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]
  • 8.72
1 CHEMBL298406_lig_chart_1 Dopamine D1 receptor HumanRat
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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]
  • 6.29
2 CHEMBL298406_lig_chart_2 Dopamine D2 receptor HumanRat
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • 5.26
3 CHEMBL298406_lig_chart_3 Dopamine D4 receptor Human
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  • D5 receptor/Dopamine D5 receptor in Human [ChEMBL: CHEMBL1850] [GtoPdb: 218] [UniProtKB: P21918]
  • 8.7
4 CHEMBL298406_lig_chart_4 Dopamine D5 receptor Human
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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]
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 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]