quinpirole [Ligand Id: 2] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL240773 (Quinpirol, Quinpirole) |
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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: 215, 293] [UniProtKB: P14416, P41594] | ||||||||
| 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 | F | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2018) 61: 8212-8225 [PMID:30180563] |
| D2 receptor/mGlu5 receptor in Rat [GtoPdb: 215, 293] [UniProtKB: P61169, P31424] | ||||||||
| 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. | F | 6.34 | pIC50 | 462 | nM | IC50 | US-9359372-B2. Hexahydrodibenzo[a,g]quinolizine compound, preparation method thereof, pharmaceutical composition and use thereof (2016) |
| ChEMBL | Partial agonist activity at human D2 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis | B | 8.58 | pIC50 | 2.63 | nM | IC50 | J Med Chem (2021) 64: 8710-8726 [PMID:34110150] |
| 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 | F | 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 | F | 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 | F | 5.64 | pEC50 | 2300 | nM | EC50 | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| 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 | Activity at dopamine D2S receptor (unknown origin) expressed in HEK293 cell membranes co-expressing Galpha protein subunit Galphai2 by [35S]GTPgammaS binding assay | F | 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 | 5.8 | 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 | F | 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 | F | 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 | F | 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 | F | 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 | F | 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 | 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 | 7.4 | pEC50 | 39.81 | 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 | 7.4 | pEC50 | 39.78 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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 histamine D2L receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay | F | 7.55 | pEC50 | 28.18 | nM | EC50 | Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637] |
| ChEMBL | Agonist activity at human D2 long receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD2longR-ElucC by beta-arrestin2 recruitment assay | F | 7.55 | pEC50 | 28.18 | nM | EC50 | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| 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 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 7.8 | pEC50 | 15.7 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Agonist activity at human dopamine D2 receptor expressed in HEK293 cells assessed as cAMP inhibition by BRET assay | F | 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 human D2R isoform 2 stably expressed in HEK293 cells assessed as inhibition of forskolin-induced increase of cAMP accumulation preincubated for 10 mins followed by forskolin addition by Glosensor cAMP reagent based luminescence assay | F | 8.29 | pEC50 | 5.1 | nM | EC50 | Eur J Med Chem (2021) 212: 113151-113151 [PMID:33450620] |
| 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 | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.52 | pEC50 | 3.02 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| 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 D2 receptor (unknown origin) expressed in HEK293T cells co-expressing Rluc8-tagged Galpahi1 assessed as Galphai1 dissociation preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.52 | pEC50 | 2.99 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at human D2 receptor expressed in HEK293T cells assessed as beta-arrestin recruitment preincubated for 10 mins with coelenterazine followed by compound addition and measured after 10 mins by BRET assay | B | 8.61 | pEC50 | 2.46 | nM | EC50 | J Med Chem (2021) 64: 8710-8726 [PMID:34110150] |
| 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 | F | 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 | F | 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 | F | 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 | F | 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] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.93 | pEC50 | 1.18 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.93 | pEC50 | 1.18 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 9.03 | pEC50 | 0.93 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Partial agonist activity at D2 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 9.03 | pEC50 | 0.93 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| 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] |
