Get vendors


Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors UniProt IUPHAR Species p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10752 2157 0 CCR5 CCR5 Human - = Unclassified
Antagonism of CCR5-mediated HIV entry <i>in vitro</i>.Antagonism of CCR5-mediated HIV entry <i>in vitro</i>.
Guide to Pharmacology None None None None None
1272 785 0 CCR5 CCR5 Human - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
3651 2462 0 CCR5 CCR5 Rat - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 574 11 1 5 6.4 CCn1nc(cc1C1CCN(CC1)C[C@H]1C[C@@H](C[C@@H]1c1cccc(c1)F)N([C@@H](C(=O)O)C(C)C)C)Cc1ccccc1 12604693
5481119 2462 0 CCR5 CCR5 Rat - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 574 11 1 5 6.4 CCn1nc(cc1C1CCN(CC1)C[C@H]1C[C@@H](C[C@@H]1c1cccc(c1)F)N([C@@H](C(=O)O)C(C)C)C)Cc1ccccc1 12604693
CHEMBL3182547 2462 0 CCR5 CCR5 Rat - = Unclassified
UnclassifiedUnclassified
Guide to Pharmacology 574 11 1 5 6.4 CCn1nc(cc1C1CCN(CC1)C[C@H]1C[C@@H](C[C@@H]1c1cccc(c1)F)N([C@@H](C(=O)O)C(C)C)C)Cc1ccccc1 12604693
3910 3078 0 CCR5 CCR5 Human - None Unclassified
UnclassifiedUnclassified
Guide to Pharmacology None None None None None
CHEMBL2372983 203846 0 CCR5 CCR5 Human 9.7 pEC50 = 9.7 Binding
Effective concentration for antagonistic activity by inhibition of T-tropic strain of HIV-1 through its specific binding to a chemokine receptorEffective concentration for antagonistic activity by inhibition of T-tropic strain of HIV-1 through its specific binding to a chemokine receptor
ChEMBL None None None NCCCC[C@@H]1NC(=O)[C@@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](N)CCCN=C(N)N)c2ccc3ccccc3c2)CSSC[C@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H]2CCCN2C1=O 10.1016/s0960-894x(00)00664-8
483407 165214 16 CCR5 CCR5 Human 9.0 pEC50 = 9 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1C1CC2CCC(C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1039/C6MD00311G
CHEMBL425618 165214 16 CCR5 CCR5 Human 9.0 pEC50 = 9 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1C1CC2CCC(C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1039/C6MD00311G
74265 201875 96 CCR5 CCR5 Human 6.0 pEC50 = 6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 0 0 2 4.0 Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C 10.1021/jm301121j
CHEMBL99384 201875 96 CCR5 CCR5 Human 6.0 pEC50 = 6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 0 0 2 4.0 Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C 10.1021/jm301121j
14434082 83133 6 CCR5 CCR5 Human 5.0 pEC50 = 5 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccnc2c1ccc1c(C=O)ccnc12 10.1021/jm301121j
CHEMBL2205801 83133 6 CCR5 CCR5 Human 5.0 pEC50 = 5 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 236 2 0 4 2.4 O=Cc1ccnc2c1ccc1c(C=O)ccnc12 10.1021/jm301121j
16726107 82840 3 CCR5 CCR5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 475 7 1 6 4.4 Cc1ccc(CN2CCC(CNC(=O)C3CCN(c4ccc(-c5cccs5)nn4)CC3)C2)cc1 10.1021/jm061389p
CHEMBL220199 82840 3 CCR5 CCR5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 475 7 1 6 4.4 Cc1ccc(CN2CCC(CNC(=O)C3CCN(c4ccc(-c5cccs5)nn4)CC3)C2)cc1 10.1021/jm061389p
14338 4120 106 CCR5 CCR5 Human 5.0 pEC50 = 5.0 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
CHEMBL101165 4120 106 CCR5 CCR5 Human 5.0 pEC50 = 5.0 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
129908110 155146 0 CCR5 CCR5 Human 5.0 pEC50 = 5.0 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 485 9 1 6 5.3 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)c3ccc(C)cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4061273 155146 0 CCR5 CCR5 Human 5.0 pEC50 = 5.0 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 485 9 1 6 5.3 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)c3ccc(C)cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
14338 4120 106 CCR5 CCR5 Human 4.9 pEC50 = 4.9 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
CHEMBL101165 4120 106 CCR5 CCR5 Human 4.9 pEC50 = 4.9 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccnc(-c2cc(C)ccn2)c1 10.1021/jm301121j
16301115 82786 5 CCR5 CCR5 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 435 7 1 6 3.8 Cc1ccc(-n2c(C)nnc2SCC(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm061389p
CHEMBL219769 82786 5 CCR5 CCR5 Human 4.9 pEC50 = 4.9 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 435 7 1 6 3.8 Cc1ccc(-n2c(C)nnc2SCC(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1021/jm061389p
129908195 157965 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 493 11 1 7 4.9 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)Cc3cccs3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4094196 157965 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 493 11 1 7 4.9 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)Cc3cccs3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
