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ChEMBL ligand: CHEMBL2180638 (3-[2-[(Cyclopropylmethyl)(Phenethyl)Amino]Ethyl]Phenol) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 | 6.93 | pKi | 118 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
GtoPdb | - | - | 6.93 | pKi | 118 | nM | Ki | J Med Chem (2012) 55: 10302-6 [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 | 6.74 | pEC50 | 181 | 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] | ||||||||
GtoPdb | - | - | 6.77 | pKi | 168 | nM | Ki | J Med Chem (2012) 55: 10302-6 [PMID:23134120] |
ChEMBL | Displacement of [3H]YM-09151-2 from human dopamine D3 receptor expressed in CHOp cells | B | 6.77 | pKi | 168 | nM | Ki | 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 | 7.49 | pEC50 | 32.2 | 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 | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
GtoPdb | - | - | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2012) 55: 10302-6 [PMID:23134120] |
ChEMBL | Inhibition of kappa opioid receptor (unknown origin) assessed as increase in beta-arrestin 2 recruitment | B | 6.35 | pEC50 | 449 | nM | EC50 | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
ChEMBL | Inhibition of kappa opioid receptor (unknown origin) by [35S]-GTPgammaS binding assay | F | 7.44 | pEC50 | 36.7 | nM | EC50 | Eur J Med Chem (2019) 183: 111701-111701 [PMID:31550662] |
ChEMBL | Agonist activity at human kappa opioid receptor expressed in CHO cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay | F | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
GtoPdb | Measuring stimulation of [35S]GTPγS binding. | - | 7.46 | pEC50 | 35 | nM | EC50 | J Med Chem (2012) 55: 10302-6 [PMID:23134120] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
GtoPdb | - | - | 6.08 | pKi | 826 | nM | Ki | J Med Chem (2012) 55: 10302-6 [PMID:23134120] |
ChEMBL | Displacement of [3H]DAMGO from human mu opioid receptor expressed in CHO cell membranes incubated for 60 mins by liquid scintillation counting | B | 6.08 | pKi | 826 | nM | Ki | J Med Chem (2012) 55: 10302-10306 [PMID:23134120] |
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]