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ChEMBL ligand: CHEMBL8946 (Eticloprida, Eticlopride) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
GtoPdb | - | - | 9.2 | pKi | - | - | - |
Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (2016) 59: 10676-10691 [PMID:27933960] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in HEK293 cell membranes measured after 60 mins by MicroBeta scintillation counting method | B | 9.93 | pKi | 0.12 | nM | Ki | J Med Chem (2021) 64: 15313-15333 [PMID:34636551] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D2 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 10.07 | pKi | 0.09 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
ChEMBL | Antagonist activity at DRD2 (unknown origin) expressed in HEK293T cells transfected with Galphai1-RLuc8 and gamma2-GFP10 assessed as inhibition of quinpirole-induced Gi1 activation pre-incubated with quinpirole for 10 mins before compound incubation for 10 mins by BRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2016) 59: 10676-10691 [PMID:27933960] |
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
ChEMBL | Evaluated in vivo for the affinity towards Dopamine receptor D2 of rat striatal tissue | B | 9.77 | pKd | 0.17 | nM | Kd | J Med Chem (1990) 33: 171-178 [PMID:2136916] |
ChEMBL | Affinity constant of compound was evaluated in rat striatum tissue preparation. | B | 9.77 | pKd | 0.17 | 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 | 9 | pKi | 0.99 | nM | Ki | J Med Chem (1991) 34: 1612-1624 [PMID:1827843] |
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 | 9.72 | pKi | 0.19 | nM | Ki | J Med Chem (1991) 34: 1612-1624 [PMID:1827843] |
ChEMBL | Inhibition of [3H]spiperone binding to rat striatal membrane Dopamine receptor D2 | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (1990) 33: 1155-1163 [PMID:1969484] |
ChEMBL | Compound was evaluated for the inhibition constant against dopamine receptor D2 in rat | B | 10.05 | pKi | 0.09 | nM | Ki | J Med Chem (1993) 36: 221-228 [PMID:8093734] |
ChEMBL | In vitro ability to inhibit the binding of [3H]spiperone to dopamine receptor D2 in rat striatal membranes. | B | 9.04 | pIC50 | 0.92 | nM | IC50 | J Med Chem (1990) 33: 1155-1163 [PMID:1969484] |
ChEMBL | Inhibition of [3H]spiperone binding to rat striatal dopamine receptor D2 was determined in vitro | B | 9.04 | pIC50 | 0.92 | nM | IC50 | J Med Chem (1991) 34: 948-955 [PMID:1672158] |
ChEMBL | Tested in vitro for inhibition of [3H]spiperone binding to dopamine receptor D2 | B | 9.04 | pIC50 | 0.92 | nM | IC50 | J Med Chem (1993) 36: 3417-3423 [PMID:7901417] |
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
GtoPdb | - | - | 8.8 | pKi | - | - | - |
Eur J Pharmacol (1994) 266: 79-85 [PMID:7907989]; J Pharmacol Exp Ther (1994) 268: 495-502 [PMID:8301592] |
ChEMBL | Compound was measured for its ability to compete with [125I]NCQ298 binding to the human Dopamine receptor D3 transfected in CHO cells | B | 9.8 | pKi | 0.16 | nM | Ki | J Med Chem (2003) 46: 4377-4392 [PMID:14521403] |
ChEMBL | Displacement of [3H]N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis | B | 9.87 | pKi | 0.13 | nM | Ki | J Med Chem (2014) 57: 4962-4968 [PMID:24848155] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D3R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay | B | 9.96 | pKi | 0.11 | nM | Ki | J Med Chem (2016) 59: 10676-10691 [PMID:27933960] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D3 receptor expressed in HEK293 cell membranes measured after 60 mins by MicroBeta scintillation counting method | B | 9.97 | pKi | 0.11 | nM | Ki | J Med Chem (2021) 64: 15313-15333 [PMID:34636551] |
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
GtoPdb | - | - | 7 | pKi | - | - | - | Life Sci (1995) 57: PL275-83 [PMID:7475902] |
ChEMBL | Displacement of [3H]N-methylspiperone from human D4R expressed in HEK293 cell membranes incubated for 1 hr by radioligand binding assay | B | 7.15 | pKi | 70.4 | nM | Ki | J Med Chem (2016) 59: 10676-10691 [PMID:27933960] |
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]