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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL8946 (Eticloprida, 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]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
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 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]