pramipexole [Ligand Id: 953] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL301265 (Ctc-501, Mirapexin, Neliprax, NSC-760426, Oprymea, Pipexus, Pramipexole, SUD-919CL2Y, SUD919CL2Y, U-98528E)
  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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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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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
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  • H4 receptor/Histamine H4 receptor in Human [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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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]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Agonist activity at human recombinant dopamine D1 receptor expressed in CHO cells assessed as stimulation of cAMP production F 5 pEC50 >10000 nM EC50 Bioorg Med Chem (2008) 16: 3438-3444 [PMID:18313303]
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]SCH23390 from D1-like receptor in Sprague-Dawley rat striatum B 4 pKi >100000 nM Ki J Med Chem (2008) 51: 5905-5908 [PMID:18785726]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 long receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 140 mins by radioligand competition binding based assay B 10.83 pKd 0.01 nM Kd J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 long receptor stably expressed in HEK293T cells co-expressing luciferase and CEK at high concentration incubated for 140 mins by radioligand competition binding based assay B 10.83 pKd 0.01 nM Kd J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL Low binding affinity towards human dopamine receptor 2 (long) expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 5.2 pKi 6300 nM Ki J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells B 5.2 pKi 6300 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Low binding affinity towards human dopamine receptor 2 (short) expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 5.72 pKi 1900 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 5.72 pKi 1900 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 long receptor stably expressed in HEK293T cells co-expressing luciferase and CEK at low concentration incubated for 140 mins by radioligand competition binding based assay B 6 pKi 1000 nM Ki J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL in vitro low binding affinity was determined on human Dopamine receptor D2L expressed in chinese hamster ovary(CHO) K-1 cells using [3H]-spiperone as radioligand. B 6.86 pKi 139 nM Ki J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
ChEMBL Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells B 7.22 pKi 60 nM Ki Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D2 short (high/low affinity is given as 40/3600) B 7.4 pKi 40 nM Ki Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
GtoPdb - - 7.4 pKi - - - Neuroreport (1995) 6: 329-332 [PMID:7756621];
Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]
ChEMBL Binding affinity of compound measured using [3H]-spiperone for the cloned human dopamine receptor D2 long (high/low affinity is given as 27/5400) B 7.57 pKi 27 nM Ki Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
ChEMBL Displacement of [3H]N-methylspiperone from human D2 long receptor stably expressed in HEK293T cells co-expressing luciferase and CEK at high concentration incubated for 140 mins by radioligand competition binding based assay B 7.59 pKi 25.7 nM Ki J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
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 7.68 pKi 21 nM Ki J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL High binding affinity towards human dopamine receptor 2 (long) expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 7.68 pKi 21 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 7.68 pKi 21 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL High inhibition constant against [3H]spiperone binding to human Dopamine receptor D2L expressed in CHO cells B 7.68 pKi 21 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Antagonist activity at human D2 dopamine receptor expressed in CHO cell membrane by GTPgammaS-binding assay F 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2013) 23: 543-547 [PMID:23237836]
ChEMBL Agonist activity at human D2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding by Perkin elmer analysis B 6.6 pEC50 251 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 7 pEC50 100 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
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 7.57 pEC50 27 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at human recombinant dopamine D2 receptor expressed in rat pituitary cells assessed as inhibition of forskolin-stimulated cAMP accumulation F 7.57 pEC50 27 nM EC50 Bioorg Med Chem Lett (2007) 17: 6691-6696 [PMID:17976986]
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 8.02 pEC50 9.6 nM EC50 J Med Chem (2017) 60: 4693-4713 [PMID:28489379]
ChEMBL Agonist activity at dopamine D2 receptor short isoform (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 8.15 pEC50 7.08 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)
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 8.19 pEC50 6.46 nM EC50 J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production F 8.3 pEC50 5 nM EC50 Bioorg Med Chem (2008) 16: 3438-3444 [PMID:18313303]
Dopamine D2 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3998] [UniProtKB: P20288]
