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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 |
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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]