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 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]
