plerixafor [Ligand Id: 844] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL18442 (Plerixafor, AMD-3100, Mozobil)
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • CXCR4/C-X-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
  • CXCR4/C-X-C chemokine receptor type 4 in Rat [ChEMBL: CHEMBL5556] [GtoPdb: 71] [UniProtKB: O08565]
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  • ACKR3 in Human [GtoPdb: 80] [UniProtKB: P25106]
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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 Displacement of [125I]MCP1 from CCR2/CXCR4 expressed in CHOK1 cells B 10.05 pIC50 0.09 nM IC50 J. Biol. Chem. (2007) 282: 30062-30069 [PMID:17715128]
ChEMBL Displacement of [125I]SDF1alpha from CCR2/CXCR4 expressed in CHOK1 cells B 10.4 pIC50 0.04 nM IC50 J. Biol. Chem. (2007) 282: 30062-30069 [PMID:17715128]
CXCR4/C-X-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 E288A mutant expressed in COS7 cells B 4.2 pKi -4.2 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 E288A mutant expressed in COS7 cells B 4.2 pKi 63000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 D262N mutant expressed in COS7 cells B 4.34 pKi 46000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 D262N mutant expressed in COS7 cells B 4.34 pKi -4.34 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 A175F mutant expressed in COS7 cells B 4.44 pKi 36000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 A175F mutant expressed in COS7 cells B 4.45 pKi -4.45 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D187A mutant expressed in COS7 cells B 4.85 pKi -4.85 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D187A mutant expressed in COS7 cells B 4.85 pKi 14000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 D171N mutant expressed in COS7 cells B 4.87 pKi -4.87 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 D171N mutant expressed in COS7 cells B 4.89 pKi 13000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y255A mutant expressed in COS7 cells B 5.01 pKi -5.01 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y255A mutant expressed in COS7 cells B 5.01 pKi 9700 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 A175F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.07 pKi 8500 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 E288A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.19 pKi 6400 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 S263A mutant expressed in COS7 cells B 5.27 pKi 5400 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 S263A mutant expressed in COS7 cells B 5.27 pKi -5.27 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F172A mutant expressed in COS7 cells B 5.33 pKi 4700 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 D262N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.33 pKi 4700 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 V196A mutant expressed in COS7 cells B 5.33 pKi -5.33 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F172A mutant expressed in COS7 cells B 5.33 pKi -5.33 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 V196A mutant expressed in COS7 cells B 5.34 pKi 4600 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259W mutant expressed in COS7 cells B 5.34 pKi 4600 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259W mutant expressed in COS7 cells B 5.34 pKi -5.34 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 N176A mutant expressed in COS7 cells B 5.38 pKi -5.38 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 N176A mutant expressed in COS7 cells B 5.39 pKi 4100 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y256A mutant expressed in COS7 cells B 5.4 pKi 4000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 Y256A mutant expressed in COS7 cells B 5.4 pKi -5.4 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F174A mutant expressed in COS7 cells B 5.49 pKi 3200 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D182A mutant expressed in COS7 cells B 5.49 pKi 3200 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 T287A mutant expressed in COS7 cells B 5.5 pKi -5.5 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 4 of human CXCR4 F174A mutant expressed in COS7 cells B 5.5 pKi -5.5 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from extracellular loop 2 of human CXCR4 D182A mutant expressed in COS7 cells B 5.5 pKi -5.5 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 T287A mutant expressed in COS7 cells B 5.51 pKi 3100 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207W mutant expressed in COS7 cells B 5.52 pKi -5.52 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207W mutant expressed in COS7 cells B 5.52 pKi 3000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200W mutant expressed in COS7 cells B 5.56 pKi -5.56 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200W mutant expressed in COS7 cells B 5.57 pKi 2700 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207F mutant expressed in COS7 cells B 5.57 pKi 2700 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 G207F mutant expressed in COS7 cells B 5.57 pKi -5.57 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 3 of human CXCR4 H113A mutant expressed in COS7 cells B 5.7 pKi 2000 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 3 of human CXCR4 H113A mutant expressed in COS7 cells B 5.71 pKi -5.71 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 H203A mutant expressed in COS7 cells B 5.74 pKi -5.74 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 D171N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.74 pKi 1800 