKi | 1600 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, low affinity site | B | 5.82 | pKi | 1520 | nM | Ki | J Med Chem (1998) 41: 4933-4938 [PMID:9836610] |
| ChEMBL | Tested for binding affinity against Dopamine receptor D2 like from bovine striatum membranes by using [3H]YM-09151-2 radioligand | B | 6.21 | pKi | 617 | nM | Ki | J Med Chem (1998) 41: 4933-4938 [PMID:9836610] |
| ChEMBL | Binding Affinity was tested on relative proportion of high Affinity Site of Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]spiperone at the binding site. | B | 7.29 | pKi | 51 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | High binding affinity for dopamine D-2 receptor from bovine anterior pituitary membrane, using radioligand [3H]spiroperidol | B | 7.47 | pKi | 34 | nM | Ki | J Med Chem (1989) 32: 961-968 [PMID:2565402] |
| ChEMBL | Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, high affinity site | B | 7.83 | pKi | 14.9 | nM | Ki | J Med Chem (1998) 41: 4933-4938 [PMID:9836610] |
| ChEMBL | Binding Affinity was tested on high Affinity Site of Bovine Dopamine D2 Receptor. Tested for ability to displace the radioligand [3H]spiperone was tested | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Binding Affinity on high Affinity Site of Bovine dopamine receptor D2. Tested for ability to displace the radioligand [3H]pramipexole was tested | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | In vitro binding affinity towards Dopamine D2 receptor using [3H]spiperone as radioligand | B | 5.1 | pIC50 | 8000 | nM | IC50 | Bioorg Med Chem Lett (1991) 1: 403-406 |
| ChEMBL | Displacement of [3H]spiroperidol from homogenized bovine pituitary Dopamine receptor D2 | B | 5.33 | pIC50 | 4700 | nM | IC50 | J Med Chem (1987) 30: 1166-1176 [PMID:2955118] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. | B | 4.31 | pKd | 49000 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | In vitro affinity at mutant D2 receptor (S194A) in C6 (glioma) cell membranes. | B | 4.43 | pKd | 37000 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | Equilibrium dissociation constant against recombinant Dopamine receptor D2A expressed in COS7 cells | B | 4.77 | pKd | 17000 | nM | Kd | J Med Chem (1996) 39: 850-859 [PMID:8632409] |
| ChEMBL | In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. | B | 5.21 | pKd | 6200 | nM | Kd | J Med Chem (2000) 43: 3005-3019 [PMID:10956209] |
| ChEMBL | Binding affinity at Dopamine receptor D2 in rat striatal homogenate by [3H]-spiperone displacement. | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (1996) 39: 4238-4246 [PMID:8863801] |
| ChEMBL | Displacement of [3H]spiperone from rat D2L dopamine receptor expressed in HEK293 cell membranes after 1 hr | B | 6 | pKi | 990 | nM | Ki | Bioorg Med Chem (2016) 24: 5088-5102 [PMID:27591013] |
| ChEMBL | Displacement of [3H]Spiroperidol from cloned rat dopamine D2L receptor expressed in HEK293 cells by liquid scintillation counting analysis | B | 6 | pKi | 990 | nM | Ki | J Med Chem (2015) 58: 9179-9195 [PMID:26555041] |
| ChEMBL | Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand | B | 6.07 | pKi | 843 | nM | Ki | J Med Chem (1990) 33: 171-178 [PMID:2136916] |
| ChEMBL | Binding Affinity was determined against Dopamine receptor D2 in rat striatal membranes using [3H]- spiperone radioligand. | B | 6.14 | pKi | 724.44 | nM | Ki | J Med Chem (2000) 43: 599-608 [PMID:10691686] |
| GtoPdb | - | - | 6.4 | pKi | - | - | - |
Nature (1990) 347: 146-51 [PMID:1975644]; Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
| ChEMBL | Inhibitory constant against binding of [125I]- IBZM to rat striatal membrane | B | 6.53 | pKi | 296 | nM | Ki | J Med Chem (1988) 31: 1039-1043 [PMID:2966245] |
| ChEMBL | Displacement of [3H]raclopride from rat dopamine D2short receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 6.71 | pKi | 197 | nM | Ki | Bioorg Med Chem (2009) 17: 4756-4762 [PMID:19454369] |
| ChEMBL | Binding affinity against Dopamine receptor D2 in rat striatal membranes using [3H]spiperone | B | 6.98 | pKi | 104.71 | nM | Ki | Bioorg Med Chem Lett (1995) 5: 2371-2376 |
