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

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ChEMBL ligand: CHEMBL518924 (Amd 070, AMD-070, AMD070, AMD-11070, AMD11070, Cxcr4 inhibitor x4p-001, Mavorixafor, X4p001, X 4P-001, X4P-001)
  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
Created with Highcharts 10.3.3ValuesChart context menuAlpha-2a adrenergic receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
Created with Highcharts 10.3.3ValuesChart context menuC-C chemokine receptor type 1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
Created with Highcharts 10.3.3ValuesChart context menuC-C chemokine receptor type 2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • CCR4/C-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
Created with Highcharts 10.3.3ValuesChart context menuC-C chemokine receptor type 4pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
Created with Highcharts 10.3.3ValuesChart context menuC-C chemokine receptor type 5pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • CXCR4/C-X-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
Created with Highcharts 10.3.3ValuesChart context menuC-X-C chemokine receptor type 4pKd HumanpKi HumanpIC50 HumanpEC50 Human0246810Highcharts.com
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
Created with Highcharts 10.3.3ValuesChart context menuDopamine D2 receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • CXCR1/Interleukin-8 receptor A in Human [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
Created with Highcharts 10.3.3ValuesChart context menuInterleukin-8 receptor ApKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
Created with Highcharts 10.3.3ValuesChart context menuInterleukin-8 receptor BpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • κ receptor/Kappa opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
Created with Highcharts 10.3.3ValuesChart context menuKappa opioid receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
Created with Highcharts 10.3.3ValuesChart context menuMu opioid receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
Created with Highcharts 10.3.3ValuesChart context menuMuscarinic acetylcholine receptor M2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
Created with Highcharts 10.3.3ValuesChart context menuNeuronal acetylcholine receptor protein alpha-7 subunitpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL Inhibition of alpha 2A adrenergic receptor (unknown origin) B 4.52 pIC50 >30000 nM IC50 J Med Chem (2022) 65: 4058-4084 [PMID:35179893]
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]
ChEMBL Binding affinity to CXCR4 (unknown origin) assessed as inhibition constant B 7.64 pKi 23 nM Ki J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
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]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Inhibition of dopamine D2 receptor (unknown origin) B 5.39 pIC50 4100 nM IC50 J Med Chem (2022) 65: 4058-4084 [PMID:35179893]
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]
κ receptor/Kappa opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Inhibition of kappa opioid receptor (unknown origin) B 4.52 pIC50 >30000 nM IC50 J Med Chem (2022) 65: 4058-4084 [PMID:35179893]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL Inhibition of mu opioid receptor (unknown origin) B 4.92 pIC50 12000 nM IC50 J Med Chem (2022) 65: 4058-4084 [PMID:35179893]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Inhibition of M2 mAChR receptor (unknown origin) B 5.12 pIC50 7500 nM IC50 J Med Chem (2022) 65: 4058-4084 [PMID:35179893]
nicotinic acetylcholine receptor α7 subunit/Neuronal acetylcholine receptor protein alpha-7 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2492] [GtoPdb: 468] [UniProtKB: P36544]
ChEMBL Inhibition of alpha7 nicotinic acetylcholine receptor (unknown origin) B 4.52 pIC50 >30000 nM IC50 J Med Chem (2022) 65: 4058-4084 [PMID:35179893]

ChEMBL data shown on this page come from version 35:

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]