quinpirole [Ligand Id: 2] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL240773 (Quinpirole)
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • D2 receptor/mGlu5 receptor/D(2) dopamine receptor/Metabotropic glutamate receptor 5 in Human [ChEMBL: CHEMBL4296096] [GtoPdb: 215293] [UniProtKB: P14416P41594]
  • D2 receptor/mGlu5 receptor in Rat [GtoPdb: 215293] [UniProtKB: P61169P31424]
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  • 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]
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  • 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]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells B 4 pKi 100000 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
D2 receptor/mGlu5 receptor/D(2) dopamine receptor/Metabotropic glutamate receptor 5 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4296096] [GtoPdb: 215293] [UniProtKB: P14416P41594]
GtoPdb - - 7.7 pKi - - - Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
Nature (1990) 347: 146-51 [PMID:1975644];
Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822];
Nature (1991) 350: 610-4 [PMID:1840645];
Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990]
ChEMBL Agonist activity at human dopamine D2 receptor /mGluR5a (unknown origin) expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay B 8.72 pEC50 1.9 nM EC50 J Med Chem (2018) 61: 8212-8225 [PMID:30180563]
D2 receptor/mGlu5 receptor in Rat [GtoPdb: 215293] [UniProtKB: P61169P31424]
GtoPdb - - 5.2 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor expressed in HEK293 cells by competitive binding assay B 4.06 pKi 87000 nM Ki J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells B 5 pKi >10000 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Displacement of [3H]SCH23390 from human dopamine D1 receptor transfected in HEK293 cells after 1 hr by scintillation counting analysis B 5.06 pKi 8700 nM Ki J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells B 5.06 pKi 8700 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Binding affinity (high) towards human dopamine receptor 2 long against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells B 7.2 pKi 63 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor in porcine striatal membranes B 4.06 pKi 87000 nM Ki J. Med. Chem. (2013) 56: 5130-5141 [PMID:23730937]
ChEMBL Displacement of [3H]SCH23390 from dopamine D1 receptor in pig striatal membranes B 4.14 pKi 72000 nM Ki J. Med. Chem. (2009) 52: 6860-6870 [PMID:19807103]
Dopamine D1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2967] [UniProtKB: Q95136]
ChEMBL Inhibition constant against [3H]SCH-23390 binding to Dopamine receptor D1 in bovine striatal membranes B 4.7 pKi >20000 nM Ki J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Binding affinity (low) towards bovine dopamine receptor 1 by using [3H]-SCH- 23390 (0.3 nM) as radioligand B 4.7 pKi >20000 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Displacement of [3H]- #NAME? from binding Dopamine receptor D1 in rat striatum B 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (1990) 33: 1756-1764 [PMID:1971308]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 long receptor expressed in CHO cells; Low binding affinity B 4.51 pKi 31000 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2533-2536 [PMID:11549463]
ChEMBL In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 short receptor expressed in CHO cells; Low binding affinity B 5.4 pKi 4000 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2533-2536 [PMID:11549463]
ChEMBL Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells B 5.51 pKi 3100 nM Ki J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Binding affinity (low) towards human dopamine receptor 2 (long) against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells B 5.51 pKi 3100 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Binding affinity (low) towards human dopamine receptor 2 short against radioligand [3H]spiperone, expressed in Chinese hamster ovary cells B 5.52 pKi 3000 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2S expressed in CHO cells B 5.52 pKi 3000 nM Ki J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 5.53 pKi 2950 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Affinity towards Dopamine receptor D2 B 5.59 pKi 2570 nM Ki J. Med. Chem. (1998) 41: 4385-4399 [PMID:9784114]
ChEMBL Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells B 5.93 pKi 1185 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D2long receptor expressed in CHO cells B 6.02 pKi 950 nM Ki J. Med. Chem. (2009) 52: 6860-6870 [PMID:19807103]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D2short receptor expressed in CHO cells B 6.06 pKi 870 nM Ki J. Med. Chem. (2009) 52: 6860-6870 [PMID:19807103]
ChEMBL Displacement of [3H]spiperone from human D2L receptor expressed in CHO cells B 6.59 pKi 260 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Displacement of [3H]spiperone from human dopamine D2L receptor expressed in CHO cells B 6.59 pKi 260 nM Ki J. Med. Chem. (2013) 56: 5130-5141 [PMID:23730937]