| ChEMBL | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells | B | 7.62 | pKi | 24 | 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 receptor D3 expressed in CHO cells; high binding affinity | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells | B | 7.62 | pKi | 23.99 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor expressed in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D3 receptor expressed in CHO cells by competitive binding assay | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D3 receptor transfected in CHO cells after 1 hr by scintillation counting analysis | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Displacement of [3H]spiroperidol from human cloned dopamine D3 receptor by liquid scintillation counting | B | 7.9 | pKi | 12.5 | nM | Ki | Bioorg Med Chem (2009) 17: 758-766 [PMID:19081257] |
| GtoPdb | - | - | 8 | pKi | 10 | nM | Ki |
Neuroreport (1995) 6: 329-332 [PMID:7756621]; 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]; J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180]; Nature (1991) 350: 610-4 [PMID:1840645]; Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990] |
| ChEMBL | Displacement of [3H]7-OH-DPAT from human D3 receptor transfected in HEK293 cells measured after 60 mins by liquid scintillation counter | B | 8.1 | pKi | 8.01 | 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 | 8.17 | pKi | 6.76 | nM | Ki | J Med Chem (2017) 60: 2890-2907 [PMID:28300398] |
| ChEMBL | Displacement of [3H]spiroperidol from cloned human dopamine receptor D3 in CHO cell membrane | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
| ChEMBL | Partial agonist activity at human D3 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis | B | 7.57 | pIC50 | 26.92 | nM | IC50 | J Med Chem (2021) 64: 8710-8726 [PMID:34110150] |
| ChEMBL | Agonist activity at D3 receptor (unknown origin) expressed in cell membranes after 40 mins by [35S]GTPgammaS binding assay | F | 6.73 | pEC50 | 186.3 | nM | EC50 | Eur J Med Chem (2016) 123: 332-353 [PMID:27487565] |
| ChEMBL | Agonist activity at D3 receptor (unknown origin) expressed in human HTLA cells assessed as induction of beta-arrestin2 recruitment measured after 16 hrs by Bright-glo reagent based Tango luminescence assay | B | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2020) 63: 4579-4602 [PMID:32282200] |
| ChEMBL | Intrinsic activity against dopamine receptor D3 by Eu-GTP binding assay | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2005) 48: 7919-7922 [PMID:16335915] |
| ChEMBL | Activation of human dopamine D3 receptor L89K mutant expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay | F | 8 | pEC50 | 10 | nM | EC50 | Bioorg Med Chem (2015) 23: 3938-3947 [PMID:25564378] |
| 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 | 8.01 | pEC50 | 9.77 | 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 | 8.01 | pEC50 | 9.7 | nM | EC50 | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| 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 | 8.08 | pEC50 | 8.4 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in CHO dhfr mutant cells assessed as stimulation of mitogenesis after 4 hrs | F | 8.28 | pEC50 | 5.2 | nM | EC50 | Bioorg Med Chem (2007) 15: 7248-7257 [PMID:17827018] |
| ChEMBL | Intrinsic activity against dopamine D3 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | F | 8.47 | pEC50 | 3.4 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.48 | pEC50 | 3.31 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GFP2-beta-arrestin2 assessed as beta-arrestin2 recruitment preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.48 | pEC50 | 3.31 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| 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 | 8.48 | pEC50 | 3.3 | nM | EC50 | J Med Chem (2016) 59: 2973-2988 [PMID:27035329] |
| ChEMBL | Intrinsic activity in mitogenesis assay using Dopamine receptor D3 expressing CHO cells | F | 8.51 | pEC50 | 3.1 | nM | EC50 | J Med Chem (2002) 45: 4594-4597 [PMID:12361386] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as inhibition of forskolin-induced cAMP release | F | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay | B | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells assessed as rate of [3H]thymidine incorporation by mitogenesis assay | F | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2006) 49: 3628-3635 [PMID:16759104] |
| ChEMBL | Effective concentration against dopamine D3 receptor | B | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| ChEMBL | Agonist activity at recombinant human D3 receptor expressed in CHOK1 cells assessed as induction of beta arrestin2 recruitment measured after 30 mins by coelenterazine-based beta-galactosidase reporter gene assay | B | 8.59 | pEC50 | 2.6 | nM | EC50 | J Med Chem (2019) 62: 5132-5147 [PMID:31021617] |
| ChEMBL | Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.59 | pEC50 | 2.59 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Agonist activity at D3 receptor in HEK293T cells assessed as G beta-gamma release from G alpha oA using coelenterazine h as substrate pretreated with substrate followed by compound addition measured after 10 mins by BRET analysis | F | 8.59 | pEC50 | 2.57 | nM | EC50 | J Med Chem (2023) 66: 1809-1834 [PMID:36661568] |