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 H203A mutant expressed in COS7 cells B 5.74 pKi 1800 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells B 5.81 pKi -5.81 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells B 5.82 pKi 1500 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 I284A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.92 pKi 1200 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 I284A mutant expressed in COS7 cells B 5.96 pKi 1100 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 I284A mutant expressed in COS7 cells B 5.96 pKi -5.96 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 Q200A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.03 pKi 930 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from human wild type CXCR4 expressed in COS7 cells B 6.05 pKi -6.05 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from human wild type CXCR4 expressed in COS7 cells B 6.05 pKi 890 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 H113A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.13 pKi 740 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 Y255A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.18 pKi 660 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 I259W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.2 pKi 630 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200A mutant expressed in COS7 cells B 6.25 pKi -6.25 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 5 of human CXCR4 Q200A mutant expressed in COS7 cells B 6.25 pKi 560 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 Q200W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.4 pKi 400 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 L120F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.48 pKi 330 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.54 pKi 290 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 H203A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.54 pKi 290 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 T287A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.54 pKi 290 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human wild type CXCR4 expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.66 pKi 220 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
GtoPdb - - 6.7 pKi 199 nM Ki Eur J Med Chem (2019) 162: 631-649 [PMID:30476826]
ChEMBL Antagonist activity at human CXCR4 H281A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.72 pKi 190 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 F172A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.77 pKi 170 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 H281A mutant expressed in COS7 cells B 6.8 pKi 160 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]12G5 antibody from transmembrane domain 7 of human CXCR4 H281A mutant expressed in COS7 cells B 6.8 pKi -6.8 - logKi J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 V196A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.85 pKi 140 nM Ki J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
GtoPdb - - 7 pKi 100 nM Ki J Biol Chem (2002) 277: 24515-24521 [PMID:11923301]
ChEMBL Displacement of [125I]SDF1alpha from CXCR4 in human HL60 cells B 4.82 pIC50 15200 nM IC50 Bioorg. Med. Chem. (2009) 17: 1486-1493 [PMID:19188071]
ChEMBL Antagonist activity at human CXCR4 A175F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.07 pIC50 -5.07 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 E288A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.19 pIC50 -5.19 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of anti-CXCR4 PE antibody clone 12G5 binding to CXCR4 in human CCRF-CEM cells preincubated for 30 mins followed by anti-CXCR4 PE antibody clone 12G5 addition measured after 30 mins by flow cytometric method B 5.21 pIC50 6200 nM IC50 J Med Chem (2017) 60: 9641-9652 [PMID:29125295]
ChEMBL Antagonist activity at human CXCR4 D262N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.33 pIC50 -5.33 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 D171N mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.75 pIC50 -5.75 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 I284A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 5.94 pIC50 -5.94 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 D262A mutant expressed in HEK293 cells B 6 pIC50 >1000 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 D171A mutant expressed in HEK293 cells B 6 pIC50 >1000 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 E288A/L290A mutant expressed in HEK293 cells B 6 pIC50 >1000 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at human CXCR4 Q200A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.03 pIC50 -6.03 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 H113A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.13 pIC50 -6.13 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 Y255A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.18 pIC50 -6.18 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
GtoPdb Antagonism of SDF-1/CXCL12 ligand binding to CXCR4 expressed by CCRF–CEM T-cells. - 6.19 pIC50 651 nM IC50 Biochem. Pharmacol. (2006) 72: 588-96 [PMID:16815309]
