ChEMBL ligand: CHEMBL216981 (Mk-7123, Navarixin, PS-291822, PS291822, SCH-527123, SCH527123)
CCR7/C-C chemokine receptor type 7 in Human [ChEMBL: CHEMBL4594] [GtoPdb: 64] [UniProtKB: P32248] There should be some charts here, you may need to enable JavaScript!
CXCR2 in Human [GtoPdb: 69] [UniProtKB: P25025] CXCR2/C-X-C chemokine receptor type 2 in Mouse [ChEMBL: CHEMBL4105830] [GtoPdb: 69] [UniProtKB: P35343] There should be some charts here, you may need to enable JavaScript!
CXCR1/Interleukin-8 receptor A in Human [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024] There should be some charts here, you may need to enable JavaScript!
CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025] 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
CCR7/C-C chemokine receptor type 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4594] [GtoPdb: 64] [UniProtKB: P32248]
ChEMBL	Antagonist activity at CCR7 in human CD4 cells by fluorescence based calcium mobilization assay	F	5.33	pIC50	4680	nM	IC50	Eur J Med Chem (2023) 251: 115240-115240 [PMID:36924670]
CXCR2 in Human [GtoPdb: 69] [UniProtKB: P25025]
GtoPdb	-	-	10.31	pIC50	0.05	nM	IC50	Pharmacol Rev (2014) 66: 1-79 [PMID:24218476]; J Med Chem (2006) 49: 7603-6 [PMID:17181143]
CXCR2/C-X-C chemokine receptor type 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105830] [GtoPdb: 69] [UniProtKB: P35343]
ChEMBL	Antagonist activity at CXCR2 in C57 mouse whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation preincubated for 1 hr followed by GROalpha stimulation measured after 10 mins by FITC-staining based FACS analysis	B	8.09	pIC50	8.1	nM	IC50	J Med Chem (2018) 61: 2518-2532 [PMID:29406702]
CXCR1/Interleukin-8 receptor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
ChEMBL	Binding affinity to NanoLuc fused Snap CXCR1 (unknown origin) expressed in HEK293 cell membrane assessed as inhibition constant using furimazine as substrate incubated with substrate for 5 mins and measured every 15 secs for 60 mins by luminescence based NanoBRET fluorescent binding assay	B	7.66	pKi	21.88	nM	Ki	J Med Chem (2023) 66: 12911-12930 [PMID:37523859]
ChEMBL	Binding affinity to CXCR1	B	7.7	pKi	20	nM	Ki	Bioorg Med Chem Lett (2009) 19: 1431-1433 [PMID:19196511]
ChEMBL	Displacement of [125I]IL8 from human CXCR1 expressed in CHO cells by SPA	B	7.74	pKi	18	nM	Ki	Bioorg Med Chem Lett (2007) 17: 3778-3783 [PMID:17459706]
ChEMBL	Antagonist activity at CXCR1 (unknown origin) stably expressed in HEK293 cells assessed as reduction in IL-8-induced intracellular calcium change incubated for 15 mins followed by IL-8-stimulation and measured after 15 mins by cAMP-d2/Eu-Anti-cAM based fluorescence assay	F	6.7	pIC50	198.3	nM	IC50	Eur J Med Chem (2020) 187: 111914-111914 [PMID:31806538]
ChEMBL	Antagonist activity at CXCR1 (unknown origin) expressed in HEK293 cells assessed as suppression of IL-8-induced inhibition of forskolin-induced cAMP formation preincubated for 15 mins followed by forskolin and IL-8 stimulation and measured after 15 mins by cAMP-d2 and Eu-Anti-cAMP based fluorescence assay	F	6.7	pIC50	198.3	nM	IC50	Eur J Med Chem (2020) 205: 112537-112537 [PMID:32768738]
ChEMBL	Antagonist activity in CXCR1 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay	F	6.8	pIC50	160	nM	IC50	ACS Med Chem Lett (2021) 12: 836-845 [PMID:34055234]
ChEMBL	Displacement of [125I]hCXCL8 from human CXCR1 receptor expressed in BaF3 cells	B	7.44	pIC50	36	nM	IC50	J Med Chem (2006) 49: 7603-7606 [PMID:17181143]
ChEMBL	Antagonist activity at CXCR1 (unknown origin)	B	7.44	pIC50	36	nM	IC50	RSC Med Chem (2021) 12: 1046-1064 [PMID:34355177]
