navarixin [Ligand Id: 8497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL216981 (Mk-7123, Navarixin, PS291822, PS-291822, SCH527123, SCH-527123)
  • CXCR2 in Human [GtoPdb: 69] [UniProtKB: P25025]
  • CXCR2/C-X-C chemokine receptor type 2 in Mouse [ChEMBL: CHEMBL4105830] [GtoPdb: 69] [UniProtKB: P35343]
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  • CXCR1/Interleukin-8 receptor A in Human [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
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  • CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 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 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 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 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 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 31:

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]