| ChEMBL | In vitro affinity against Dopamine receptor D2 using [3H]DP-5,6-ADTN radioligand in rat striatal homogenate. | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1986) 29: 1889-1895 [PMID:3761308] |
| ChEMBL | Concentration that produces 50 % displacement of specific [3H]spiroperidol binding to rat caudate membrane preparations. | B | 5.27 | pIC50 | 5340 | nM | IC50 | J Med Chem (1984) 27: 28-35 [PMID:6317860] |
| ChEMBL | Inhibitory activity against [3H]spiperone in Rat Striatal membrane | B | 5.46 | pIC50 | 3500 | nM | IC50 | J Med Chem (1992) 35: 4408-4414 [PMID:1360027] |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D2 trunk/D2 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 5.49 | pIC50 | 3260 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D2 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 5.5 | pIC50 | 3140 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Neuroleptic activity in terms of [3H]spiroperidol binding in rat striatal membrane to Dopamine receptor D2 | B | 5.52 | pIC50 | 3045 | nM | IC50 | J Med Chem (1991) 34: 194-197 [PMID:1671414] |
| ChEMBL | Compound was evaluated for the inhibition of [3H]spiperone binding to Dopamine receptor D2 of rat striatal membranes | B | 5.66 | pIC50 | 2200 | nM | IC50 | J Med Chem (1990) 33: 2408-2412 [PMID:1975274] |
| ChEMBL | Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain | B | 5.73 | pIC50 | 1860 | nM | IC50 | J Med Chem (1988) 31: 2027-2033 [PMID:3172140] |
| ChEMBL | Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (1988) 31: 2027-2033 [PMID:3172140] |
| ChEMBL | Displacement of [3H]- -spiperone from Dopamine receptor D2 in rat striatum | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (1990) 33: 1756-1764 [PMID:1971308] |
| ChEMBL | Compound was for its ability to displace [3H]haloperidol binding to rat striatal Dopamine receptor D2 | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (1986) 29: 186-193 [PMID:3950903] |
| ChEMBL | Agonist activity at rat dopamine D2short receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting | F | 5.85 | pEC50 | 1425 | nM | EC50 | Bioorg Med Chem (2009) 17: 4756-4762 [PMID:19454369] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D2 using FLIPR assay | B | 8.1 | pEC50 | 8 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 8.3 | pEC50 | 5 | nM | EC50 | J Med Chem (2006) 49: 6848-6857 [PMID:17154515] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D2 using FLIPR assay | B | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at rat D2 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D3 F6.51W mutant receptor expressed in human HEK293 cells | B | 4.1 | pKi | >80000 | nM | Ki | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Binding Affinity was tested on low Affinity Site of Dopamine receptor D3 | B | 5.8 | pKi | 1600 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Displacement of [3H]spiperone from human D3 D3.32E mutant receptor expressed in human HEK293 cells | B | 5.96 | pKi | 1100 | nM | Ki | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 6.53 | pKi | 293 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| 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 D3 | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 6.62 | pKi | 240 | nM | Ki | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Displacement of [3H]spiperone from human wild type D3 receptor expressed in human HEK293 cells | B | 7.14 | pKi | 72 | nM | Ki | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Binding Affinity was tested on relative proportion of High Affinity Site of Dopamine receptor D3 | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| GtoPdb | - | - | 7.3 | 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]; Nature (1990) 347: 146-51 [PMID:1975644] |
| ChEMBL | Binding Affinity was tested on the high affinity site of Dopamine receptor D3 | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2013) 21: 1680-1684 [PMID:23428965] |
| ChEMBL | Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Displacement of [3H]raclopride from human D3 receptor expressed in HEK293 cells | B | 7.82 | pKi | 15 | nM | Ki | Eur J Med Chem (2012) 55: 255-261 [PMID:22846798] |