ChEMBL Displacement of [3H]Spiperone from human dopamine D2 long receptor expressed in CHO cells by competitive binding assay B 6.59 pKi 260 nM Ki J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Displacement of [3H]spiperone from human dopamine D2L receptor transfected in CHO cells after 1 hr by scintillation counting analysis B 6.59 pKi 260 nM Ki J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells B 7.15 pKi 70 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Displacement of [3H]Spiperone from human dopamine D2 short receptor expressed in CHO cells by competitive binding assay B 7.15 pKi 70 nM Ki J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Displacement of [3H]spiperone from human dopamine D2S receptor expressed in CHO cells B 7.15 pKi 70 nM Ki J. Med. Chem. (2013) 56: 5130-5141 [PMID:23730937]
ChEMBL Displacement of [3H]spiperone from human dopamine D2S receptor transfected in CHO cells after 1 hr by scintillation counting analysis B 7.15 pKi 70 nM Ki J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D2 long in CHO cells B 7.19 pKi 64 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 851-854 [PMID:12617906]
ChEMBL In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 long receptor expressed in CHO cells; high binding affinity B 7.19 pKi 64 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2533-2536 [PMID:11549463]
ChEMBL High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells B 7.2 pKi 63 nM Ki J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL In vitro for its ability to displace [3H]- spiperone from cloned human dopamine D2 short receptor expressed in CHO cells; high binding affinity B 7.28 pKi 52 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2533-2536 [PMID:11549463]
ChEMBL In vitro binding affinity to displace [3H]-spiperone from the cloned human dopamine receptor D2 short in CHO cells B 7.28 pKi 52 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 851-854 [PMID:12617906]
ChEMBL High binding affinity towards human dopamine receptor 2 (short) expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 7.46 pKi 35 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2S expressed in CHO cells B 7.46 pKi 35 nM Ki J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
GtoPdb - - 7.7 pKi - - - Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010];
Eur J Pharmacol (1992) 225: 331-7 [PMID:1354163];
Nature (1990) 347: 146-51 [PMID:1975644];
Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822];
Nature (1991) 350: 610-4 [PMID:1840645];
Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990]
ChEMBL Displacement of [3H]7-OH-DPAT from human dopamine D2L receptor expressed in CHO cells B 7.74 pKi 18 nM Ki J. Med. Chem. (2013) 56: 5130-5141 [PMID:23730937]
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 7.88 pKi 13.1 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 8.25 pKi 5.56 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL Affinity Assay: Each medicament was dissolved in serum-free F12 culture medium containing 100 μM of IBMX. CHO cells which can stably express D2 receptor were pre-incubated at 37° C. for 10 min, and then 10 μM Forskoline and 10 μM Dopanie were added at the same time to react for 10 min. 100 μL, of pre-cooled 1 M of HClO4 was added and the reaction was terminated at 4° C. for 1 hour. 20 μL of 2 M K2CO3 was added to neutralize the reaction. The resulting mixture was centrifugated at 3000 rpm for 15 min, and the precipitate KClO4 was discarded. A certain amount of the supernatant was taken for cAMP detection. Spiperone and Quinpirole were used as positive control. B 6.34 pIC50 462 nM IC50 US-9359372-B2. Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof (2016)
ChEMBL Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay B 5.55 pEC50 2800 nM EC50 J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Intrinsic activity at human dopamine D2L receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay B 5.57 pEC50 2700 nM EC50 J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galphai2 assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay B 5.64 pEC50 2300 nM EC50 J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay B 5.79 pEC50 1621.81 nM EC50 Bioorg. Med. Chem. (2015) 23: 6195-6209 [PMID:26299826]
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 5.79 pEC50 1621.81 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 5.8 pEC50 1600 nM EC50 J. Med. Chem. (2014) 57: 4861-4875 [PMID:24831693]
ChEMBL Intrinsic activity at human dopamine D2S receptor expressed in HEK293 cells co-transfected with Galpha0i assessed as [35S]GTPgammaS binding after 30 mins by [35S]GTPgammaS incorporation assay B 5.8 pEC50 1600 nM EC50 J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Agonist activity at D2 receptor (unknown origin) after 40 mins by [35S]GTP-gammaS binding assay F 6.17 pEC50 680 nM EC50 Bioorg. Med. Chem. (2014) 22: 5838-5846 [PMID:25308766]
ChEMBL Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphao1 by [35S]GTPgammaS binding assay B 6.21 pEC50 616.6 nM EC50 Bioorg. Med. Chem. (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused Galphai1/GFP10-fused Ggamma2 by BRET assay B 6.45 pEC50 353.2 nM EC50 J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL Intrinsic activity against dopamine D2(long) receptor expressed in CHO cells by GTPgammaS assay F 6.48 pEC50 330 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 2955-2959 [PMID:16563764]