| ChEMBL | Activation of wild type human dopamine D3 receptor expressed in HEK293 cells co-expressing GaqG66Di5- incubated for 120 mins by scintillation counting based myo-[3H]inositol phosphate accumulation assay | F | 8.62 | pEC50 | 2.4 | nM | EC50 | Bioorg Med Chem (2015) 23: 3938-3947 [PMID:25564378] |
| 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 | 8.62 | pEC50 | 2.4 | 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 | 8.64 | pEC50 | 2.29 | 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 | 8.64 | pEC50 | 2.27 | nM | EC50 | J Med Chem (2023) 66: 10304-10341 [PMID:37467430] |
| ChEMBL | Intrinsic activity at human D3 receptor expressed in CHO dhfr- cells by [3H]thymidine incorporation assay | B | 8.68 | pEC50 | 2.1 | nM | EC50 | J Med Chem (2008) 51: 6829-6838 [PMID:18834111] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.71 | pEC50 | 1.97 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Partial agonist activity at D3 receptor (unknown origin) expressed in HEK293T cells co-expressing GalphaoA preincubated for 2 mins with coelenterazine followed by compound addition and measured after 2 mins by BRET assay | F | 8.71 | pEC50 | 1.95 | nM | EC50 | J Med Chem (2021) 64: 17239-17258 [PMID:34797051] |
| ChEMBL | Agonist activity at human histamine D3 receptor receptor expressed in HEK293T cells co-expressing ELucC by beta arrestin2 recruitment assay | F | 8.75 | pEC50 | 1.78 | nM | EC50 | Eur J Med Chem (2021) 214: 113190-113190 [PMID:33548637] |
| ChEMBL | Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay | F | 8.75 | pEC50 | 1.78 | nM | EC50 | J Med Chem (2021) 64: 8684-8709 [PMID:34110814] |
| ChEMBL | Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay (intrinsic activity) | B | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2000) 43: 3549-3557 [PMID:11000009] |
| ChEMBL | Agonist activity at human dopamine D3 receptor expressed in dhfr-deficient CHO cells assessed as [3H]thymidine incorporation | F | 8.85 | pEC50 | 1.4 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2670-2674 [PMID:21273071] |
| ChEMBL | Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor | F | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2005) 48: 3696-3699 [PMID:15916420] |
| 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 | 9.38 | pEC50 | 0.42 | nM | EC50 | J Med Chem (2020) 63: 4579-4602 [PMID:32282200] |
| ChEMBL | Agonist activity at human D3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation after 4 hrs by luciferase reporter gene assay | F | 10.01 | pEC50 | 0.1 | nM | EC50 | Medchemcomm (2018) 9: 1457-1465 [PMID:30288220] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| GtoPdb | - | - | 7.8 | pKi | - | - | - |
Neuropsychopharmacology (1995) 12: 335-45 [PMID:7576010]; Nature (1990) 347: 146-51 [PMID:1975644] |
| ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 8.25 | pKi | 5.65 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
| 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 | 7.54 | pIC50 | 29 | 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 | 7.6 | pIC50 | 25 | nM | IC50 | Med Chem Res (2004) 13: 25-33 |
| ChEMBL | Basal binding towards Dopamine receptor D3 was evaluated using [35S]- GTP-gamma S radioligand | B | 7.1 | pEC50 | 80 | nM | EC50 | J Med Chem (2003) 46: 3822-3839 [PMID:12930145] |
| ChEMBL | Agonist activity by measuring the [3H]thymidine uptake against Dopamine receptor D3 from rat | F | 8.77 | pEC50 | 1.7 | nM | EC50 | J Med Chem (2000) 43: 2871-2882 [PMID:10956195] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | In vitro for its ability to displace [3H]- spiperone from cloned human Dopamine receptor D4 expressed in CHO cells; Low binding affinity | B | 7.28 | pKi | 53 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Low binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 7.28 | pKi | 53 | nM | Ki | J Med Chem (2005) 48: 5771-5779 [PMID:16134944] |
| GtoPdb | - | - | 7.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Nature (1991) 350: 610-4 [PMID:1840645]; Mol Pharmacol (1996) 50: 1658-64 [PMID:8967990] |
| ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D4.4 receptor expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2009) 52: 6860-6870 [PMID:19807103] |
| ChEMBL | Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells | B | 8.07 | pKi | 8.5 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor transfected in CHO cells after 1 hr by scintillation counting analysis | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| ChEMBL | Displacement of [3H]Spiperone from human dopamine D4.4 receptor expressed in CHO cells by competitive binding assay | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2014) 57: 4861-4875 [PMID:24831693] |
| ChEMBL | Displacement of [3H]spiperone from human dopamine D4.4 receptor expressed in CHO cells | B | 8.07 | pKi | 8.5 | nM | Ki | J Med Chem (2013) 56: 5130-5141 [PMID:23730937] |