| ChEMBL | Displacement of [3H]raclopride from human dopamine D3 receptor expressed in HEK293 cells by scintillation counting analysis | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2013) 21: 4143-4150 [PMID:23727194] |
| ChEMBL | Displacement of [3H]raclopride from Dopamine receptor D3 | B | 7.88 | pKi | 13.2 | nM | Ki | J Med Chem (1996) 39: 4421-4429 [PMID:8893836] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 8.12 | pKi | 7.58 | nM | Ki | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Displacement of [3H]-(R)-(+)-7-OH-DPAT from human dopamine D3 receptor expressed in HEK293 cell membranes after 90 mins by micro beta scintillation counting analysis | B | 8.53 | pKi | 2.97 | nM | Ki | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Agonist activity at RLuc8-fused human D3R Y198A/Y365A double mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 6.09 | pEC50 | 820 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at RLuc8-fused human D3R Y198A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at RLuc8-fused human D3R Y365A mutant expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 7.48 | pEC50 | 33 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 7.97 | pEC50 | 10.6 | nM | EC50 | J Med Chem (2014) 57: 1557-1572 [PMID:24471976] |
| ChEMBL | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | F | 8.03 | pEC50 | 9.33 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human dopamine D3 receptor transiently expressed in HEK293 cells co-expressing Galphao1 after 30 mins by [35S]GTPgammaS binding assay | F | 8.03 | pEC50 | 9.3 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.07 | pEC50 | 8.57 | nM | EC50 | J Med Chem (2012) 55: 5826-5840 [PMID:22642365] |
| ChEMBL | Activity at human dopamine D3 receptor expressed in AtT cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.07 | pEC50 | 8.53 | nM | EC50 | Bioorg Med Chem (2009) 17: 3923-3933 [PMID:19427222] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in mouse AtT-20 cells assessed as stimulation of [35S]GTPgamma binding | F | 8.07 | pEC50 | 8.53 | nM | EC50 | J Med Chem (2010) 53: 1023-1037 [PMID:20038106] |
| ChEMBL | Agonist activity at human cloned dopamine D3 receptor expressed in AtT-20 cells assessed as stimulation of [35S]GTP-gamma-S binding | F | 8.07 | pEC50 | 8.53 | nM | EC50 | J Med Chem (2008) 51: 101-117 [PMID:18072730] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in mouse ATt-20 cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.07 | pEC50 | 8.53 | nM | EC50 | J Med Chem (2008) 51: 3005-3019 [PMID:18410082] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis | F | 8.12 | pEC50 | 7.64 | nM | EC50 | Bioorg Med Chem (2013) 21: 3164-3174 [PMID:23623679] |
| ChEMBL | Agonist activity at human D3 dopamine receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.14 | pEC50 | 7.26 | nM | EC50 | Bioorg Med Chem (2016) 24: 5088-5102 [PMID:27591013] |
| ChEMBL | Agonist activity at human D3R expressed in CHOK1 cells assessed as induction of beta-arrestin recruitment measured after 90 mins by beta-galactosidase based PathHunter assay | B | 8.19 | pEC50 | 6.4 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at human D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by Perkin elmer analysis | B | 8.21 | pEC50 | 6.13 | nM | EC50 | Bioorg Med Chem (2023) 78: 117131-117131 [PMID:36571976] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay | F | 8.21 | pEC50 | 6.1 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human cloned dopamine D3 receptor expressed in CHO cells by [35S]GTP gammaS binding assay | F | 8.24 | pEC50 | 5.8 | nM | EC50 | ACS Med Chem Lett (2012) 3: 991-996 [PMID:23275802] |
| ChEMBL | Agonist activity at human D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.27 | pEC50 | 5.34 | nM | EC50 | J Med Chem (2015) 58: 9179-9195 [PMID:26555041] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 8.32 | pEC50 | 4.76 | nM | EC50 | J Med Chem (2010) 53: 2114-2125 [PMID:20146482] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding | F | 8.32 | pEC50 | 4.76 | nM | EC50 | Bioorg Med Chem (2010) 18: 5661-5674 [PMID:20605099] |