129908301 155886 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 516 10 1 8 4.9 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)c3ccc([N+](=O)[O-])cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
132519568 155886 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 516 10 1 8 4.9 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)c3ccc([N+](=O)[O-])cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4069939 155886 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 516 10 1 8 4.9 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)c3ccc([N+](=O)[O-])cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
129908428 158129 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 417 8 3 5 4.6 COc1ccc(C(=O)Nc2ccc(CCC(=O)/C=C/c3ccc(O)c(O)c3)cc2)cc1 10.1039/C6MD00311G
CHEMBL4095938 158129 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 417 8 3 5 4.6 COc1ccc(C(=O)Nc2ccc(CCC(=O)/C=C/c3ccc(O)c(O)c3)cc2)cc1 10.1039/C6MD00311G
129908452 155223 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 518 11 1 8 4.8 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)c3ccc([N+](=O)[O-])cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4062349 155223 0 CCR5 CCR5 Human 4.8 pEC50 = 4.8 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 518 11 1 8 4.8 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)c3ccc([N+](=O)[O-])cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
93149 106479 66 CCR5 CCR5 Human 5.8 pEC50 = 5.8 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
CHEMBL316589 106479 66 CCR5 CCR5 Human 5.8 pEC50 = 5.8 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
129908456 157056 0 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 395 8 3 4 4.8 O=C(CCc1ccc(NC(=O)C2CCCCC2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
CHEMBL4083941 157056 0 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 395 8 3 4 4.8 O=C(CCc1ccc(NC(=O)C2CCCCC2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
129908453 157068 0 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 479 10 1 6 5.2 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)C3CCCCC3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4084066 157068 0 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 479 10 1 6 5.2 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)C3CCCCC3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
129908111 156853 0 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 501 10 1 7 5.0 COc1ccc(C(=O)Nc2ccc(CCC(=O)/C=C/c3ccc(OC(C)=O)c(OC(C)=O)c3)cc2)cc1 10.1039/C6MD00311G
CHEMBL4081563 156853 0 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 501 10 1 7 5.0 COc1ccc(C(=O)Nc2ccc(CCC(=O)/C=C/c3ccc(OC(C)=O)c(OC(C)=O)c3)cc2)cc1 10.1039/C6MD00311G
3258407 84241 17 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 389 9 1 5 4.9 C=C(C)Cc1c(C)c(C#N)c2nc3ccccc3n2c1NCCCN(CC)CC 10.1021/jm061389p
CHEMBL223686 84241 17 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 389 9 1 5 4.9 C=C(C)Cc1c(C)c(C#N)c2nc3ccccc3n2c1NCCCN(CC)CC 10.1021/jm061389p
12987698 83140 2 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
CHEMBL2205809 83140 2 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
1474 153597 124 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
CHEMBL39879 153597 124 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
12987698 83140 2 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
CHEMBL2205809 83140 2 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1cnc2c(ccc3cc(C)cnc32)c1 10.1021/jm301121j
15783796 83142 1 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
CHEMBL2205810 83142 1 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
93149 106479 66 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
CHEMBL316589 106479 66 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1ccnc2c1ccc1cccnc12 10.1021/jm301121j
2733927 83139 80 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
CHEMBL2205808 83139 80 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
1474 153597 124 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
CHEMBL39879 153597 124 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 156 1 0 2 2.1 c1ccc(-c2ccccn2)nc1 10.1021/jm301121j
16728788 82787 0 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 450 7 1 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1NC(=O)CSc1nnc(C)n1-c1ccccc1 10.1021/jm061389p
CHEMBL219770 82787 0 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 450 7 1 7 3.4 Cc1cc(CN2CCN(C)CC2)ccc1NC(=O)CSc1nnc(C)n1-c1ccccc1 10.1021/jm061389p
15783796 83142 1 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
