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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 |
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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 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]