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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 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]