ChEMBL ligand: CHEMBL4782111
ACKR3 in Human [GtoPdb: 80] [UniProtKB: P25106] Atypical chemokine receptor 3 in Dog [ChEMBL: CHEMBL4739676] [UniProtKB: P11613] ACKR3/Atypical chemokine receptor 3 in Mouse [ChEMBL: CHEMBL4105796] [GtoPdb: 80] [UniProtKB: P56485] ACKR3/Atypical chemokine receptor 3 in Rat [ChEMBL: CHEMBL4739671] [GtoPdb: 80] [UniProtKB: O89039] 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] There should be some charts here, you may need to enable JavaScript!
ACKR3/C-X-C chemokine receptor type 7 in Human [ChEMBL: CHEMBL2010631] [GtoPdb: 80] [UniProtKB: P25106] There should be some charts here, you may need to enable JavaScript!
Kv11.1/HERG in Human [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] 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
ACKR3 in Human [GtoPdb: 80] [UniProtKB: P25106]
GtoPdb	Measuring antagonism of CXCL12-induced β-arrestin recruitment	-	8.49	pIC50	3.2	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
Atypical chemokine receptor 3 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739676] [UniProtKB: P11613]
ChEMBL	Antagonist activity at dog CXCR7 expressed in CHO-K1 cells co-expressing beta-arrestin assessed as reduction in CXCL12-alpha induced response incubated for 24 hrs	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ACKR3/Atypical chemokine receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105796] [GtoPdb: 80] [UniProtKB: P56485]
ChEMBL	Antagonist activity at mouse CXCR7 expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12-alpha induced response incubated for 24 hrs	B	8.64	pIC50	2.3	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ACKR3/Atypical chemokine receptor 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4739671] [GtoPdb: 80] [UniProtKB: O89039]
ChEMBL	Antagonist activity at rat CXCR7 expressed in HEK293 cells co-expressing beta-arrestin assessed as reduction in CXCL12-alpha induced response incubated for 24 hrs	B	8.51	pIC50	3.1	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
CXCR4/C-X-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
ChEMBL	Antagonist activity CXCR4 in human MOLT-4 cells co-expressing beta-arrestin assessed as reduction in CXCL12-alpha induced response pre-incubated for 20 mins before CXCL12 addition by FLIPR assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ACKR3/C-X-C chemokine receptor type 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2010631] [GtoPdb: 80] [UniProtKB: P25106]
ChEMBL	Binding affinity to SNAP-tag fused human CXCR7 expressed in HEK293 cells by HTRF assay	B	9.28	pKi	0.53	nM	Ki	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
GtoPdb	Measuring antagonism of CXCL12-induced β-arrestin recruitment	-	8.49	pIC50	3.2	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12-alpha induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 24 hrs	B	8.49	pIC50	3.2	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Antagonist activity at CXCR7 in human Tango CXCR7-bla U2OS cells co-expressing TEV-fused-beta-arrestin using CCF4-AM as substrate incubated for 2 hrs and measured by FRET assay	F	8.52	pIC50	3	nM	IC50	US-20210115033-A1. Crystalline forms of the cxcr7 receptor antagonist (3s,4s)-1-cyclopropylmethyl-4-{[5-(2,4-difluoro-phenyl)-isoxazole-3-carbonyl]-amino}-piperidine-3-carboxylic acid (1-pyrimidin-2-yl-cyclopropyl)-amide (2021)
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL11 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 1 uM CXCL11 level	B	8.55	pIC50	2.83	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL11 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 333 nM CXCL11 level	B	8.55	pIC50	2.79	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL11 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 111 nM CXCL11 level	B	8.63	pIC50	2.32	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL11 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 37 nM CXCL11 level	B	8.69	pIC50	2.03	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL11 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 4.11 nM CXCL11 level	B	8.74	pIC50	1.84	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL11 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 12.3 nM CXCL11 level	B	8.78	pIC50	1.65	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 1.97 nM CXCL12 level	B	8.94	pIC50	1.15	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 4.11 nM CXCL12 level	B	9	pIC50	0.99	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 12.3 nM CXCL12 level	B	9.01	pIC50	0.98	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 111 nM CXCL12 level	B	9.02	pIC50	0.96	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 333 nM CXCL12 level	B	9.04	pIC50	0.9	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 1 uM CXCL12 level	B	9.05	pIC50	0.9	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
ChEMBL	Insurmountable antagonist activity at CXCR7 (unknown origin) expressed in human U2OS cells co-expressing beta-arrestin assessed as reduction in CXCL12 induced response pre-incubated for 15 mins before CXCL12-alpha addition and measured after 25.5 hrs in presence of 37 nM CXCL12 level	B	9.06	pIC50	0.86	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL	Inhibition of human ERG expressed in CHO cells at -40 mV holding potential by Q-patch clamp assay	B	5.24	pIC50	5700	nM	IC50	J Med Chem (2020) 63: 15864-15882 [PMID:33314938]

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]