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ChEMBL ligand: CHEMBL38576 (ICI-199441) |
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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 | Inhibitory constant against human Opioid receptor delta 1 using [3H]diprenorphine as radio ligand | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2647-2652 [PMID:15863335] |
ChEMBL | Displacement of [3H]diprenorphine from human delta opioid receptor expressed in CHO-K1 cells | B | 7.62 | pKi | 24 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3667-3671 [PMID:18487043] |
ChEMBL | Tested for inhibitory concentration against [3H]DPDPE binding at sites of delta-opioid receptor in guinea pig brain membrane | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | In vitro binding affinity towards Opioid receptor kappa 1 by displacement of bound [3H]U-69593 | B | 10.27 | pKi | 0.05 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2567-2570 [PMID:11086731] |
ChEMBL | Displacement of [3H]diprenorphine from human kappa opioid receptor expressed in CHO-K1 cells | B | 10.36 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3667-3671 [PMID:18487043] |
ChEMBL | In vitro binding affinity for human kappa opioid receptor was determined by using [3H]diprenorphine as radioligand | B | 10.37 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1279-1282 [PMID:15713370] |
ChEMBL | Inhibitory constant against human Opioid receptor kappa using [3H]diprenorphine as radio ligand | B | 10.4 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2647-2652 [PMID:15863335] |
GtoPdb | Displacement of [3H]diprenorphine from human κ opioid receptor | - | 10.4 | pKi | 0.04 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1279-82 [PMID:15713370] |
ChEMBL | Agonist activity at kappa opioid receptor | F | 9.4 | pEC50 | 0.4 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3716-3719 [PMID:18524591] |
ChEMBL | Agonist activity assessed by ability to stimulate [35S]GTP gammaS binding to opioid receptor kappa in human membranes | F | 9.52 | pEC50 | 0.3 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 2647-2652 [PMID:15863335] |
ChEMBL | Agonist activity at human kappa opioid receptor transfected in CHO cells by [35S]GTP-gamma-S binding assay | F | 9.52 | pEC50 | 0.3 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 3667-3671 [PMID:18487043] |
κ receptor/Kappa opioid receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4329] [GtoPdb: 318] [UniProtKB: P33534] | ||||||||
ChEMBL | Inhibitory activity against Opioid receptor kappa 1 in electrically stimulated mouse vas deferens (MVD) preparation. | B | 8.6 | pIC50 | 2.5 | nM | IC50 | J Med Chem (1996) 39: 1729-1735 [PMID:8648612] |
Kappa opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3952] [UniProtKB: P41144] | ||||||||
ChEMBL | Binding affinity against opioid receptor kappa, in guinea pig brain membrane, using [3H]bremazocine as the radioligand. | B | 8.16 | pIC50 | 6.9 | nM | IC50 | J Med Chem (1991) 34: 3149-3158 [PMID:1659636] |
ChEMBL | Compound was evaluated for the Opioid receptor kappa 1 affinity using guinea pig brain membranes. | B | 8.16 | pIC50 | 6.9 | nM | IC50 | J Med Chem (1991) 34: 181-189 [PMID:1846918] |
ChEMBL | Tested for inhibitory concentration against [3H]U-69593 binding at sites of kappa-opioid receptor in guinea pig brain membrane | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
ChEMBL | Inhibitory activity against Opioid receptor kappa 1 in electrically stimulated guinea pig longitudinal ileal muscle (GPI) preparation. | B | 9.57 | pIC50 | 0.27 | nM | IC50 | J Med Chem (1996) 39: 1729-1735 [PMID:8648612] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Inhibitory constant against human Opioid receptor mu 1 using [3H]diprenorphine as radio ligand | B | 7.28 | pKi | 53 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 2647-2652 [PMID:15863335] |
ChEMBL | Displacement of [3H]diprenorphine from human mu opioid receptor expressed in CHO-K1 cells | B | 7.28 | pKi | 53 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3667-3671 [PMID:18487043] |
GtoPdb | Displacement of [3H]diprenorphine from human μ opioid receptor expressed in CHO-K1 cells | - | 7.28 | pKi | 53 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3667-71 [PMID:18487043] |
Mu opioid receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4354] [UniProtKB: P97266] | ||||||||
ChEMBL | Tested for inhibitory concentration against [3H]DAMGO binding at sites of mu-opioid receptor in guinea pig brain membrane | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (1994) 37: 2856-2864 [PMID:8071934] |
UT receptor/Urotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3764] [GtoPdb: 365] [UniProtKB: Q9UKP6] | ||||||||
ChEMBL | Binding affinity to human urotensin-2 receptor | B | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3716-3719 [PMID:18524591] |
ChEMBL data shown on this page come from version 32:
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]