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Ligand source activities (1 row/activity)

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	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

Ligands				Receptor	Activity									Chemical information
Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

1,10-Phenanthroline	6	None	76	Human	Binding	IC50	=	53000.00	4.28	-	5	Displacement of [125I]-CCL3 from human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs	ChEMBL	180.1	0	0	2	2.78	c1cnc2c(c1)ccc1cccnc12	https://dx.doi.org/10.1021/jm301121j
1,10-Phenanthroline	6	None	76	Human	Binding	IC50	=	50118.72	4.30	-	5	Displacement of [125I]-CCL3 from human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr after 3 hrs	ChEMBL	180.1	0	0	2	2.78	c1cnc2c(c1)ccc1cccnc12	https://dx.doi.org/10.1021/jm301121j
ancriviroc	415	None	10	Human	Binding	pKi	=	-	8.25	-1	2	Unclassified	Guide to Pharmacology	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://pubmed.ncbi.nlm.nih.gov/16476734
ancriviroc	415	None	10	Human	Binding	pKi	=	-	8.25	-1	2	Unclassified	Guide to Pharmacology	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://pubmed.ncbi.nlm.nih.gov/16304152
ancriviroc	415	None	10	Human	Binding	pKi	=	-	8.25	-1	2	Unclassified	Guide to Pharmacology	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://pubmed.ncbi.nlm.nih.gov/11585437
ancriviroc	415	None	10	Human	Binding	pKd	None	-	8.90	-1	2	Unclassified	Guide to Pharmacology	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://pubmed.ncbi.nlm.nih.gov/16304152
ancriviroc	415	None	10	Human	Binding	Ki	=	2.00	8.70	-1	2	Binding affinity to CCR5	ChEMBL	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://dx.doi.org/10.1021/jm300682j
ancriviroc	415	None	10	Human	Binding	Ki	=	2.10	8.68	-1	2	Inhibition of RANTES binding to the human C-C chemokine receptor type 5 (CCR5)	ChEMBL	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://dx.doi.org/10.1021/jm030265z
ancriviroc	415	None	10	Human	Binding	Ki	=	2.10	8.68	-1	2	Inhibition of RANTES binding to C-C chemokine receptor type 5	ChEMBL	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://dx.doi.org/10.1021/jm015526o
ancriviroc	415	None	10	Mouse	Binding	Ki	=	2.10	8.68	1	2	Inhibition of RANTES binding to Chemokine receptor type 5 receptor from NIH 3T3 cells	ChEMBL	556.2	6	0	5	4.85	CCO/N=C(\c1ccc(Br)cc1)C1CCN(C2(C)CCN(C(=O)c3c(C)cc[n+]([O-])c3C)CC2)CC1	https://dx.doi.org/10.1021/jm0200815
aplaviroc	443	None	22	Human	Binding	pKi	=	-	8.50	-	4	Unclassified	Guide to Pharmacology	577.3	10	3	6	4.58	CCCCN1C(=O)[C@@H]([C@H](O)C2CCCCC2)NC(=O)C12CCN(Cc1ccc(Oc3ccc(C(=O)O)cc3)cc1)CC2	https://pubmed.ncbi.nlm.nih.gov/16476734
aplaviroc	443	None	22	Human	Binding	Kd	=	3.00	8.52	-	4	Binding affinity to CCR5	ChEMBL	577.3	10	3	6	4.58	CCCCN1C(=O)[C@@H]([C@H](O)C2CCCCC2)NC(=O)C12CCN(Cc1ccc(Oc3ccc(C(=O)O)cc3)cc1)CC2	https://dx.doi.org/10.1021/jm300682j
aplaviroc	443	None	22	Human	Binding	IC50	=	5.80	8.24	-	4	Displacement of MIP-1alpha from human CCR5 expressed in CHO cells	ChEMBL	577.3	10	3	6	4.58	CCCCN1C(=O)[C@@H]([C@H](O)C2CCCCC2)NC(=O)C12CCN(Cc1ccc(Oc3ccc(C(=O)O)cc3)cc1)CC2	https://dx.doi.org/10.1016/j.bmc.2011.05.022
aplaviroc	443	None	22	Mouse	Binding	IC50	=	0.40	9.40	-	4	Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr	ChEMBL	577.3	10	3	6	4.58	CCCCN1C(=O)[C@@H]([C@H](O)C2CCCCC2)NC(=O)C12CCN(Cc1ccc(Oc3ccc(C(=O)O)cc3)cc1)CC2	https://dx.doi.org/10.1016/j.ejmech.2018.01.085
AZD-5363	82603	None	0	Human	Binding	IC50	=	0.17	9.77	-	1	Binding affinity to CCR5	ChEMBL	638.3	11	0	6	5.00	CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cc(F)cc(F)c2)C2CCC(S(C)(=O)=O)CC2)CC1	https://dx.doi.org/10.1021/jm300682j
AZD5672	550	None	1	Human	Binding	pIC50	=	-	9.59	-	1	Displacement of [125I]MIP-1α from human recombinant CCR5 expressed in CHO cells	Guide to Pharmacology	639.3	11	0	6	4.07	CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cc(F)cc(F)c2)C2CCN(S(C)(=O)=O)CC2)CC1	https://pubmed.ncbi.nlm.nih.gov/22266038
AZD5672	550	None	1	Human	Binding	IC50	=	0.26	9.59	-	1	Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells	ChEMBL	639.3	11	0	6	4.07	CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cc(F)cc(F)c2)C2CCN(S(C)(=O)=O)CC2)CC1	https://dx.doi.org/10.1016/j.bmcl.2011.12.117
BMS-681	672	None	2	Human	Binding	IC50	=	2.40	8.62	-	5	Antagonist activity at CCR5 (unknown origin) expressed in human HT1080 cells assessed as blockade of MIP1beta-binding to receptor	ChEMBL	491.3	7	1	5	5.34	CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O	https://dx.doi.org/10.1021/acsmedchemlett.8b00439
BMS-681	672	None	2	Human	Binding	IC50	=	4.30	8.37	-	5	Antagonist activity against CCR5 in whole blood (unknown origin) assessed as reduction in CD11b upregulation	ChEMBL	491.3	7	1	5	5.34	CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O	https://dx.doi.org/10.1021/ml500505q
BMS-681	672	None	2	Human	Binding	IC50	=	2.40	8.62	-	5	Inhibition of [125I]MCP1-beta binding to CCR5 in human HT1080 cell membranes incubated for 4 to 6 hrs	ChEMBL	491.3	7	1	5	5.34	CCC[C@@H]1C[C@H](N(C)C(C)C)CC[C@@H]1N1CC[C@H](Nc2ncnc3ccc(C(F)(F)F)cc23)C1=O	https://dx.doi.org/10.1021/ml500505q

Showing 1 to 20 of 2,322 entries

	Ligands				Receptor	Activity									Chemical information
	Common name	GPCRdb ID	Reference ligand	Vendors	Species	Assay Type	Activity Type	Activity Relation	Activity Value	p-value (-log)	Fold selectivity	Tested GPCRs	Assay Description	Source	Mol weight	Rot Bonds	H don	H acc	LogP	Smiles	DOI

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Ligand source activities (1 row/activity)