HS665 [Ligand Id: 9189] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2180639 (3-[2-[(Cyclobutylmethyl)(Phenethyl)Amino]Ethyl]Phenol)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Displacement of [3H]pCl-DPDPE from human delta opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting B 5 pKi >10000 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL Displacement of [3H]SCH-23390 from human dopamine D1 receptor expressed in LHD1 cells B 5 pKi >10000 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [3H]YM-09151-2 from human dopamine D2 receptor expressed in CHOp cells B 6.35 pKi 450 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
GtoPdb - - 6.35 pKi 450 nM Ki J. Med. Chem. (2012) 55: 10302-6 [PMID:23134120]
ChEMBL Antagonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay F 5.78 pIC50 1647 nM IC50 J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Agonist activity at human dopamine D2 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay F 5 pEC50 >10000 nM EC50 J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells B 6.55 pKi 282 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
GtoPdb - - 6.55 pKi 282 nM Ki J. Med. Chem. (2012) 55: 10302-6 [PMID:23134120]
ChEMBL Antagonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as inhibition of quinpirol-induced mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay F 6.02 pIC50 953 nM IC50 J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
ChEMBL Agonist activity at human dopamine D3 receptor expressed in CHOp cells assessed as stimulation of mitogenesis incubated for 24 hrs by [3H]thymidine incorporation assay F 5 pEC50 >10000 nM EC50 J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting B 9.31 pKi 0.49 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
GtoPdb - - 9.31 pKi 0.49 nM Ki J. Med. Chem. (2012) 55: 10302-6 [PMID:23134120]
GtoPdb Measuring stimulation of [35S]GTPγS binding. - 8.44 pEC50 3.62 nM EC50 J. Med. Chem. (2012) 55: 10302-6 [PMID:23134120]
ChEMBL Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay F 8.44 pEC50 3.62 nM EC50 J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting B 6.27 pKi 542 nM Ki J. Med. Chem. (2012) 55: 10302-10306 [PMID:23134120]
GtoPdb - - 6.27 pKi 542 nM Ki J. Med. Chem. (2012) 55: 10302-6 [PMID:23134120]

ChEMBL data shown on this page come from version 27:

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]