CHEMBL2205810 83142 1 CCR5 CCR5 Human 5.7 pEC50 = 5.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 194 0 0 2 3.1 Cc1cnc2c(ccc3cccnc32)c1 10.1021/jm301121j
2733927 83139 80 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
CHEMBL2205808 83139 80 CCR5 CCR5 Human 4.7 pEC50 = 4.7 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 216 3 0 4 2.2 COc1ccnc(-c2cc(OC)ccn2)c1 10.1021/jm301121j
129908196 156216 0 CCR5 CCR5 Human 4.6 pEC50 = 4.6 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 389 8 3 4 4.5 O=C(CCc1ccc(NC(=O)c2ccccc2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
CHEMBL4073567 156216 0 CCR5 CCR5 Human 4.6 pEC50 = 4.6 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 389 8 3 4 4.5 O=C(CCc1ccc(NC(=O)c2ccccc2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
15664 83138 85 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
CHEMBL2205807 83138 85 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
129908454 157264 0 CCR5 CCR5 Human 4.6 pEC50 = 4.6 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 487 10 1 6 5.2 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)c3ccc(C)cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4086440 157264 0 CCR5 CCR5 Human 4.6 pEC50 = 4.6 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 487 10 1 6 5.2 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)c3ccc(C)cc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
137660245 158461 0 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assayPositive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay
ChEMBL 461 7 1 4 4.4 CC(C)CN1CC(C(=O)Nc2ccc(CN(C)C3CCOCC3)cc2)=Cc2ccccc2C1=O 10.1016/j.ejmech.2017.04.046
CHEMBL4099473 158461 0 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assayPositive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay
ChEMBL 461 7 1 4 4.4 CC(C)CN1CC(C(=O)Nc2ccc(CN(C)C3CCOCC3)cc2)=Cc2ccccc2C1=O 10.1016/j.ejmech.2017.04.046
15664 83138 85 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
CHEMBL2205807 83138 85 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 184 1 0 2 2.8 Cc1ccc(-c2ccc(C)cn2)nc1 10.1021/jm301121j
72792 193310 71 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 193310 71 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
72792 193310 71 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
CHEMBL593442 193310 71 CCR5 CCR5 Human 5.6 pEC50 = 5.6 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccnc2c1ccc1c(C)ccnc12 10.1021/jm301121j
70848 200216 94 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
CHEMBL89445 200216 94 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
129908109 157520 0 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 477 9 1 6 5.3 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)C3CCCCC3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4089429 157520 0 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 477 9 1 6 5.3 CC(=O)Oc1ccc(/C=C/C(=O)CCc2ccc(NC(=O)C3CCCCC3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
1167892 82789 1 CCR5 CCR5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 463 9 1 6 4.7 Cc1ccc(NC(=O)CSc2nnc(CCN3CCCCC3)n2Cc2ccccc2)c(C)c1 10.1021/jm061389p
CHEMBL219781 82789 1 CCR5 CCR5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assayAgonist activity at CCR5 expressed in CHO-K1 cells in aqeuorin based assay
ChEMBL 463 9 1 6 4.7 Cc1ccc(NC(=O)CSc2nnc(CCN3CCCCC3)n2Cc2ccccc2)c(C)c1 10.1021/jm061389p
129908455 155452 0 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 503 11 1 7 4.9 COc1ccc(C(=O)Nc2ccc(CCC(=O)CCc3ccc(OC(C)=O)c(OC(C)=O)c3)cc2)cc1 10.1039/C6MD00311G
CHEMBL4064975 155452 0 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 503 11 1 7 4.9 COc1ccc(C(=O)Nc2ccc(CCC(=O)CCc3ccc(OC(C)=O)c(OC(C)=O)c3)cc2)cc1 10.1039/C6MD00311G
70848 200216 94 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
CHEMBL89445 200216 94 CCR5 CCR5 Human 4.5 pEC50 = 4.5 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 233 2 0 3 3.2 c1ccc(-c2cccc(-c3ccccn3)n2)nc1 10.1021/jm301121j
129908558 155364 0 CCR5 CCR5 Human 4.4 pEC50 = 4.4 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 403 8 3 4 4.8 Cc1ccc(C(=O)Nc2ccc(CCC(=O)CCc3ccc(O)c(O)c3)cc2)cc1 10.1039/C6MD00311G
CHEMBL4063935 155364 0 CCR5 CCR5 Human 4.4 pEC50 = 4.4 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 403 8 3 4 4.8 Cc1ccc(C(=O)Nc2ccc(CCC(=O)CCc3ccc(O)c(O)c3)cc2)cc1 10.1039/C6MD00311G
10585 1018 1 CCR5 CCR5 Human 8.4 pEC50 = 8.4 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1018 1 CCR5 CCR5 Human 8.4 pEC50 = 8.4 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1018 1 CCR5 CCR5 Human 8.4 pEC50 = 8.4 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
129907953 158677 0 CCR5 CCR5 Human 4.4 pEC50 = 4.4 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 434 9 3 6 4.4 O=C(CCc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