ChEMBL Antagonist activity at human CXCR4 I259W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.2 pIC50 -6.2 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 E277A mutant expressed in HEK293 cells B 6.33 pIC50 469.5 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at human CXCR4 Q200W mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.4 pIC50 -6.4 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 L120F mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.49 pIC50 -6.49 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells B 6.52 pIC50 300.2 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 H113A mutant expressed in HEK293 cells B 6.53 pIC50 296.4 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Displacement of 12G5-CXCL12 from CXCR4 in human HPBALL cells after 3 hrs by FACS analysis B 6.54 pIC50 290 nM IC50 Eur J Med Chem (2018) 149: 30-44 [PMID:29494843]
ChEMBL Inhibition of Mab 12G5 binding to wild type CXCR4 expressed in HEK293 cells B 6.54 pIC50 289.1 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at transmembrane domain 6 of human CXCR4 I259A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.54 pIC50 -6.54 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 H203A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.54 pIC50 -6.54 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Antagonist activity at human CXCR4 T287A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.54 pIC50 -6.54 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 I284A mutant expressed in HEK293 cells B 6.58 pIC50 265.8 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 H203A mutant expressed in HEK293 cells B 6.59 pIC50 259 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 V99A mutant expressed in HEK293 cells B 6.59 pIC50 258.5 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Displacement of [125I]CXCL12 from CXCR4 in human CEM cells B 6.61 pIC50 245 nM IC50 J. Med. Chem. (2008) 51: 7915-7920 [PMID:19053768]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 E275A mutant expressed in HEK293 cells B 6.63 pIC50 235.6 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at human wild type CXCR4 expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.66 pIC50 -6.66 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Displacement of [125I]CXCL12 from human CXCR4 expressed in HEK293 cell membranes after 1.5 hrs by Topcount method B 6.67 pIC50 213.1 nM IC50 J Med Chem (2018) 61: 818-833 [PMID:29314840]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 V112A mutant expressed in HEK293 cells B 6.71 pIC50 196.6 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at human CXCR4 H281A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.73 pIC50 -6.73 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 V280A mutant expressed in HEK293 cells B 6.76 pIC50 175.3 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at human CXCR4 F172A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.77 pIC50 -6.77 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 D181A mutant expressed in HEK293 cells B 6.84 pIC50 143.7 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at human CXCR4 V196A mutant expressed in COS7 cells coexpressing G protein Gqi4myr assessed as inhibition of CXCL12-induced phosphatidylinositol turnover F 6.86 pIC50 -6.86 - logIC50 J. Biol. Chem. (2007) 282: 27354-27365 [PMID:17599916]
ChEMBL Binding affinity to CXCR4 B 7.13 pIC50 74 nM IC50 J. Med. Chem. (2012) 55: 9363-9392 [PMID:22931505]
ChEMBL Inhibition of Mab 12G5 binding to CXCR4 H281A mutant expressed in HEK293 cells B 7.14 pIC50 72.7 nM IC50 Antimicrob. Agents Chemother. (2009) 53: 2940-2948 [PMID:19451305]
ChEMBL Antagonist activity at CXCR4 (unknown origin) F 7.36 pIC50 44 nM IC50 Eur J Med Chem (2017) 139: 519-530 [PMID:28826086]
ChEMBL Antagonist activity at CXCR4 in human Jurkat cells assessed as inhibition of SDF1-induced cell migration F 7.56 pIC50 27.4 nM IC50 Bioorg. Med. Chem. (2009) 17: 1486-1493 [PMID:19188071]
ChEMBL Antagonist activity at CXCR4 in human CD4+ T cells assessed as inhibition of CXCL12-mediated cytosolic calcium level preincubated with compounds followed by CXCL12 stimulation by calcium 4 dye-based FLIPR assay F 7.74 pIC50 18 nM IC50 Eur J Med Chem (2018) 149: 30-44 [PMID:29494843]
ChEMBL Inhibition of PE-conjugated-12G5 anti-CXCR4 antibody binding to CXCR4 in human CEM-CCRF cells preincubated for 30 mins followed by antibody addition by FACS Canto II cytofluorometric analysis B 8.22 pIC50 6 nM IC50 J Med Chem (2016) 59: 8369-8380 [PMID:27571038]
ChEMBL Displacement of [125I]SDF1alpha from CXCR4 expressed in CHOK1 cells B 9.09 pIC50 0.81 nM IC50 J. Biol. Chem. (2007) 282: 30062-30069 [PMID:17715128]
CXCR4/C-X-C chemokine receptor type 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5556] [GtoPdb: 71] [UniProtKB: O08565]
ChEMBL Displacement of [125I]CXCL12 from CXCR4 in rat IR983F cells B 6.97 pIC50 108 nM IC50 J. Med. Chem. (2008) 51: 7915-7920 [PMID:19053768]
ChEMBL Competitive Binding Assay: A synthetic 14-mer peptide, TN14003, was previously reported to block both SDF-1/CXCR4 mediated invasion in vitro and metastasis in vivo with a high specificity by binding competitively with its ligand SDF-1. Aa competitive binding assay using biotin-labeled TN14003 and streptavidin-conjugated rhodamine was developed to determine the binding efficiency of new chemical entities to the SDF-1 binding domain of CXCR4. Cells incubated with high affinity compounds show only blue nuclear staining, whereas compounds with low affinity result in staining CXCR4 (red; rhodamine) as well as the nuclei (blue; cytox blue). B 7 pIC50 100 nM IC50 US-9205085-B2. Tricyclic amino containing compounds for treatment or prevention of symptoms associated with endocrine dysfunction (2015)
ACKR3 in Human [GtoPdb: 80] [UniProtKB: P25106]
GtoPdb - - 6.85 pEC50 - - - J. Biol. Chem. (2010) 285: 37939-43 [PMID:20956518];
Mol. Pharmacol. (2009) 75: 1240-7 [PMID:19255243]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]