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 6.53 pEC50 295 nM EC50 J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
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 6.57 pEC50 270 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at dopamine D2 receptor expressed in HEK293 cells by by [35S]GTPgammaS binding assay F 6.62 pEC50 240 nM EC50 Bioorg. Med. Chem. (2009) 17: 4873-4880 [PMID:19559623]
ChEMBL Intrinsic activity against dopamine D2(short) receptor expressed in CHO cells by GTPgammaS assay F 6.64 pEC50 230 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 2955-2959 [PMID:16563764]
ChEMBL Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control B 6.82 pEC50 151.36 nM EC50 J Nat Prod (2020) 83: 127-133 [PMID:31933369]
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 6.82 pEC50 151 nM EC50 J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Agonist activity at human D2S receptor expressed in CHOK1 cells assessed as inhibition of forskolin induced cAMP production preincubated for 10 mins followed by forskolin addition and measured after 5 mins by HTRF assay relative to control B 6.82 pEC50 150 nM EC50 J Nat Prod (2020) 83: 127-133 [PMID:31933369]
ChEMBL Agonist activity at renilla luciferase-tagged human dopamine D2 receptor expressed in HEK293 cells coexpressing mVenus-fused beta-arrestin 2 assessed as induction of beta-arrestin 2 recruitment by BRET assay B 6.83 pEC50 147.6 nM EC50 J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL Agonist activity at DRD2 Long receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation by bioluminescence assay F 6.85 pEC50 140 nM EC50 J. Med. Chem. (2011) 54: 7911-7919 [PMID:21999579]
ChEMBL Agonist activity at ARMS2-PK-tagged D2S receptor (unknown origin) transfected in HEK293 cells after 5 hrs by beta-arrestin assay B 7.07 pEC50 86 nM EC50 Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Agonist activity at ARMS2-PK2-tagged human dopamine D2S receptor expressed in HEK293 cells co-expressing (EA)-tagged beta arrestin fusion protein assessed as recruitment of beta-arrestin-2 after 5 hrs by chemiluminescence assay B 7.08 pEC50 83 nM EC50 J. Med. Chem. (2015) 58: 2703-2717 [PMID:25734236]
ChEMBL Agonist activity at human D2SR expressed in HEK293 cells incubated for 5 hrs by beta-Arrestin 2 recruitment assay B 7.14 pEC50 73 nM EC50 Bioorg Med Chem (2017) 25: 5613-5628 [PMID:28870802]
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 7.19 pEC50 64 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 assessed as induction of beta-arrestin2 recruitment after 5 hrs by chemiluminescence assay B 7.28 pEC50 52 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Activity at pro-link-tagged D2S-ARMS2PK2 (unknown origin) expressed in HEK293 cells by beta-arrestin-2 recruitment assay B 7.29 pEC50 51 nM EC50 Bioorg. Med. Chem. (2015) 23: 6195-6209 [PMID:26299826]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in HEK293 cells coexpressing renilla luciferase-fused GalphaoA/GFP10-fused Ggamma2 by BRET assay B 7.41 pEC50 38.7 nM EC50 J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
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 7.72 pEC50 19 nM EC50 J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
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 7.8 pEC50 16 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay B 7.96 pEC50 10.9 nM EC50 J Med Chem (2017) 60: 2890-2907 [PMID:28300398]
ChEMBL Intrinsic activity against dopamine D2(short) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay F 8 pEC50 10 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 2955-2959 [PMID:16563764]
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 8.09 pEC50 8.2 nM EC50 J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL In vitro inhibition of forskolin-stimulated cAMP accumulation in GH4C1 cells transfected with the human Dopamine D2 receptor F 8.12 pEC50 7.6 nM EC50 J. Med. Chem. (1994) 37: 4251-4257 [PMID:7990124]
ChEMBL Intrinsic activity against dopamine D2(long) receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay F 8.13 pEC50 7.4 nM EC50 Bioorg. Med. Chem. Lett. (2006) 16: 2955-2959 [PMID:16563764]
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 8.23 pEC50 5.9 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 Galphai2 after 10 mins by BRET assay B 8.29 pEC50 5.1 nM EC50 J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Effective dose was measured by the stimulation of mitogenesis at Dopamine receptor D4.2 B 8.43 pEC50 3.7 nM EC50 J. Med. Chem. (2000) 43: 4563-4569 [PMID:11087581]
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 8.52 pEC50 3 nM EC50 J Med Chem (2017) 60: 2908-2929 [PMID:28248104]
ChEMBL Partial agonist activity at human D2L receptor expressed in HEK293T cells co-expressing Galpahi1/Gbeta1/GFP2-Ggamma2 assessed as Galphai1 dissociation after 15 mins in presence of coelenterazine 400a by luciferase reporter gene assay B 8.62 pEC50 2.4 nM EC50 J Med Chem (2019) 62: 4755-4771 [PMID:30964661]
