ChEMBL ligand: CHEMBL2178578 (CCX282, CCX-282-B, GSK1605786, GSK-1605786, Vercirnon, Verecimon)
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	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 32:

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]