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ChEMBL ligand: CHEMBL301265 (Ctc-501, Mirapexin, Neliprax, NSC-760426, Oprymea, Pipexus, Pramipexole, SUD-919CL2Y, SUD919CL2Y, U-98528E) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]