| ChEMBL | Agonist activity at human D3 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis | F | 8.37 | pEC50 | 4.27 | nM | EC50 | J Med Chem (2023) 66: 12141-12162 [PMID:37646374] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in pathHunter cells assessed as beta-arrestin translocation activity incubated for 90 to 180 mins by pathHunter microplate based TANGO assay | F | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| ChEMBL | Agonist activity at human D3R expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 5 mins in presence of beta-adrenergic blocker propranolol and coelenterazine H by CAMYEL BRET assay | F | 8.46 | pEC50 | 3.5 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at human D3R stably expressed in CHOK1 cells assessed as increase in ERK1/2 phosphorylation measured after 15 mins by AlphaScreen surefire assay | B | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at recombinant human D3 receptor expressing in CHOp cells assessed as receptor mediated stimulation of mitogenesis measured as [3H]thymidine incorporation after 24 hrs by scintillation spectrometry | B | 8.57 | pEC50 | 2.7 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at RLuc8-fused human D3R expressed in HEK293 cells co-expressing N-terminal Venus-tagged beta-arrestin2 and GRK3 assessed as induction of beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8.64 | pEC50 | 2.3 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at dopamine D3 receptor (unknown origin) expressed in HEK293 cells assessed as induction of calcium flux after 60 mins by calcium 4-dye based FLIPR assay | F | 8.68 | pEC50 | 2.1 | nM | EC50 | J Med Chem (2018) 61: 10017-10039 [PMID:30383372] |
| ChEMBL | Agonist activity at human D3 receptor transfected in HEK293T cells by BRET based G0 activation assay | B | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Agonist activity at dopamine D3 receptor (unknown origin) expressed in CHOK1 cells coexpressing Galpha15 by FLIPR assay | B | 8.74 | pEC50 | 1.8 | nM | EC50 | J Med Chem (2013) 56: 4671-4690 [PMID:23675993] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in HEK-T cells assessed as cAMP production incubated for 30 mins in the presence of NKH-477 by fluorescence based analysis | F | 8.8 | pEC50 | 1.6 | nM | EC50 | J Med Chem (2023) 66: 10060-10079 [PMID:37421373] |
| ChEMBL | Agonist activity at RLuc8-fused Go-coupled human D3R expressed in HEK293 cells untagged beta1 and mVenus-tagged gamma2 measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8.96 | pEC50 | 1.1 | nM | EC50 | J Med Chem (2020) 63: 5526-5567 [PMID:32342685] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in HEK293T cells assessed as GalphaoA activation preincubated for 5 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | F | 9.05 | pEC50 | 0.89 | nM | EC50 | J Med Chem (2021) 64: 7778-7808 [PMID:34011153] |
| ChEMBL | Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 9.17 | pEC50 | 0.68 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Agonist activity at SNAP-tagged human D3R receptor transfected in HEK293T cells coexpressing wild type Galpha-oA, venus-tagged Gbeta-1 (156 to 239 residues), venus-tagged Ggamma2 (1 to 155 residues) and Rluc8 fused masGRK3ct assessed as Galpha-oA activation using coelenterazine as substrate incubated for 40 mins by BRET based GPA assay | F | 9.17 | pEC50 | 0.68 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Agonist activity at human Gi/o-coupled D3 receptor expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol addition by Glosensor-based luminescence assay | F | 9.96 | pEC50 | 0.11 | nM | EC50 | J Med Chem (2020) 63: 4579-4602 [PMID:32282200] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| ChEMBL | Displacement of [3H]Spiroperidol from cloned rat dopamine D3 receptor expressed in HEK293 cells by liquid scintillation counting analysis | B | 7 | pKi | 101 | nM | Ki | J Med Chem (2015) 58: 9179-9195 [PMID:26555041] |
| ChEMBL | Displacement of [3H]spiperone from rat D3 dopamine receptor expressed in HEK293 cell membranes after 1 hr | B | 7 | pKi | 101 | nM | Ki | Bioorg Med Chem (2016) 24: 5088-5102 [PMID:27591013] |
| ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 7.31 | pKi | 49.3 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
| ChEMBL | Binding affinity which represents concentration giving half-maximal inhibition of [3H]7-OH-DPAT binding to Dopamine receptor D3 in rat tissue homogenate | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (1998) 41: 3763-3772 [PMID:9748351] |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) chimeric dopamine D3 trunk/D3 tail receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 6.91 | pIC50 | 124 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Displacement of [3H]nemonapride from Rattus norvegicus (rat) wild type dopamine D3 receptor transfected in african green monkey COS7 cells after 1 hr by beta scintillation counting | B | 6.95 | pIC50 | 111 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| 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 D4.4 | B | 7.01 | pKi | 97 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Binding Affinity was tested on low Affinity Site of Dopamine receptor D4.4 | B | 7.21 | pKi | 62 | 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 D4.4 | B | 7.24 | pKi | 57 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | Nature (1991) 350: 610-4 [PMID:1840645] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 8.05 | pKi | 8.9 | nM | Ki | Bioorg Med Chem (2013) 21: 1680-1684 [PMID:23428965] |
| ChEMBL | Displacement of [3H]spiperone from human D4 receptor expressed in CHO cells | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Binding Affinity was tested on the high affinity site of Dopamine receptor D4.4 | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2000) 43: 756-762 [PMID:10691700] |
| ChEMBL | Agonist activity at human D4 receptor stably expressed in CHO-K1 cells assessed as beta arrestin recruitment preincubated for 90 mins by tropix-gal screen substrate based luminescence analysis | F | 6.94 | pIC50 | 114 | nM | IC50 | J Med Chem (2023) 66: 12141-12162 [PMID:37646374] |
| ChEMBL | Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as beta arrestin-2 recruitment measured after 2.5 mins by BRET assay | F | 6.57 | pEC50 | 269.15 | nM | EC50 | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as mVenus-fused beta-arrestin2 recruitment after 2 mins by BRET assay | B | 7.04 | pEC50 | 91.2 | nM | EC50 | J Med Chem (2018) 61: 3712-3725 [PMID:29589445] |
| ChEMBL | Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as Gi protein activation measured after 2.5 mins by BRET assay | F | 7.68 | pEC50 | 20.89 | nM | EC50 | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Agonist activity at D4R (unknown origin) expressed in human HEK293T cells assessed as G0 protein activation measured after 2.5 mins by BRET assay | F | 7.83 | pEC50 | 14.79 | nM | EC50 | J Med Chem (2022) 65: 12124-12139 [PMID:36098685] |
| ChEMBL | Agonist activity at human SP/Myc epitope-tagged dopamine D4 receptor expressed in HEK293T cells assessed as RLuc8-fused Galphai1 activation after 2 mins by BRET assay | B | 7.91 | pEC50 | 12.3 | nM | EC50 | J Med Chem (2018) 61: 3712-3725 [PMID:29589445] |
| ChEMBL | Activity at human dopamine D4.4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production | F | 8 | pEC50 | 10 | nM | EC50 | J Med Chem (2006) 49: 6848-6857 [PMID:17154515] |
| ChEMBL | Agonist activity at human D4 receptor stably expressed in CHO-K1 cells assessed as inhibition of forskolin stimulated cAMP production incubated for 30 mins by Lance ultra cAMP assay | F | 8.42 | pEC50 | 3.78 | nM | EC50 | J Med Chem (2023) 66: 12141-12162 [PMID:37646374] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with human Dopamine receptor D4 using FLIPR assay | B | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at human D4.4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| ChEMBL | Agonist activity at D4R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gi-cAMP Glosensor assay | F | 8.74 | pEC50 | 1.8 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| D4 receptor/Dopamine D4 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3361] [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| GtoPdb | - | - | 7.4 | pKi | - | - | - | Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with ferret Dopamine receptor D4 using FLIPR assay | B | 8.57 | pEC50 | 2.7 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | In vitro effective concentration tested on HEK293 cells co-transfected with rat Dopamine receptor D4 using FLIPR assay | B | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2004) 47: 3853-3864 [PMID:15239663] |