132519569 158677 0 CCR5 CCR5 Human 4.4 pEC50 = 4.4 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 434 9 3 6 4.4 O=C(CCc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
CHEMBL4101931 158677 0 CCR5 CCR5 Human 4.4 pEC50 = 4.4 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 434 9 3 6 4.4 O=C(CCc1ccc(NC(=O)c2ccc([N+](=O)[O-])cc2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
129908281 157751 0 CCR5 CCR5 Human 5.3 pEC50 = 5.3 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 473 10 1 6 4.9 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)c3ccccc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
CHEMBL4091826 157751 0 CCR5 CCR5 Human 5.3 pEC50 = 5.3 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 473 10 1 6 4.9 CC(=O)Oc1ccc(CCC(=O)CCc2ccc(NC(=O)c3ccccc3)cc2)cc1OC(C)=O 10.1039/C6MD00311G
1318 161142 105 CCR5 CCR5 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 c1cnc2c(c1)ccc1cccnc12 10.1021/jm301121j
CHEMBL415879 161142 105 CCR5 CCR5 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 c1cnc2c(c1)ccc1cccnc12 10.1021/jm301121j
10585 1018 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1018 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1018 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 173237 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173237 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 173237 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173237 1 CCR5 CCR5 Human 8.3 pEC50 = 8.3 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 30 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
1318 161142 105 CCR5 CCR5 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 c1cnc2c(c1)ccc1cccnc12 10.1021/jm301121j
CHEMBL415879 161142 105 CCR5 CCR5 Human 5.3 pEC50 = 5.3 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 180 0 0 2 2.8 c1cnc2c(c1)ccc1cccnc12 10.1021/jm301121j
129908560 156117 0 CCR5 CCR5 Human 4.3 pEC50 = 4.3 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 409 9 3 5 4.5 O=C(CCc1ccc(NC(=O)Cc2cccs2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
CHEMBL4072528 156117 0 CCR5 CCR5 Human 4.3 pEC50 = 4.3 Binding
Antagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assayAntagonist activity at CCR5 in human TZM-bl cells infected with CCR5-tropic HIV-1 Bal assessed as inhibition of viral entry after 3 days by luciferase reporter gene assay
ChEMBL 409 9 3 5 4.5 O=C(CCc1ccc(NC(=O)Cc2cccs2)cc1)CCc1ccc(O)c(O)c1 10.1039/C6MD00311G
155491018 173237 1 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173237 1 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
155491018 173237 1 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173237 1 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 100 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
65237 136834 88 CCR5 CCR5 Human 4.2 pEC50 = 4.2 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
CHEMBL375781 136834 88 CCR5 CCR5 Human 4.2 pEC50 = 4.2 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
65237 136834 88 CCR5 CCR5 Human 4.2 pEC50 = 4.2 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
CHEMBL375781 136834 88 CCR5 CCR5 Human 4.2 pEC50 = 4.2 Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL 208 0 0 2 3.4 Cc1ccc2ccc3ccc(C)nc3c2n1 10.1021/jm301121j
183790 3514 6 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assayPositive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
783 3514 6 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assayPositive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
CHEMBL1178786 3514 6 CCR5 CCR5 Human 8.2 pEC50 = 8.2 Functional
Positive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assayPositive allosteric modulation of human CCR5 expressed in HEK293T cells co-expressing CAMYEL assessed as increase in CCL4-induced inhibition of forskolin-stimulated cAMP accumulation after 10 mins by BRET assay
ChEMBL 495 6 1 2 6.8 Cc1ccc(cc1)c1ccc2c(c1)C=C(CCC2)C(=O)Nc1ccc(cc1)C[N+](C1CCOCC1)(C)C 10.1016/j.ejmech.2017.04.046
10585 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
10585 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 173237 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173237 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as pEC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 8.42 +/- 0.06 No_unit)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
10585 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
145996522 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
CHEMBL4531005 1018 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 1000 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 351 3 2 5 3.0 Nc1nn2c(n1)[nH]c(c(c2=O)Cc1cccc(c1Cl)Cl)C(C)C 10.1021/acs.jmedchem.9b00742
