raclopride [Ligand Id: 94] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL8809 (Raclopride) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Dopamine D1 receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5067] [UniProtKB: P50130] | ||||||||
| ChEMBL | Displacement of [3H]SCH23990 from dopamine D1 receptor in pig striatal membrane | B | 4.43 | pKi | 37000 | nM | Ki | Bioorg Med Chem (2007) 15: 6819-6829 [PMID:17765546] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | In vivo inhibitory activity against dopamine (D1) receptor in rat caudate-putamen tissue | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4015-4017 [PMID:14592497] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from dopamine D2short receptor in CHO cells | B | 7.51 | pKi | 31 | nM | Ki | Bioorg Med Chem (2007) 15: 6819-6829 [PMID:17765546] |
| ChEMBL | Displacement of [3H]spiperone from dopamine D2long receptor in CHO cells | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem (2007) 15: 6819-6829 [PMID:17765546] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 7.9 | pKi | 12.7 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
| ChEMBL | Binding affinity to dopamine D2 receptor (unknown origin) | B | 7.9 | pKi | 12.7 | nM | Ki | J Med Chem (2016) 59: 7634-7650 [PMID:27508895] |
| GtoPdb | - | - | 8 | pKi | 10 | nM | Ki | J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180] |
| ChEMBL | Displacement of [3H]spiperone from human D2 receptor transfected in HEK cells | B | 8.92 | pKi | 1.21 | nM | Ki | J Med Chem (2014) 57: 4368-4381 [PMID:24779610] |
| ChEMBL | Antagonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 6.98 | pIC50 | 104.2 | nM | IC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Antagonist activity at D2 long receptor (unknown origin) transfected in human HEK293T cells assessed as increase in cAMP accumulation incubated for 2 hrs by cAMP Glo-sensor assay | F | 7 | pIC50 | 100 | nM | IC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Antagonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8.74 | pIC50 | 1.83 | nM | IC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| ChEMBL | Antagonist activity at C-terminal RLuc8-fused D2 long receptor (unknown origin) transfected in human HEK293T cells co-expressing N-terminal Venus-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment measured after 5 mins in presence of coelenterazine H by BRET assay | B | 8.74 | pIC50 | 1.82 | nM | IC50 | ACS Med Chem Lett (2020) 11: 385-392 [PMID:32184974] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | Affinity constant of compound was evaluated in human brain | B | 8.15 | pKd | 7.1 | nM | Kd | J Med Chem (1988) 31: 1039-1043 [PMID:2966245] |
| ChEMBL | Affinity constant of compound was evaluated in rat striatum tissue preparation. | B | 8.96 | pKd | 1.1 | nM | Kd | J Med Chem (1988) 31: 1039-1043 [PMID:2966245] |
| ChEMBL | Displacement of [3H]- spiperone from dopamine receptor D2 of striatal membranes without sodium chloride | B | 7.48 | pKi | 32.8 | nM | Ki | J Med Chem (1991) 34: 1612-1624 [PMID:1827843] |
| ChEMBL | Compound was evaluated for binding affinity towards DA D-2 receptor using radioligand [3H]SPI | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (1992) 35: 2355-2363 [PMID:1535660] |
| ChEMBL | Compound was evaluated for binding affinity towards dopamine receptor D2 in striatal membranes, using [3H]- spiperone as radioligand in the presence of sodium chloride | B | 8.08 | pKi | 8.29 | nM | Ki | J Med Chem (1991) 34: 1612-1624 [PMID:1827843] |
| ChEMBL | Displacement of [3H]raclopride from dopamine D2 receptor in Sprague-Dawley rat striatal membranes after 30 mins | B | 8.59 | pKi | 2.6 | nM | Ki | Eur J Med Chem (2015) 101: 367-383 [PMID:26164842] |
| ChEMBL | In vitro binding affinity against dopamine receptor D2 in rat striata; value ranges from 1.8-3.0 nM | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (1990) 33: 2430-2437 [PMID:2391685] |
