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 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]
