ChEMBL ligand: CHEMBL2178578 (CCX282, CCX-282-B, GSK-1605786, GSK1605786, Vercirnon, Verecimon)
CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597] There should be some charts here, you may need to enable JavaScript!
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
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL	Binding affinity to CCR2 (unknown origin) assessed as dissociation constant	B	10	pKd	0.1	nM	Kd	J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
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 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]