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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	=	74000.00	4.13	-	5	Displacement of [125I]-CCL3 from human CCR1 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	=	79432.82	4.10	-	5	Displacement of [125I]-CCL3 from human CCR1 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
AZD4818	82599	None	0	Human	Binding	Ki	=	5.00	8.30	-	1	Binding affinity to CCR1	ChEMBL	461.2	9	4	6	3.39	CC(=O)Nc1ccc(O)cc1OC[C@@](C)(O)CNC1CCN(Cc2ccc(Cl)cc2)CC1	https://dx.doi.org/10.1021/jm300682j
banyu (I)	574	None	5	Human	Binding	IC50	=	1900.00	5.72	-	2	Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells	ChEMBL	480.1	6	2	6	5.06	Nc1ccc2nc(SCC(=O)NC3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)sc2c1	https://dx.doi.org/10.1016/s0960-894x(01)00176-7
BERLEX COMPOUND	118652	None	11	Human	Binding	Ki	=	52.00	7.28	-	4	Inhibition of [125I]-MIP-1 alpha binding to recombinant human C-C chemokine receptor type 1 expressed in HEK293 cells	ChEMBL	444.2	7	1	3	5.91	N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	https://dx.doi.org/10.1021/jm990316l
BERLEX COMPOUND	118652	None	11	Human	Binding	IC50	=	48.00	7.32	-	4	Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.	ChEMBL	444.2	7	1	3	5.91	N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	https://dx.doi.org/10.1021/jm0004244
BERLEX COMPOUND	118652	None	11	Human	Binding	IC50	=	630.00	6.20	-	4	Inhibitory activity against human Chemokine receptor type 1 expressed in chinese hamster ovary cells	ChEMBL	444.2	7	1	3	5.91	N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	https://dx.doi.org/10.1021/jm0201767
BERLEX COMPOUND	118652	None	11	Mouse	Binding	IC50	=	5000.00	5.30	-	4	Inhibitory activity against [125I]-MIP-1 alpha binding to mouse CCR1 receptors.	ChEMBL	444.2	7	1	3	5.91	N#CC(CCCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1	https://dx.doi.org/10.1021/jm0004244
BI 639667	171085	None	20	Human	Binding	IC50	=	2.00	8.70	-	2	Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.1016/j.bmcl.2018.12.024
BI 639667	171085	None	20	Human	Binding	IC50	=	5.40	8.27	-	2	Scintillation Proximity Assay binding	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.6019/CHEMBL4507278
BI 639667	171085	None	20	Human	Binding	IC50	=	24.00	7.62	-	2	Ca flux	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.6019/CHEMBL4507278
BI 639667	171085	None	20	Human	Binding	IC50	=	2.40	8.62	-	2	Chemotaxis	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.6019/CHEMBL4507278
BI 639667	171085	None	20	Human	Binding	IC50	=	2.40	8.62	-	2	Affinity On-target Cellular interaction (Chemotaxis in THP-1 cells) EUB0000352a CCR1	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.6019/CHEMBL5210121
BI 639667	171085	None	20	Human	Binding	IC50	=	9.00	8.05	-	2	Receptor internalization	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.6019/CHEMBL4507278
BI 639667	171085	None	20	Human	Binding	IC50	=	5.40	8.27	-	2	Affinity Biochemical interaction (Scintillation Proximity Assay (SPA)) EUB0000352a CCR1	ChEMBL	451.1	5	1	7	2.78	CS(=O)(=O)c1cc(C2(NC(=O)c3cncc4c3cnn4-c3ccc(F)cc3)CC2)ccn1	https://dx.doi.org/10.6019/CHEMBL5210307
BMS-817399	675	None	16	Human	Binding	IC50	=	1.50	8.82	-	2	Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay	ChEMBL	438.2	6	3	4	3.09	CC(C)[C@@H](NC(=O)CC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1	https://dx.doi.org/10.1016/j.bmcl.2018.11.015
BMS-817399	675	None	16	Human	Binding	Ki	=	3.70	8.43	-	2	Binding Assay: For radioligand competition studies, a final concentration of 1x105 THP-1 monocytic leukemia cells are combined with 100 μg of LS WGA PS beads (Amersham, Cat.#: RPNQ 0260) in 40 μL of assay buffer (RPMI 1640 without phenol red, 50 mM HEPES, 5 mM MgCl2, 1 mM CaCl2, 0.1% BSA). The THP-1 cell/bead mixture was added to each well of a 384-well assay plate (PerkinElmer, Cat. #:6007899) containing test compound in 3-fold serial dilution, with final concentrations ranging from 8 μM to 0.14 nM. A final concentration of 0.1 nM [125I]-MIP-1α (PerkinElmer, Cat. #NEX298) in 20 μL assay buffer was added to the reaction. Unlabeled MIP-1α was added in excess to some wells to determine non-specific binding. Sealed assay plates were incubated at room temperature for 12 h then analyzed by LEADseeker.	ChEMBL	438.2	6	3	4	3.09	CC(C)[C@@H](NC(=O)CC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1	-
BMS-817399	675	None	16	Human	Binding	IC50	=	42.00	7.38	-	2	Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr	ChEMBL	438.2	6	3	4	3.09	CC(C)[C@@H](NC(=O)CC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1	https://dx.doi.org/10.1021/jm5003167
BMS-817399	675	None	16	Human	Binding	IC50	=	25.00	7.60	-	2	Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr	ChEMBL	438.2	6	3	4	3.09	CC(C)[C@@H](NC(=O)CC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1	https://dx.doi.org/10.1021/jm5003167
BMS-817399	675	None	16	Human	Binding	IC50	=	14.30	7.84	-	2	Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins	ChEMBL	438.2	6	3	4	3.09	CC(C)[C@@H](NC(=O)CC(C)(C)O)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1	https://dx.doi.org/10.1021/jm5003167

Showing 1 to 20 of 917 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)