155491018 173237 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
CHEMBL4544504 173237 1 CCR5 CCR5 Human 8.1 pEC50 = 8.1 Functional
Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)Non-competitive insurmountable antagonist activity at human CCR5 expressed in human U2OS cell membranes assessed as EC50 for CCL3-stimulated [35S]GTPgammaS binding at 300 nM preincubated for 30 mins followed by [35S]GTPgammaS addition and measured after 90 mins (Rvb = 4 nM)
ChEMBL 395 3 2 5 3.1 CC(C)c1[nH]c2nc(N)nn2c(=O)c1Cc1ccc(Cl)c(Br)c1 10.1021/acs.jmedchem.9b00742
483747 104692 2 CCR5 CCR5 Human 11.0 pIC50 = 11 Binding
Inhibition of 0.1 nM of MIP-1beta induced migration of recombinant mouse pro-B cell line BA/F3 expressing human CCR5Inhibition of 0.1 nM of MIP-1beta induced migration of recombinant mouse pro-B cell line BA/F3 expressing human CCR5
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1016/s0960-894x(02)00918-6
CHEMBL311795 104692 2 CCR5 CCR5 Human 11.0 pIC50 = 11 Binding
Inhibition of 0.1 nM of MIP-1beta induced migration of recombinant mouse pro-B cell line BA/F3 expressing human CCR5Inhibition of 0.1 nM of MIP-1beta induced migration of recombinant mouse pro-B cell line BA/F3 expressing human CCR5
ChEMBL 503 4 0 5 4.9 Cc1ncnc(C)c1C(=O)N1CCC(C)(N2CCN([C@@H](C)c3ccc(C(F)(F)F)cc3)[C@@H](C)C2)CC1 10.1016/s0960-894x(02)00918-6
44590586 175959 0 CCR5 CCR5 Human 10.3 pIC50 = 10.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 543 10 1 3 6.3 CCN(C(=O)Cc1ccc(Cl)c(Cl)c1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
CHEMBL460845 175959 0 CCR5 CCR5 Human 10.3 pIC50 = 10.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 543 10 1 3 6.3 CCN(C(=O)Cc1ccc(Cl)c(Cl)c1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
10076141 77746 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 546 11 1 3 6.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL21106 77746 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 546 11 1 3 6.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
10076141 77746 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 546 11 1 3 6.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL21106 77746 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 546 11 1 3 6.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
10076141 77746 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 546 11 1 3 6.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL21106 77746 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 546 11 1 3 6.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44590681 174328 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 553 11 1 5 4.4 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
CHEMBL457043 174328 0 CCR5 CCR5 Human 10.2 pIC50 = 10.2 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 553 11 1 5 4.4 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
15941255 81125 0 CCR5 CCR5 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 527 9 2 6 4.5 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2Cl)CC1 10.1021/ml2002604
CHEMBL2164207 81125 0 CCR5 CCR5 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 527 9 2 6 4.5 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2Cl)CC1 10.1021/ml2002604
57402801 68650 0 CCR5 CCR5 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 600 12 2 7 5.2 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(C(=O)NC(C)C)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1926899 68650 0 CCR5 CCR5 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 600 12 2 7 5.2 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(C(=O)NC(C)C)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
44273531 74445 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 542 11 1 4 6.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL20345 74445 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 542 11 1 4 6.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
501062 77143 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 488 11 1 3 6.1 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL20896 77143 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 488 11 1 3 6.1 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL1649924 56693 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 497 6 1 6 3.9 COC(=O)N1CCc2nc(C)n([C@@H]3C[C@@H]4CC[C@H](C3)N4CC[C@H](NC(C)=O)c3cccc(F)c3)c2C1 10.1021/jm100978n
15940800 81120 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 561 10 1 7 3.9 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)CN2CCOC2=O)CC1 10.1021/ml2002604
CHEMBL2164202 81120 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 561 10 1 7 3.9 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)CN2CCOC2=O)CC1 10.1021/ml2002604
