JTC-801 [Ligand Id: 1692] 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: CHEMBL140979 (JTC-801)
  • δ receptor/Delta opioid receptor in Human [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
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]
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]
There should be some charts here, you may need to enable JavaScript!
  • NOP receptor/Nociceptin receptor in Human [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
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
δ receptor/Delta opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL236] [GtoPdb: 317] [UniProtKB: P41143]
ChEMBL Inhibition of [3H]naltrindole (0.55 nM) binding from human Opioid receptor delta 1 expressed in CHO-K1 cells. B 5.06 pKi 8647.2 nM Ki J Med Chem (2000) 43: 4667-4677 [PMID:11101358]
ChEMBL Binding affinity for opioid receptor type, human Opioid receptor delta 1 expressed in membrane homogenates of COS-1 or CHO cells B 5.06 pKi 8647 nM Ki J Med Chem (2002) 45: 5353-5357 [PMID:12431062]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Inhibition of [3H]naltrindole (0.55 nM) binding from human Opioid receptor kappa 1 B 5.98 pKi 1057.5 nM Ki J Med Chem (2000) 43: 4667-4677 [PMID:11101358]
ChEMBL Binding affinity for opioid receptor type, human Opioid receptor kappa 1 expressed in membrane homogenates of COS-1 or CHO cells B 5.98 pKi 1057 nM Ki J Med Chem (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Displacement of [3H]-naltrindole from human kappa opioid receptor expressed in human HEK293 cells after 2 hrs by scintillation counting B 5.12 pIC50 7512 nM IC50 Eur J Med Chem (2011) 46: 1207-1221 [PMID:21330016]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Inhibition of [3H]diprenorphine (0.33 nM) binding from human Opioid receptor mu 1 expressed in CHO-K1 cells. B 6.99 pKi 102.9 nM Ki J Med Chem (2000) 43: 4667-4677 [PMID:11101358]
ChEMBL Binding affinity for opioid receptor type, human Opioid receptor mu 1 expressed in membrane homogenates of COS-1 or CHO cells B 6.99 pKi 102 nM Ki J Med Chem (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Displacement of [3H]-naltrindole from human mu opioid receptor expressed in CHO cells after 2 hrs by scintillation counting B 5.82 pIC50 1507 nM IC50 Eur J Med Chem (2011) 46: 1207-1221 [PMID:21330016]
NOP receptor/Nociceptin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2014] [GtoPdb: 320] [UniProtKB: P41146]
ChEMBL Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells B 8.09 pKi 8.2 nM Ki J Med Chem (2002) 45: 5353-5357 [PMID:12431062]
ChEMBL Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells. B 8.09 pKi 8.2 nM Ki J Med Chem (2000) 43: 4667-4677 [PMID:11101358]
GtoPdb - - 8.1 pKi - - - J Med Chem (2000) 43: 4667-77 [PMID:11101358]
ChEMBL Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting B 7.52 pIC50 30 nM IC50 Eur J Med Chem (2011) 46: 1207-1221 [PMID:21330016]

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]