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 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]
