RO5101576 [Ligand Id: 6158] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1098560 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in CHO cells assessed as reduction of current amplitude | B | 5.52 | pIC50 | >3000 | nM | IC50 | J Med Chem (2010) 53: 3502-3516 [PMID:20380377] |
| BLT1 receptor/Leukotriene B4 receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3911] [GtoPdb: 267] [UniProtKB: Q15722] | ||||||||
| ChEMBL | Antagonist activity at FLAG-tagged human BLT1 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge | F | 6.94 | pIC50 | 114 | nM | IC50 | J Med Chem (2010) 53: 3502-3516 [PMID:20380377] |
| GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Prostaglandins Other Lipid Mediat (2010) 92: 33-43 [PMID:20214997] |
| ChEMBL | Antagonist activity at BLT1 receptor expressed in human HL60 cells assessed as inhibition of LTB4-stimulated calcium flux after 30 mins | F | 9.36 | pIC50 | 0.44 | nM | IC50 | J Med Chem (2010) 53: 3502-3516 [PMID:20380377] |
| BLT2 receptor/Leukotriene B4 receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3191] [GtoPdb: 268] [UniProtKB: Q9NPC1] | ||||||||
| ChEMBL | Antagonist activity at FLAG-tagged human BLT2 receptor expressed in HEK293 cells assessed as inhibition of LTB4-stimulated calcium mobilization preincubated for 10 mins before LTB4 challenge | F | 6.79 | pIC50 | 164 | nM | IC50 | J Med Chem (2010) 53: 3502-3516 [PMID:20380377] |
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]