ChEMBL Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay (intrinsic activity) B 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (2000) 43: 3549-3557 [PMID:11000009]
ChEMBL Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay B 8.74 pEC50 1.82 nM EC50 J Med Chem (2019) 62: 4755-4771 [PMID:30964661]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation preincubated for 15 mins followed by forskolin addition by GloSensor-based assay F 8.74 pEC50 1.8 nM EC50 J Med Chem (2018) 61: 8212-8225 [PMID:30180563]
ChEMBL Partial agonist activity at human Gi/o-coupled D2R expressed in HEK293T cells assessed as inhibition of isoproterenol-induced cAMP accumulation preincubated for 15 mins followed by isoproterenol-stimulation and measured by Glosensor-based luminescence assay B 8.74 pEC50 1.8 nM EC50 J Med Chem (2019) 62: 4755-4771 [PMID:30964661]
ChEMBL Agonist activity at human D2S receptor expressed in HEK293 cells cotransfected with Gqi5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol B 8.8 pEC50 1.6 nM EC50 Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
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 B 8.89 pEC50 1.3 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 GalphaoA after 10 mins by BRET assay B 8.92 pEC50 1.2 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 GalphaoB after 10 mins by BRET assay B 8.92 pEC50 1.2 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 Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, low affinity site B 5.59 pKi 2580 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 5.82 pKi 1500 nM Ki J. Med. Chem. (1998) 41: 4933-4938 [PMID:9836610]
ChEMBL Inhibition of [3H]YM-09151-2 binding to bovine retina membrane Dopamine receptor D2, high affinity site B 7.23 pKi 59.4 nM Ki J. Med. Chem. (1998) 41: 4933-4938 [PMID:9836610]
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 (S194A) in C6 (glioma) cell membranes. B 5.17 pKd 6700 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 5.46 pKd 3500 nM Kd J. Med. Chem. (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at mutant D2 receptor (S197A) in C6 (glioma) cell membranes. B 5.64 pKd 2300 nM Kd J. Med. Chem. (2000) 43: 3005-3019 [PMID:10956209]
ChEMBL In vitro affinity at wild type Dopamine receptor D2 on C6 (glioma) cell membranes. B 5.72 pKd 1900 nM Kd J. Med. Chem. (2000) 43: 3005-3019 [PMID:10956209]
GtoPdb - - 5.2 pKi - - - Nature (1990) 347: 146-51 [PMID:1975644]
ChEMBL Binding affinity against Dopamine receptor D2 in rat striatal membranes using [3H]spiperone B 7.2 pKi 63.1 nM Ki Bioorg. Med. Chem. Lett. (1995) 5: 2371-2376
ChEMBL Compound was evaluated for its ability to displace [3H]raclopride from dopamine receptor D2 in rat striatal homogenates B 7.27 pKi 54 nM Ki J. Med. Chem. (1992) 35: 1076-1092 [PMID:1348089]
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 5.32 pIC50 4784 nM IC50 Med Chem Res (2004) 13: 25-33
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 5.36 pIC50 4321 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Displacement of [3H]- -spiperone from Dopamine receptor D2 in rat striatum B 7 pIC50 100 nM IC50 J. Med. Chem. (1990) 33: 1756-1764 [PMID:1971308]
ChEMBL Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay B 7.32 pEC50 48 nM EC50 J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Effective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assay B 7.77 pEC50 17 nM EC50 J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Activity at rat dopamine D2L receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production F 8.05 pEC50 9 nM EC50 J. Med. Chem. (2006) 49: 6848-6857 [PMID:17154515]
ChEMBL Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D2L from rat F 8.66 pEC50 2.2 nM EC50 J. Med. Chem. (2000) 43: 2871-2882 [PMID:10956195]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Low binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 6.38 pKi 420 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells B 6.38 pKi 420 nM Ki J. Med. Chem. (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL In vitro for its ability to displace [3H]- spiperoneI from cloned human Dopamine receptor D3 expressed in CHO cells; Low binding affinity B 6.38 pKi 420 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 2533-2536 [PMID:11549463]
ChEMBL Tested for the ability to displace [125I]iodosulpiride from human cloned Dopamine receptor D3, expressed in CHO cells B 7 pKi 100 nM Ki Bioorg. Med. Chem. Lett. (1999) 9: 2715-2720 [PMID:10509922]
ChEMBL Displacement of [3H]spiperone from human cloned dopamine D3 receptor expressed in CHO cells B 7.31 pKi 49 nM Ki J. Med. Chem. (2009) 52: 6860-6870 [PMID:19807103]
ChEMBL Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells B 7.37 pKi 43 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter B 7.53 pKi 29.3 nM Ki J. Med. Chem. (2016) 59: 2973-2988 [PMID:27035329]
ChEMBL High binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 7.62 pKi 24 nM Ki J. Med. Chem. (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL In vitro binding affinity to displace [3H]spiperone from the cloned human dopamine receptor D3 in CHO cells B 7.62 pKi 24 nM Ki Bioorg. Med. Chem. Lett. (2003) 13: 851-854 [PMID:12617906]