(R)-Ro65-6570 [Ligand Id: 8864] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL355202 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353] | ||||||||
| ChEMBL | Affinity against Corticotropin releasing factor receptor 1 | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143] | ||||||||
| ChEMBL | Displacement of [3H]-naloxone from Opioid receptor delta 1 | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| δ receptor/Delta opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533] | ||||||||
| ChEMBL | Inhibition against binding of radioligand [Ile5,6-3H]-deltorphin to membrane from baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor delta 1 | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696] |
| D1 receptor/Dopamine D1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616] | ||||||||
| ChEMBL | Affinity against Dopamine receptor D1 | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Affinity against Dopamine receptor D2 | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Affinity against Dopamine receptor D3 | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Affinity against Dopamine receptor D4.4 | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| GABAA receptor π subunit/GABAA receptor δ subunit/GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABAA receptor α3 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABAA receptor α4 subunit/GABAA receptor ε subunit/GABAA receptor α6 subunit/GABAA receptor γ1 subunit/GABAA receptor γ3 subunit/GABAA receptor θ subunit/GABA-A receptor; anion channel in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2093872] [GtoPdb: 419, 416, 404, 410, 414, 412, 408, 406, 405, 411, 407, 417, 409, 413, 415, 418] [UniProtKB: O00591, O14764, P14867, P18505, P18507, P28472, P31644, P34903, P47869, P47870, P48169, P78334, Q16445, Q8N1C3, Q99928, Q9UN88] | ||||||||
| ChEMBL | Binding affinity for GABA-A central benzodiazepine receptor | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145] | ||||||||
| ChEMBL | Displacement of [3H]naloxone from human kappa opioid receptor | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| κ receptor/Kappa opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975] | ||||||||
| ChEMBL | Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor kappa 1 | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Displacement of [3H]naloxone from human mu opioid receptor | B | 8.4 | pKi | 3.98 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| μ receptor/Mu opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535] | ||||||||
| ChEMBL | Inhibition against binding of radioligand [N-allyl-2-3-3H]-naloxone to membrane of baby hamster kidney cells infected with forest virus encoding the cDNAs for rat Opioid receptor mu 1 | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696] |
| NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146] | ||||||||
| ChEMBL | Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor | B | 9.6 | pKi | 0.25 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - | Bioorg Med Chem Lett (1999) 9: 2343-8 [PMID:10476866] |
| GtoPdb | Stimulation of GTP-γ35S binding | - | 7.4 | pEC50 | - | - | - | Bioorg Med Chem Lett (1999) 9: 2343-8 [PMID:10476866] |
| ChEMBL | Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| NOP receptor/Nociceptin receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4503] [GtoPdb: 320] [UniProtKB: P35370] | ||||||||
| ChEMBL | Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1 | B | 9.39 | pKi | 0.41 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 831-834 [PMID:10782696] |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | Affinity against 5-hydroxytryptamine 1D receptor alpha | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Affinity against 5-hydroxytryptamine 2A receptor | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Affinity against 5-hydroxytryptamine 2C receptor | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Affinity against 5-hydroxytryptamine 6 receptor | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Affinity against 5-hydroxytryptamine 7 receptor | B | 6.5 | pKi | <316.23 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2343-2348 [PMID:10476866] |
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]
