vercirnon [Ligand Id: 9046] 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: CHEMBL2178578 (Vercirnon, Verecimon, CCX-282, GSK-1605786, CCX-282-B, GSK1605786)
  • CCR9/C-C chemokine receptor type 9 in Human [ChEMBL: CHEMBL5815] [GtoPdb: 66] [UniProtKB: P51686]
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
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 B 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 B 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 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 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 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 B 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 B 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 data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]