SB-649868 [Ligand Id: 4461] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1272307 (GSK649868, Sb-649868, SB-649868) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| OX1 receptor/Orexin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613] | ||||||||
| GtoPdb | - | - | 9.1 | pKi | 0.79 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-7 [PMID:21831639] |
| ChEMBL | Displacement of [3H]almorexant from recombinant human OX1R expressed in CHO cells | B | 9.12 | pKi | 0.76 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-5567 [PMID:21831639] |
| ChEMBL | Antagonist activity against human orexin 1 receptor expressed in CHO cells assessed as effect in calcium mobilization by FLIPR assay | F | 9.5 | pKi | 0.32 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 6405-6407 [PMID:20933413] |
| ChEMBL | Antagonist activity at recombinant human OX1R expressed in CHO cells by FLIPR calcium based functional assay | F | 9.5 | pKi | 0.32 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-5567 [PMID:21831639] |
| ChEMBL | Binding affinity to orexin receptor 1 (unknown origin) | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - |
J Med Chem (2010) 53: 5320-32 [PMID:20565075]; Bioorg Med Chem Lett (2011) 21: 5562-7 [PMID:21831639]; Front Neurosci (2013) 7: 230 [PMID:24376396] |
| OX1 receptor in Mouse [GtoPdb: 321] [UniProtKB: P58307] | ||||||||
| OX1 receptor/Orexin receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075232] [GtoPdb: 321] [UniProtKB: P56718] | ||||||||
| ChEMBL | Antagonist activity at recombinant rat OX1R expressed in CHO cells by FLIPR calcium based functional assay | F | 9.93 | pKi | 0.12 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-5567 [PMID:21831639] |
| OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614] | ||||||||
| ChEMBL | Displacement of [125I]-Orexin A from human OX2R expressed in CHO cells after 30 mins by topcount analysis | B | 8.07 | pKi | 8.5 | nM | Ki | Bioorg Med Chem (2014) 22: 6071-6088 [PMID:25267004] |
| ChEMBL | Displacement of [3H]almorexant from recombinant human OX2R expressed in CHO cells | B | 8.89 | pKi | 1.29 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-5567 [PMID:21831639] |
| ChEMBL | Binding affinity to orexin receptor 2 (unknown origin) | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
| ChEMBL | Antagonist activity against human orexin 2 receptor expressed in CHO cells assessed as effect in calcium mobilization by FLIPR assay | F | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 6405-6407 [PMID:20933413] |
| ChEMBL | Antagonist activity at recombinant human OX2R expressed in CHO cells by FLIPR calcium based functional assay | F | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-5567 [PMID:21831639] |
| GtoPdb | - | - | 9.8 | pKi | - | - | Ki |
J Med Chem (2010) 53: 5320-32 [PMID:20565075]; Front Neurosci (2013) 7: 230 [PMID:24376396] |
| OX2 receptor in Mouse [GtoPdb: 322] [UniProtKB: P58308, P58308-2] | ||||||||
| OX2 receptor/Orexin receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1275216] [GtoPdb: 322] [UniProtKB: P56719] | ||||||||
| ChEMBL | Antagonist activity at recombinant rat OX2R expressed in CHO cells by FLIPR calcium based functional assay | F | 10.11 | pKi | 0.08 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5562-5567 [PMID:21831639] |
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]