| ChEMBL | High binding affinity towards human dopamine receptor 4.4 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand | B | 8.74 | pKi | 1.8 | 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 D4 in CHO cells | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells | B | 8.74 | pKi | 1.8 | 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 receptor D4 expressed in CHO cells; high binding affinity | B | 8.74 | pKi | 1.8 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Partial agonist activity at human D4 receptor expressed in HEK293T cells assessed as inhibition of forskolin-induced cAMP production incubated for 1 hr by HTRF analysis | B | 7.48 | pIC50 | 33.11 | nM | IC50 | J Med Chem (2021) 64: 8710-8726 [PMID:34110150] |
| ChEMBL | Agonist activity at PKA-tagged D4 receptor (unknown origin) expressed in HEK293 cells co-expressing beta-arrestin2 assessed as induction of beta-arrestin2 recruitment incubated for 6 hrs by Path-Hunter assay | B | 7.08 | pEC50 | 83 | nM | EC50 | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Agonist activity at PKA-tagged human dopamine D4 receptor transfected in HEK293T cells expressing (EA)-beta-arrestin assessed as beta-arrestin recruitment incubated for 3 hrs by chemiluminescence based PathHunter assay | F | 7.17 | pEC50 | 67 | nM | EC50 | J Med Chem (2023) 66: 9710-9730 [PMID:37450764] |
| ChEMBL | Activity at human D4.4 receptor expressed in CHOK1 cells assessed as stimulation of [35S]GTP-gammaS binding | F | 7.31 | pEC50 | 49 | nM | EC50 | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
| ChEMBL | Effective concentration for [35S]GTP-gamma-S, binding in CHO-K1 cells expressing human dopamine D4 receptor | F | 7.31 | pEC50 | 49 | nM | EC50 | J Med Chem (2005) 48: 3696-3699 [PMID:15916420] |
| ChEMBL | Agonist effect on the Dopamine D4.2 receptor was determined by evaluating effective concentration causing stimulation of mitogenesis | F | 7.51 | pEC50 | 31 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 2533-2536 [PMID:11549463] |
| ChEMBL | Intrinsic activity against dopamine D4 receptor expressed in CHO cells by GTPgammaS assay | F | 7.64 | pEC50 | 23 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2 | F | 7.72 | pEC50 | 19 | nM | EC50 | J Med Chem (2005) 48: 3696-3699 [PMID:15916420] |
| ChEMBL | Agonist activity at PKA-tagged human dopamine D4 receptor transfected in HEK293T cells expressing (EA)-beta-arrestin and GRK2 assessed as beta-arrestin recruitment incubated for 3 hrs by chemiluminescence based PathHunter assay | F | 7.8 | pEC50 | 16 | nM | EC50 | J Med Chem (2023) 66: 9710-9730 [PMID:37450764] |
| ChEMBL | Intrinsic activity against dopamine D4 receptor assessed as [3H]thymidine uptake in CHO cells by mitogenesis assay | F | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 2955-2959 [PMID:16563764] |
| ChEMBL | Effective concentration for [3H]thymidine uptake in growing CHO cells stably expressing the dopamine D4.2 receptor | B | 8 | pEC50 | 9.9 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 851-854 [PMID:12617906] |
| ChEMBL | Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay | B | 8.06 | pEC50 | 8.7 | nM | EC50 | J Med Chem (2005) 48: 2493-2508 [PMID:15801839] |
| ChEMBL | Activity at human dopamine D4.4 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 | 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 | 8.57 | pEC50 | 2.7 | nM | EC50 | ACS Med Chem Lett (2019) 10: 792-799 [PMID:31098001] |
| ChEMBL | Effective concentration of compound required against human Dopamine D4.2 receptor | F | 8.66 | pEC50 | 2.2 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 1937-1940 [PMID:12113813] |
| ChEMBL | Agonist activity at human D4 receptor expressed in HEK293T cells co-expressing G-alphaqi assessed as accumulation of inositol monophosphate using d2-labelled IP1 conjugate incubated for 90 mins by HTRF assay | F | 8.66 | pEC50 | 2.2 | nM | EC50 | J Med Chem (2019) 62: 9658-9679 [PMID:31613617] |
| ChEMBL | Agonist activity at human dopamine D4 receptor transfected in HEK293T cells co-transfected with Galpha-qi assessed as activation of GPCR-mediated receptor signaling incubated for 90 mins by IP-one HTRF assay | F | 8.68 | pEC50 | 2.1 | nM | EC50 | J Med Chem (2023) 66: 9710-9730 [PMID:37450764] |
| ChEMBL | Tested for the effective concentration against CHO 10001 cells in human D4.2 receptor established in mitogenesis assay | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 633-636 [PMID:11844688] |
| ChEMBL | Activity at human D4.2 receptor assessed as [3H]thymidine incorporation in CHO 10001 cells by mitogenesis assay | F | 8.85 | pEC50 | 1.4 | nM | EC50 | J Med Chem (2006) 49: 3938-3947 [PMID:16789750] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor transfected in HEK293 cells by scintillation counting analysis | B | 4.6 | pKi | 25000 | nM | Ki | J Med Chem (2015) 58: 2703-2717 [PMID:25734236] |
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 5.8 | pKi | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 447-53 [PMID:10431754] |
| 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
| 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 5.5 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 791-804 [PMID:12388666]; Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733] |
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]
