vercirnon [Ligand Id: 9046] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2178578 (CCX282, CCX-282-B, GSK-1605786, GSK1605786, Vercirnon, Verecimon) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CCR9/C-C chemokine receptor type 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5815] [GtoPdb: 66] [UniProtKB: P51686] | ||||||||
| ChEMBL | Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCl25-mediated cell migration preincubated for 30 mins followed CCL25 addition incubated for 2 hrs by ChemoTx plate system | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2016) 59: 3098-3111 [PMID:26987013] |
| ChEMBL | Antagonist activity at CCR9A receptor (unknown origin) overexpressed in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | F | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2016) 59: 3098-3111 [PMID:26987013] |
| ChEMBL | Antagonist activity at CCR9 receptor in human MOLT4 cells assessed as inhibition of CCL25-induced increase in intracellular calcium level preincubated for 1 hr followed CCL25 addition by FLIPR assay | F | 8.96 | pKi | 1.1 | nM | Ki | J Med Chem (2016) 59: 3098-3111 [PMID:26987013] |
| ChEMBL | Antagonist activity against CCR9 in human MOLT4 cells assessed as inhibition of human recombinant TECK-induced cell migration pre-treated for 15 mins before TECK stimulation for 150 mins by fluorescence based assay | F | 6 | pIC50 | <1000 | nM | IC50 | US-7420055-B2. Aryl sulfonamides (2008) |
| ChEMBL | Antagonist activity against CCR9 in human MOLT4 cells assessed as inhibition of human recombinant TECK-induced calcium response pre-treated before TECK stimulation by Flou-4-AM dye based FLIPR assay | F | 6 | pIC50 | <1000 | nM | IC50 | US-7420055-B2. Aryl sulfonamides (2008) |
| ChEMBL | Antagonist activity at CCR9 receptor (unknown origin) by serum chemotaxis assay | B | 6.27 | pIC50 | 539 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3661-3664 [PMID:26117562] |
| ChEMBL | Antagonist activity against CCR9 in human MOLT4 cells assessed as inhibition of human recombinant TECK-induced cell migration pre-treated for 15 mins before TECK stimulation for 150 mins by fluorescence based assay | F | 7 | pIC50 | <100 | nM | IC50 | US-7582661-B2. Aryl sulfonamides (2009) |
| ChEMBL | Antagonist activity against CCR9 in human MOLT4 cells assessed as inhibition of human recombinant TECK-induced calcium response pre-treated before TECK stimulation by Flou-4-AM dye based FLIPR assay | F | 7 | pIC50 | <100 | nM | IC50 | US-7582661-B2. Aryl sulfonamides (2009) |
| ChEMBL | Antagonist activity at CCR9 receptor (unknown origin) by buffer chemotaxis assay | B | 7.96 | pIC50 | 11 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3661-3664 [PMID:26117562] |
| ChEMBL | Antagonist activity at CCR9 receptor (unknown origin) assessed as inhibition of TECK-induced calcium mobilization incubated for 10 mins prior to TECK induction | F | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3661-3664 [PMID:26117562] |
| GtoPdb | Measuring inhibition of antagonist tracer [3H]CCX807 binding to human Molt-4 cells. | - | 8.22 | pIC50 | 6 | nM | IC50 | J Pharmacol Exp Ther (2010) 335: 61-9 [PMID:20660125] |
| ChEMBL | Binding affinity to CCR9 | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| ChEMBL | Antagonist activity at CCR9 (unknown origin) assessed as inhibition of TECK-stimulated calcium mobilization preincubated for 10 mins followed by agonist addition measured for 90 sec by fluo-8 dye-based FLIPR assay | F | 8.3 | pIC50 | 5 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3322-3325 [PMID:27256913] |
| ChEMBL | Antagonist activity at CCR9 assessed as inhibition of CCL25-induced chemotaxis by cell based assay | F | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| ChEMBL | Antagonist activity at recombinant human CCR9A expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Eur J Med Chem (2020) 185: 111805-111805 [PMID:31703817] |
| ChEMBL | Antagonist activity at recombinant human CCR9B expressed in BAF3 cells assessed as reduction in CCL25-induced chemotaxis preincubated for 10 mins followed by addition of CCL25 and measured after 120 min by QUANT dye based fluorescence assay | B | 8.59 | pIC50 | 2.6 | nM | IC50 | Eur J Med Chem (2020) 185: 111805-111805 [PMID:31703817] |
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]
