GB88 [Ligand Id: 6658] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL2431617 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| PAR2/Proteinase-activated receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5963] [GtoPdb: 348] [UniProtKB: P55085] | ||||||||
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 986-991 [PMID:26725028] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay | B | 5.02 | pIC50 | 9600 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 986-991 [PMID:26725028] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay | F | 5.44 | pIC50 | 3600 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1179-1184 [PMID:27994760] |
| ChEMBL | Antagonist activity at protease-activated receptor 2 (unknown origin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | Bioorg Med Chem (2015) 23: 7717-7727 [PMID:26631441] |
| GtoPdb | - | - | 5.7 | pIC50 | 2000 | nM | IC50 | Br J Pharmacol (2012) 165: 1413-23 [PMID:21806599] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay | F | 5.8 | pIC50 | 1584.89 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1179-1184 [PMID:27994760] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay | B | 5.9 | pIC50 | 1258.93 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 986-991 [PMID:26725028] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay | F | 5.96 | pIC50 | 1100 | nM | IC50 | ACS Med Chem Lett (2016) 7: 1179-1184 [PMID:27994760] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 986-991 [PMID:26725028] |
| ChEMBL | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization | F | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2013) 56: 7477-7497 [PMID:23895492] |
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]
