ecopipam [Ligand Id: 3304] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL298406 (Ecopipam, SCH-39166)
  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • 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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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
GtoPdb - - 8.3 pKi 5 nM Ki Pharmacol Biochem Behav (1994) 49: 567-71 [PMID:7862709]
ChEMBL Binding affinity to displace [3H]-SCH- 23390 against Dopamine receptor D1 B 8.72 pKi 1.9 nM Ki J Med Chem (1990) 33: 2197-2204 [PMID:1973733]
ChEMBL Compound was tested for the displacement of [3H]-SCH- 23390 from dopamine receptor D1 B 8.72 pKi 1.9 nM Ki J Med Chem (1992) 35: 502-507 [PMID:1531365]
ChEMBL Binding affinity to dopamine D1 receptor B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2010) 20: 836-840 [PMID:20061148]
ChEMBL Displacement of [3H]SCh23390 from dopamine D1 receptor expressed in mouse LTK cells by scintillation counting B 8.92 pKi 1.2 nM Ki Bioorg Med Chem Lett (2010) 20: 832-835 [PMID:20064718]
ChEMBL Binding affinity to human dopamine D1 receptor B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
ChEMBL Inhibition of [3H]SCH-23390 binding to rat striatal homogenate dopamine receptor D1 B 8.72 pKi 1.9 nM Ki J Med Chem (1989) 32: 1913-1921 [PMID:2666667]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Binding affinity to human dopamine D2 receptor B 5.91 pKi 1240 nM Ki Bioorg Med Chem Lett (2020) 30: 127563-127563 [PMID:32976928]
ChEMBL Binding affinity to dopamine D2 receptor B 6.01 pKi 980 nM Ki Bioorg Med Chem Lett (2010) 20: 836-840 [PMID:20061148]
ChEMBL Displacement of [3H]methylspiperon from dopamine D2 receptor expressed in mouse LTK cells by scintillation counting B 6.01 pKi 980 nM Ki Bioorg Med Chem Lett (2010) 20: 832-835 [PMID:20064718]
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]spiperone from rat striatal homogenate dopamine receptor D2 B 6.29 pKi 514 nM Ki J Med Chem (1989) 32: 1913-1921 [PMID:2666667]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL Displacement of radioligand from dopamine D4 receptor expressed in mouse LTK cells by scintillation counting B 5.26 pKi 5520 nM Ki Bioorg Med Chem Lett (2010) 20: 832-835 [PMID:20064718]
ChEMBL Binding affinity to dopamine D4 receptor B 5.26 pKi 5515 nM Ki Bioorg Med Chem Lett (2010) 20: 836-840 [PMID:20061148]
D5 receptor/Dopamine D5 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
GtoPdb - - 8.3 pKi - - - Nature (1991) 350: 614-9 [PMID:1826762]
ChEMBL Binding affinity to dopamine D5 receptor B 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2010) 20: 836-840 [PMID:20061148]
ChEMBL Displacement of radioligand from dopamine D5 receptor expressed in mouse LTK cells by scintillation counting B 8.7 pKi 2 nM Ki Bioorg Med Chem Lett (2010) 20: 832-835 [PMID:20064718]

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]