| ChEMBL | Agonist activity at rat D4 receptor in HEK293 cells coexpressing G-alpha-qo5 by FLIPR | F | 8.62 | pEC50 | 2.4 | nM | EC50 | J Med Chem (2006) 49: 7450-7465 [PMID:17149874] |
| D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918] | ||||||||
| ChEMBL | Inhibitory constant for [3H]SCH-23390 binding to Dopamine receptor D1-like of porcine striatal membranes | B | 5.61 | pKi | 2440 | nM | Ki | J Med Chem (2005) 48: 2646-2654 [PMID:15801855] |
| GtoPdb | - | - | 6.6 | pKi | - | - | - | Nature (1991) 350: 614-9 [PMID:1826762] |
| ChEMBL | Agonist activity at D5R (unknown origin) expressed in HEK293 cells assessed as effect on cAMP accumulation incubated for 10 mins by Gs-cAMP Glosensor assay | F | 8.7 | pEC50 | 2 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Displacement of [125I]RT155 binding in HEK cells expressing human DAT | B | 5.19 | pKi | 6400 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
| ChEMBL | Inhibition of [3H]dopamine uptake in HEK cells expressing human DAT | B | 6.34 | pIC50 | 460 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibitory constant towards reuptake of [125I]-12 from dopamine transporter in rat striatal membranes | B | 5.3 | pKi | >5000 | nM | Ki | J Med Chem (1994) 37: 1535-1542 [PMID:8182712] |
| ChEMBL | Inhibition of dopamine transporter-mediated [3H]dopamine uptake in Wistar rat striatal synaptosomes by liquid scintillation spectrometry | B | 6.7 | pIC50 | 200 | nM | IC50 | J Nat Prod (1995) 58: 1475-1484 [PMID:8676127] |
| lysine demethylase 4E/Lysine-specific demethylase 4D-like in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293226] [GtoPdb: 2679] [UniProtKB: B2RXH2] | ||||||||
| ChEMBL | Inhibition of N-terminal His-6-tagged human JMJD2E (1 to 337 residues) expressed in Escherichia coli by MALDI-TOF/MS analysis | B | 5.52 | pIC50 | 3000 | nM | IC50 | Medchemcomm (2012) 3: 135-161 |
| MT1 receptor/Melatonin receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1945] [GtoPdb: 287] [UniProtKB: P48039] | ||||||||
| ChEMBL | Displacement of 2-[125I]iodomelatonin from human Melatonin receptor type 1A expressed in CHO cells | B | 5.15 | pKi | 7100 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2409-2414 |
| MT2 receptor/Melatonin receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1946] [GtoPdb: 288] [UniProtKB: P49286] | ||||||||
| ChEMBL | Inhibition of 2-[125I]iodomelatonin binding to human Melatonin receptor type 1B expressed in CHO cells | B | 5.04 | pKi | 9100 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 2409-2414 |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Displacement of [125I]RT155 binding in HEK cells expressing human NET | B | 4.55 | pKi | >28000 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
| ChEMBL | Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET | B | 8.18 | pIC50 | 6.63 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Inhibition of [3H]5-HT uptake in HEK cells expressing human SERT | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4133-4137 [PMID:14592523] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in OCT3-expressing HRPE cells | F | 4.21 | pIC50 | 62000 | nM | IC50 | J Biol Chem (1998) 273: 32776-32786 [PMID:9830022] |
| TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0] | ||||||||
| ChEMBL | Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis | F | 5.77 | pEC50 | 1710 | nM | EC50 | ACS Med Chem Lett (2022) 13: 92-98 [PMID:35047111] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FYN in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of peptide EPQ (pY) EEIPI binding to Fyn protein kinase SH2 domain at 100 uM (no inhibition) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 113-116 |
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]
