(R)-Ro65-6570 [Ligand Id: 8864] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL355202
  • CRF1 receptor/Corticotropin releasing factor receptor 1 in Rat [ChEMBL: CHEMBL4649] [GtoPdb: 212] [UniProtKB: P35353]
There should be some charts here, you may need to enable JavaScript!
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
  • δ receptor/Delta opioid receptor in Rat [ChEMBL: CHEMBL269] [GtoPdb: 317] [UniProtKB: P33533]
There should be some charts here, you may need to enable JavaScript!
  • D1 receptor/Dopamine D1 receptor in Mouse [ChEMBL: CHEMBL3071] [GtoPdb: 214] [UniProtKB: Q61616]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
  • κ receptor/Kappa opioid receptor in Rat [ChEMBL: CHEMBL3614] [GtoPdb: 318] [UniProtKB: P34975]
There should be some charts here, you may need to enable JavaScript!
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
  • μ receptor/Mu opioid receptor in Rat [ChEMBL: CHEMBL270] [GtoPdb: 319] [UniProtKB: P33535]
There should be some charts here, you may need to enable JavaScript!
  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
  • NOP receptor/Nociceptin receptor in Rat [ChEMBL: CHEMBL4503] [GtoPdb: 320] [UniProtKB: P35370]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
There should be some charts here, you may need to enable JavaScript!
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 33:

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]