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ChEMBL ligand: CHEMBL357076 (J-113397) |
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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]diprenorphine from human cloned delta type opioid receptor expressed in CHO cell membranes by scintillation counter | B | 6.4 | pKi | >400 | nM | Ki | J Med Chem (2012) 55: 4955-4967 [PMID:22541041] |
ChEMBL | Binding affinity in CHO cells stably expressing cloned human Opioid receptor delta 1 by displacing radioligand [3H][D-Ala2,D-Leu5]enkephalin | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (1999) 42: 5061-5063 [PMID:10602690] |
ChEMBL | Displacement of [3H]naltrindole from cloned human delta opioid receptor expressed in CHO cells | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2006) 49: 847-849 [PMID:16451050] |
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human cloned kappa type opioid receptor expressed in CHO cell membranes by scintillation counter | B | 6.4 | pKi | >400 | nM | Ki | J Med Chem (2012) 55: 4955-4967 [PMID:22541041] |
ChEMBL | Displacement of [3H]U-69593 from cloned human kappa opioid receptor expressed in CHO cells | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2006) 49: 847-849 [PMID:16451050] |
ChEMBL | Binding affinity in CHO cells stably expressing cloned human Opioid receptor kappa 1 by displacing radioligand [3H]U-69593 | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (1999) 42: 5061-5063 [PMID:10602690] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Displacement of [3H]diprenorphine from human cloned mu type opioid receptor expressed in CHO cell membranes by scintillation counter | B | 6.4 | pKi | >400 | nM | Ki | J Med Chem (2012) 55: 4955-4967 [PMID:22541041] |
ChEMBL | Displacement of [3H]diprenorphin from cloned human mu opioid receptor expressed in CHO cells | B | 5.47 | pIC50 | 3400 | nM | IC50 | J Med Chem (2006) 49: 847-849 [PMID:16451050] |
ChEMBL | Binding affinity in CHO cells stably expressing cloned human Opioid receptor mu 1 by displacing diprenorphine | B | 5.66 | pIC50 | 2200 | nM | IC50 | J Med Chem (1999) 42: 5061-5063 [PMID:10602690] |
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
ChEMBL | Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay | B | 8.64 | pKi | 2.3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1347-1351 [PMID:14980696] |
GtoPdb | - | - | 8.7 | pKi | - | - | - | Eur J Pharmacol (2000) 402: 45-53 [PMID:10940356] |
ChEMBL | Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter | B | 9.39 | pKi | 0.4 | nM | Ki | J Med Chem (2012) 55: 4955-4967 [PMID:22541041] |
ChEMBL | Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells | F | 8.25 | pIC50 | 5.6 | nM | IC50 | J Med Chem (1999) 42: 5061-5063 [PMID:10602690] |
GtoPdb | - | - | 8.3 | pIC50 | - | - | IC50 | J Med Chem (1999) 42: 5061-3 [PMID:10602690] |
ChEMBL | Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (2006) 49: 847-849 [PMID:16451050] |
ChEMBL | Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (1999) 42: 5061-5063 [PMID:10602690] |
ChEMBL | Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2009) 52: 4091-4094 [PMID:19537798] |
ChEMBL | Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells | F | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2006) 49: 847-849 [PMID:16451050] |
ChEMBL | Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1999) 42: 5061-5063 [PMID:10602690] |
ChEMBL | Agonist activity on nociceptin-induced maximal [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2006) 49: 847-849 [PMID:16451050] |
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]