| ChEMBL | Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1990) 33: 1155-1163 [PMID:1969484] |
| ChEMBL | Inhibition of [3H]raclopride binding to rat striatal dopamine receptor D2 | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1991) 34: 948-955 [PMID:1672158] |
| ChEMBL | Inhibition constant against dopamine receptor D2 in rat | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1993) 36: 221-228 [PMID:8093734] |
| ChEMBL | Competitive binding assay against Dopamine receptor D2 in rat striatal membranes and [125I]-IBF radioligand | B | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (1990) 33: 171-178 [PMID:2136916] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
Nature (1990) 347: 146-51 [PMID:1975644]; Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
| ChEMBL | Inhibition of [3H]spiperone binding to rat striatal dopamine receptor D2 was determined in vitro | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1991) 34: 948-955 [PMID:1672158] |
| ChEMBL | In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes. | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1990) 33: 1155-1163 [PMID:1969484] |
| ChEMBL | Inhibitory concentration required for displacing radioligand [3H]SPI from DA D-2 receptor | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1992) 35: 2355-2363 [PMID:1535660] |
| ChEMBL | The affinity for the Dopamine receptor D2 was assessed by the inhibition of [3H]-spiperone binding in rat striatal membranes in vitro. | B | 7.49 | pIC50 | 32 | nM | IC50 | J Med Chem (1990) 33: 2305-2309 [PMID:1973734] |
| ChEMBL | Inhibition of [3H](S)-sulpiride binding in striatal homogenates of rat brain | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (1988) 31: 2027-2033 [PMID:3172140] |
| ChEMBL | In vivo inhibitory activity against dopamine (D2) receptor in rat caudate-putamen tissue | B | 8.14 | pIC50 | 7.2 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 4015-4017 [PMID:14592497] |
| ChEMBL | In vitro binding affinity for Dopamine D2 receptor of rat using [3H]YM-09151 as radioligand | B | 8.47 | pIC50 | 3.4 | nM | IC50 | J Med Chem (2002) 45: 4655-4668 [PMID:12361392] |
| ChEMBL | Inhibition of 0.1 nM of [125I]- (S)-N-(1-Ethyl-pyrrolidin-2-ylmethyl)-5-iodo-2-methoxy-benzamide binding in striatal homogenates of rat brain | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (1988) 31: 2027-2033 [PMID:3172140] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from dopamine D3 receptor in CHO cells | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2007) 15: 6819-6829 [PMID:17765546] |
| ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 7.87 | pKi | 13.4 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
| ChEMBL | Binding affinity to dopamine D3 receptor (unknown origin) | B | 7.87 | pKi | 13.4 | nM | Ki | J Med Chem (2016) 59: 7634-7650 [PMID:27508895] |
| GtoPdb | - | - | 7.9 | pKi | - | - | - | J Pharmacol Exp Ther (1995) 275: 885-898 [PMID:7473180] |
| ChEMBL | Compound was measured for its ability to compete with [3H]spiperone binding to the human Dopamine receptor D3 transfected in CHO cells | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
| D3 receptor/Dopamine D3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3138] [GtoPdb: 216] [UniProtKB: P19020] | ||||||||
| GtoPdb | - | - | 7.5 | pKi | - | - | - | Nature (1990) 347: 146-51 [PMID:1975644] |
| ChEMBL | Tested for binding affinity against dopamine receptor D3 expressed in Sf9 cells. | B | 8.03 | pKi | 9.25 | nM | Ki | J Med Chem (1993) 36: 1499-1500 [PMID:8098771] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from dopamine D4.4 receptor in CHO cells | B | 5.51 | pKi | 3100 | nM | Ki | Bioorg Med Chem (2007) 15: 6819-6829 [PMID:17765546] |
| D4 receptor in Rat [GtoPdb: 217] [UniProtKB: P30729] | ||||||||
| GtoPdb | - | - | 5.7 | pKi | - | - | - | Mol Pharmacol (2000) 57: 144-52 [PMID:10617689] |
| 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| GtoPdb | - | - | 5.2 | pKi | - | - | - | Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
