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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL18442 (AMD 3100, AMD3100, JM 3100, Mozobil, Plerixafor, Plerixafor hydrochloride, Plerixafor octahydrochloride, SID 791)
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • ACKR3 in Human [GtoPdb: 80] [UniProtKB: P25106]
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
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 E288A/L290A 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 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 Antagonist activity at CXCR4 receptor in human SUP-T1 cells assessed as reduction in SDF-1alpha-stimulated cell migration and measured by CellTiter-96 assay F 6.2 pIC50 624.9 nM IC50 Eur J Med Chem (2022) 231: 114150-114150 [PMID:35124530]
ChEMBL Inhibition of APC-conjugated anti-human CXCR4 clone 12G5 binding to CXCR4 in human HPBALL cells measured after 3 hrs by FACS analysis B 6.25 pIC50 561 nM IC50 Eur J Med Chem (2020) 205: 112537-112537 [PMID:32768738]
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 Binding affinity to CXCR4 (unknown origin) expressed in CHO cells incubated for 40 mins by competitive binding assay method B 6.49 pIC50 325.3 nM IC50 Eur J Med Chem (2020) 200: 112410-112410 [PMID:32492596]
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 Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured by 12G5 competitive binding method B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2022) 231: 114150-114150 [PMID:35124530]
ChEMBL Displacement of 12G5 mAb from CXCR4 (unknown origin) expressed in CHO cells incubated for 40 mins by spectrophotometric method B 6.49 pIC50 320 nM IC50 Eur J Med Chem (2022) 244: 114797-114797 [PMID:36270088]
ChEMBL Antagonist activity at CXCR4 in human HPBALL cells assessed as inhibition of APC-conjugate clone 12G5 antibody signal incubated for 3 hrs by flow cytometric analysis B 6.52 pIC50 303 nM IC50 Eur J Med Chem (2020) 187: 111914-111914 [PMID:31806538]
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 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 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 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 Displacement of [125I]-CXCL12 from human CXCR4 receptor expressed in HEK293T cell membranes after 2 hrs by scintillation counting analysis B 6.7 pIC50 199.53 nM IC50 Eur J Med Chem (2019) 162: 631-649 [PMID:30476826]
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 Binding affinity to CXCR4 (unknown origin) expressed in CHO cells measured after 40 mins by 12G5 antibody competition assay B 7.19 pIC50 65 nM IC50 Bioorg Med Chem (2016) 24: 5393-5399 [PMID:27658790]
ChEMBL Competitive binding affinity to CXCR4 receptor (unknown origin) expressed in CHO cells incubated for 40 mins by 12G5 antibody based fluorescence analysis B 7.29 pIC50 51 nM IC50 Eur J Med Chem (2019) 172: 174-185 [PMID:30978562]
ChEMBL Competitive binding affinity to CXCR4 in human SupT1 cells incubated for 40 mins by 12G5 antibody based fluorescence analysis B 7.36 pIC50 44 nM IC50 Eur J Med Chem (2019) 172: 174-185 [PMID:30978562]
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 Antagonist activity at CXCR4 in human CD4-positive T cells assessed as inhibition of CXCL12-induced cytosolic calcium flux preincubated for 20 mins followed by CXCL12 addition by calcium 4 dye based FLIPR TETRA analysis F 8.21 pIC50 6.13 nM IC50 Eur J Med Chem (2020) 205: 112537-112537 [PMID:32768738]
ChEMBL Antagonist activity at CXCR4 in human CD4-positive T cells assessed as inhibition of CXCL12-induced calcium signal incubated for 20 mins by FLIPR assay F 8.21 pIC50 6.13 nM IC50 Eur J Med Chem (2020) 187: 111914-111914 [PMID:31806538]
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 Antagonist activity at CXCR4 receptor in SDF-1alpha-stimulated human SUP-T1 cells measured by calcium mobilization assay F 8.51 pIC50 3.1 nM IC50 Eur J Med Chem (2022) 231: 114150-114150 [PMID:35124530]
ChEMBL Antagonist activity at CXCR4 receptor in SDF-1alpha-stimulated human SUP-T1 cells incubated for 30 mins by calcium mobilization assay B 8.54 pIC50 2.9 nM IC50 Eur J Med Chem (2020) 200: 112410-112410 [PMID:32492596]
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]
ChEMBL Inhibition of CXCR4 (unknown origin) B 9.09 pIC50 0.81 nM IC50 J Med Chem (2017) 60: 4735-4779 [PMID:28165741]
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)
Stromal cell-derived factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3286074] [UniProtKB: P48061]
ChEMBL Inhibition of SDF-1 alpha induced cell migration in human SUP-T1 cells pre-incubated for 30 mins followed by SDF-1 alpha addition measured after 3 hrs by cell Titer-96 reagent based analysis B 6.22 pIC50 608.2 nM IC50 Eur J Med Chem (2020) 200: 112410-112410 [PMID:32492596]
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 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]