ChEMBL Binding affinity of compound against Dopamine receptor D2 was measured using [3H]pramipexole in Bovine striatal membranes B 8.8 pKd 1.6 nM Kd Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]Spiperone from Sprague-Dawley rat dopamine D2-like receptor after 90 mins B 7.41 pKi 39 nM Ki ACS Med Chem Lett (2011) 2: 620-625 [PMID:22125662]
ChEMBL Displacement of [3H]Spiperone from D2 receptor in Sprague-Dawley rat caudate-putamen B 8.51 pKi 3.1 nM Ki J Med Chem (2008) 51: 5905-5908 [PMID:18785726]
ChEMBL Affinity of the Compound for Dopamine receptor D2 in rat striatal membrane was determined in vitro using Dopamine Antagonist [3H]spiperone as ligand F 5.33 pIC50 4700 nM IC50 Bioorg Med Chem Lett (1991) 1: 189-192
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 6.35 pIC50 450 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Agonist activity at Rattus norvegicus (rat) dopamine D2 receptor transfected in african green monkey COS7 cells assessed as inhibition of forskolin-stimulated adenylyl cyclase activity after 10 min F 7.67 pEC50 21.5 nM EC50 Med Chem Res (2004) 13: 25-33
ChEMBL Effective concentration required for agonistic activity against rat D2 short receptor F 7.92 pEC50 12 nM EC50 Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
ChEMBL Effective concentration to stimulate rat Dopamine receptor D2S mediated [3H]thymidine incorporation into growing cells using mitogenesis assay B 7.92 pEC50 12 nM EC50 J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Effective concentration required for agonistic activity against rat D2 long receptor F 8.04 pEC50 9.2 nM EC50 Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
ChEMBL Effective concentration to stimulate rat Dopamine receptor D2L mediated [3H]thymidine incorporation into growing cells using mitogenesis assay B 8.04 pEC50 9.2 nM EC50 J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D2L by mitogenesis assay F 8.77 pEC50 1.7 nM EC50 J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 140 mins by radioligand competition binding based assay B 10.59 pKd 0.03 nM Kd J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells B 7.42 pKi 38 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Low binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 7.42 pKi 38 nM Ki J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Displacement of [3H]-methylspiperon from human D3R expressed in HEK293 cell membranes measured after 90 mins in Tris buffer containing NaCl by topcount assay B 7.77 pKi 17 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL Displacement of [3H]-methylspiperon from human D3R expressed in HEK293 cell membranes measured after 90 mins in Tris buffer by topcount assay B 7.89 pKi 13 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL Agonist activity at dopamine D3 receptor (unknown origin) B 8.07 pKi 8.5 nM Ki Bioorg Med Chem Lett (2013) 23: 5586-5591 [PMID:24012118]
ChEMBL Displacement of [3H]-methylspiperon from human D3R expressed in HEK293 cell membranes measured after 90 mins in EBSS buffer by topcount assay B 8.09 pKi 8.2 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL Displacement of [3H]-7-OH-DPAT from human D3R expressed in HEK293 cell membranes measured after 90 mins in Tris buffer containing NaCl by topcount assay B 8.25 pKi 5.6 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL in vitro low binding affinity was determined on human Dopamine receptor D3 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand. B 8.56 pKi 2.78 nM Ki J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
GtoPdb - - 8.7 pKi - - - Neuroreport (1995) 6: 329-332 [PMID:7756621];
Eur J Pharmacol (1995) 290: 29-36 [PMID:7664822]
ChEMBL Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D3 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis B 8.88 pKi 1.32 nM Ki J Med Chem (2019) 62: 6287-6314 [PMID:31257877]
ChEMBL Displacement of [3H]-7-OH-DPAT from human D3R expressed in HEK293 cell membranes measured after 90 mins in EBSS buffer by topcount assay B 8.96 pKi 1.1 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL Displacement of [3H]-7-OH-DPAT from human D3R expressed in HEK293 cell membranes measured after 90 mins in Tris buffer by topcount assay B 9.03 pKi 0.94 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL Displacement of [3H]-N-methylspiperone from D3 receptor (unknown origin) measured after 90 mins by microbeta scintillation counting method B 9.05 pKi 0.9 nM Ki J Med Chem (2020) 63: 5526-5567 [PMID:32342685]
ChEMBL High binding affinity towards human dopamine receptor 3 expressed in Chinese hamster ovary cells using [3H]spiperone (0.5 nM) as radioligand B 9.06 pKi 0.88 nM Ki J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL High inhibition constant against [3H]spiperone binding to human Dopamine receptor D3 expressed in CHO cells B 9.06 pKi 0.88 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Binding affinity of compound measured using [3H]-spiperone for the cloned human Dopamine receptor D3 (high/low affinity is given as 0.87/44) B 9.06 pKi 0.87 nM Ki Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
ChEMBL Inhibition constant against [3H]-spiperone binding to human Dopamine receptor D3 expressed in CHO cells B 9.14 pKi 0.72 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Displacement of [3H]N-methylspiperone from human D3 receptor stably expressed in HEK293T cells co-expressing luciferase and CEK incubated for 140 mins by radioligand competition binding based assay B 9.18 pKi 0.66 nM Ki J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