ChEMBL	Binding affinity to CXCR1	B	8.41	pIC50	3.9	nM	IC50	J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
GtoPdb	-	-	8.41	pIC50	3.9	nM	IC50	Pharmacol Rev (2014) 66: 1-79 [PMID:24218476]; J Med Chem (2006) 49: 7603-6 [PMID:17181143]
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
ChEMBL	Binding affinity to CXCL2 (unknown origin)	B	10.3	pKd	0.05	nM	Kd	J Med Chem (2023) 66: 12911-12930 [PMID:37523859]
ChEMBL	Displacement of [3H]Sch527123 from human CXCR2 assessed as dissociation constant measured every 30 secs for 48 hrs by radioligand binding assay	B	10.31	pKd	0.05	nM	Kd	J Med Chem (2023) 66: 12911-12930 [PMID:37523859]
ChEMBL	Displacement of [125I]IL8 from human CXCR2 expressed in CHO cells by SPA	B	8.3	pKi	5	nM	Ki	Bioorg Med Chem Lett (2007) 17: 3778-3783 [PMID:17459706]
ChEMBL	Displacement of human [125I]IL-8 from human CXCR2	B	8.3	pKi	5	nM	Ki	Bioorg Med Chem Lett (2009) 19: 4446-4449 [PMID:19525110]
ChEMBL	Binding affinity to CXCR2	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem Lett (2009) 19: 1431-1433 [PMID:19196511]
ChEMBL	Binding affinity to NanoLuc fused Snap CXCR2 (unknown origin) expressed in HEK293 cell membrane assessed as inhibition constant using furimazine as substrate incubated with substrate for 5 mins and measured every 15 secs for 60 mins by luminescence based NanoBRET fluorescent binding assay	B	9.19	pKi	0.65	nM	Ki	J Med Chem (2023) 66: 12911-12930 [PMID:37523859]
ChEMBL	Antagonist activity at CXCR2 in human whole blood assessed as inhibition of GROalpha-stimulated CD11b upregulation preincubated for 15 mins followed by GROalpha stimulation measured after 15 mins by FITC-staining based FACS analysis	B	6.17	pIC50	680	nM	IC50	J Med Chem (2018) 61: 2518-2532 [PMID:29406702]
ChEMBL	Antagonist activity at CXCR2 in human whole blood by CD11b assay	B	6.35	pIC50	450	nM	IC50	Bioorg Med Chem Lett (2014) 24: 5493-5496 [PMID:25455491]
ChEMBL	Antagonist activity in CXCR2 (unknown origin) expressed in human HEK293 cells co-expressing Galpha16 assessed as reduction in calcium immobilization pretreated with Fluo-4AM for 45 mins followed by compound addition and measured after 10 mins by Fluo-4AM dye based fluorescence assay	F	8	pIC50	10	nM	IC50	ACS Med Chem Lett (2021) 12: 836-845 [PMID:34055234]
ChEMBL	Antagonist activity at CXCR2 in human CD4 cells by fluorescence based calcium mobilization assay	F	8.3	pIC50	5	nM	IC50	Eur J Med Chem (2023) 251: 115240-115240 [PMID:36924670]
ChEMBL	Inhibition of CXCR2 (unknown origin) expressed in HEK293 coexpressing snap-CXCR2-LGBit and beta-arrestin2-SMBit using furimazine as substrate preincubated for 1 hr followed by substrate addition and measured after 5 mins by bioluminescence based NanoBiT assay	F	8.54	pIC50	2.88	nM	IC50	J Med Chem (2023) 66: 12911-12930 [PMID:37523859]
ChEMBL	Antagonist activity at CXCR2 (unknown origin)	B	8.59	pIC50	2.6	nM	IC50	RSC Med Chem (2021) 12: 1046-1064 [PMID:34355177]
ChEMBL	Displacement of [125I]hCXCL8 from human CXCR2 receptor expressed in BaF3 cells	B	8.59	pIC50	2.6	nM	IC50	J Med Chem (2006) 49: 7603-7606 [PMID:17181143]
ChEMBL	Inhibition of CXCL1-induced human neutrophil chemotaxis	F	9	pIC50	<1	nM	IC50	J Med Chem (2006) 49: 7603-7606 [PMID:17181143]
ChEMBL	Binding affinity to CXCR2	B	10.31	pIC50	0.05	nM	IC50	J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
GtoPdb	-	-	10.31	pIC50	0.05	nM	IC50	Pharmacol Rev (2014) 66: 1-79 [PMID:24218476]; J Med Chem (2006) 49: 7603-6 [PMID:17181143]

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]