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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 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]