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 8.27 pEC50 5.4 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 8.39 pEC50 4.08 nM EC50 Bioorg Med Chem (2023) 78: 117131-117131 [PMID:36571976]
ChEMBL Effective concentration to stimulate human Dopamine receptor D3 mediated [3H]-thymidine incorporation into growing cells using mitogenesis assay B 8.82 pEC50 1.5 nM EC50 J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL Effective concentration against dopamine D3 receptor B 8.82 pEC50 1.5 nM EC50 J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Effective concentration required for agonistic activity against human D3 receptor F 8.82 pEC50 1.5 nM EC50 Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
ChEMBL Agonist activity at human recombinant dopamine D3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation F 9 pEC50 1 nM EC50 Bioorg Med Chem Lett (2007) 17: 6691-6696 [PMID:17976986]
ChEMBL Agonist activity at human D3 receptor stably expressed in HEK293T cells co-expressing ElucN-betaarr2 hD3R-ElucC by beta-arrestin2 recruitment assay F 9.09 pEC50 0.81 nM EC50 J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020]
ChEMBL Displacement of [3H]PD128907 from dopamine D3 receptor in Sprague-Dawley rat ventral striatum B 9.11 pKi 0.78 nM Ki J Med Chem (2008) 51: 5905-5908 [PMID:18785726]
ChEMBL Displacement of [3H]-R(+)-7-OHDPAT from dopamine D3 receptor in rat brain homogenates B 9.11 pKi 0.78 nM Ki Bioorg Med Chem Lett (2012) 22: 5612-5617 [PMID:22871578]
ChEMBL Displacement of [3H]R(+)-7-OH-DPAT from Sprague-Dawley rat dopamine D3 receptor after 90 mins B 9.35 pKi 0.45 nM Ki ACS Med Chem Lett (2011) 2: 620-625 [PMID:22125662]
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 8.11 pIC50 7.8 nM IC50 Med Chem Res (2004) 13: 25-33
ChEMBL Effective concentration was determined as thymidine uptake in CHO-L6 cells transfected with the rat Dopamine receptor D3 by mitogenesis assay F 9.68 pEC50 0.21 nM EC50 J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL in vitro low binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand. B 6.86 pKi 138 nM Ki J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
ChEMBL Low inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells B 6.89 pKi 130 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 6.89 pKi 130 nM Ki J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL Binding affinity of compound measured using [3H]spiperone for the cloned human dopamine receptor D4.4 (high/low affinity is given as 8.5/130) B 8.07 pKi 8.5 nM Ki Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
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 8.09 pKi 8.1 nM Ki J Med Chem (2005) 48: 5771-5779 [PMID:16134944]
ChEMBL High inhibition constant against [3H]spiperone binding to human Dopamine receptor D4.4 expressed in CHO cells B 8.09 pKi 8.1 nM Ki J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
ChEMBL in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand. B 8.56 pKi 2.76 nM Ki J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
ChEMBL in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand. B 8.68 pKi 2.07 nM Ki J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
ChEMBL in vitro high binding affinity was determined on human Dopamine receptor D4 expressed in chinese hamster ovary(CHO) K-1 cells using [3H]spiperone as radioligand. B 9.31 pKi 0.49 nM Ki J Med Chem (2000) 43: 3549-3557 [PMID:11000009]
ChEMBL Effective concentration required for agonistic activity against human D4.2 receptor F 7.82 pEC50 15 nM EC50 Bioorg Med Chem Lett (2002) 12: 2377-2380 [PMID:12161137]
ChEMBL Effective concentration to stimulate human Dopamine receptor D4.2 mediated [3H]thymidine incorporation into growing cells using mitogenesis assay B 7.82 pEC50 15 nM EC50 J Med Chem (2005) 48: 2493-2508 [PMID:15801839]
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL Displacement of [3H] mepyramine from human histamine H1 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RGS4 incubated for 60 mins by scintillation counting analysis B 8.35 pKd 4.5 nM Kd J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
ChEMBL Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis B 7.91 pKd 12.2 nM Kd J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL Displacement of [3H]UR-DE257 from human histamine H2 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing RG-Salpha S incubated for 60 mins by scintillation counting analysis B 4.86 pKi 13803.84 nM Ki J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
ChEMBL Agonist activity at human histamine H2 receptor stably expressed in HEK293T cells co-expressing NlucN-mGs/hH2R-NlucC assessed as induction of mini-Gi protein recruitment using furimazine as substrate measured for 45 mins by luminescence assay F 6.78 pEC50 165.96 nM EC50 J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
H4 receptor/Histamine H4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3759] [GtoPdb: 265] [UniProtKB: Q9H3N8]
ChEMBL Displacement of [3H]-histamine from human histamine H4 receptor stably expressed in baculovirus infected Sf9 cell membrane co-expressing G-alphai2 and G-beta1gamma2 incubated for 60 mins by scintillation counting analysis B 7.8 pKd 16 nM Kd J Med Chem (2021) 64: 8684-8709 [PMID:34110814]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Agonist activity at 5HT2A receptor (unknown origin) expressed in mouse NIH/3T3 cells by R-SAT assay B 5.93 pEC50 1174.9 nM EC50 US-20040213816-A1. Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases (2004)

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]