eticlopride [Ligand Id: 966] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL8946 (Eticlopride)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • 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]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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]