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ChEMBL ligand: CHEMBL8946 (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 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]