mavorixafor [Ligand Id: 8580] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL518924 (Amd070, Amd 070, AMD070, AMD-070, AMD11070, AMD-11070, Cxcr4 inhibitor x4p-001, Mavorixafor, X4p001, X 4P-001, X4P-001)
  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
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  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • CCR4/C-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
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  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
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  • CXCR4/C-X-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
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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
CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
ChEMBL Displacement of radiolabeled MIP1alpha from CCR1 receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL Displacement of radiolabeled MCP1 from CCR2b receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]
CCR4/C-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
ChEMBL Displacement of radiolabeled TARC from CCR4 receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
ChEMBL Displacement of radiolabeled MIP1beta from CCR5 receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]
CXCR4/C-X-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
GtoPdb Assay using 125I-SDF-1α as tracer, in Cf2Th cells expressing hCXCR4. - 7.96 pKi 11 nM Ki Mol Pharmacol (2008) 74: 1485-95 [PMID:18768385]
ChEMBL Antagonist activity at CXCR4 in human PBMC assessed as inhibition of HIV-1 3B infection B 7.52 pIC50 30 nM IC50 ACS Med. Chem. Lett. (2013) 4: 1025-1030 [PMID:24936240]
ChEMBL Displacement of [125I]SDF-1-alpha from CXCR4 in human CEM-CCRF cells by liquid scintillation counting B 7.89 pIC50 13 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]
GtoPdb Displacement of [125I]SDF-1α binding from CXCR4 in human CEM-CCRF cells by liquid scintillation counting. - 7.89 pIC50 13 nM IC50 J Med Chem (2010) 53: 3376-88 [PMID:20297846]
ChEMBL Antagonist activity at CXCR4 receptor in human CCRF-CEM cells assessed as inhibition of SDF-1alpha-induced calcium release preincubated for 25 mins followed by SDF-1alpha addition and monitered for 90 sec F 8.29 pIC50 5.18 nM IC50 ACS Med Chem Lett (2021) 12: 1605-1612 [PMID:34676043]
ChEMBL Antagonist activity at CXCR4 in human CCRF-CEM cells assessed as inhibition of SDS1alpha-induced calcium flux pretreated for 25 mins followed by SDS1alpha addition measured for 90 secs by calcium-dye based assay F 8.3 pIC50 5 nM IC50 ACS Med Chem Lett (2018) 9: 446-451 [PMID:29795757]
CXCR1/Interleukin-8 receptor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
ChEMBL Displacement of radiolabeled IL8 from CXCR1 receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
ChEMBL Displacement of radiolabeled IL8 from CXCR2 receptor B 5 pIC50 >10000 nM IC50 J. Med. Chem. (2010) 53: 3376-3388 [PMID:20297846]

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]