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!
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 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 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 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 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 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	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	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	Antagonist activity at CXCR4 (unknown origin)	F	7.36	pIC50	44	nM	IC50	Eur J Med Chem (2017) 139: 519-530 [PMID:28826086]
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 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	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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]