15941086 81128 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 518 9 2 7 3.7 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(C#N)nc2Cl)CC1 10.1021/ml2002604
CHEMBL2164210 81128 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 518 9 2 7 3.7 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(C#N)nc2Cl)CC1 10.1021/ml2002604
501062 77143 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 488 11 1 3 6.1 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2005.02.030
CHEMBL20896 77143 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 488 11 1 3 6.1 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2005.02.030
44273531 74445 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 542 11 1 4 6.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL20345 74445 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 542 11 1 4 6.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44332684 106458 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 474 11 1 3 5.7 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL316475 106458 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 474 11 1 3 5.7 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
501060 107860 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 474 10 1 3 5.7 O=C(O)[C@@H](C1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL320386 107860 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 474 10 1 3 5.7 O=C(O)[C@@H](C1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
501055 4363 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 502 10 1 3 6.5 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL102826 4363 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 502 10 1 3 6.5 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
501062 77143 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 488 11 1 3 6.1 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL20896 77143 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 488 11 1 3 6.1 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
44332684 106458 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 474 11 1 3 5.7 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL316475 106458 0 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 474 11 1 3 5.7 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
501060 107860 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 474 10 1 3 5.7 O=C(O)[C@@H](C1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL320386 107860 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 474 10 1 3 5.7 O=C(O)[C@@H](C1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
11285792 833 24 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 833 24 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 833 24 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 833 24 CCR5 CCR5 Human 10.0 pIC50 = 10 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
490018 110894 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 568 11 0 6 6.1 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN(Cc3ccccc3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
CHEMBL328445 110894 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 568 11 0 6 6.1 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN(Cc3ccccc3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
3002976 200815 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 634 14 0 7 5.9 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(CC[C@](C)(CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
CHEMBL93139 200815 1 CCR5 CCR5 Human 10.0 pIC50 = 10 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 634 14 0 7 5.9 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(CC[C@](C)(CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
62706107 81135 0 CCR5 CCR5 Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 554 9 2 6 5.5 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)Nc2cccnc2)CC1 10.1021/ml2002604
CHEMBL2164217 81135 0 CCR5 CCR5 Human 10.0 pIC50 = 10.0 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 554 9 2 6 5.5 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)Nc2cccnc2)CC1 10.1021/ml2002604
44373756 50140 0 CCR5 CCR5 Human 9.9 pIC50 = 9.9 Binding
Ability to displace [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesAbility to displace [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 588 9 0 7 6.3 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN3OC4(CCCCC4)C[C@H]3[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00835-6
CHEMBL157491 50140 0 CCR5 CCR5 Human 9.9 pIC50 = 9.9 Binding
Ability to displace [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesAbility to displace [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 588 9 0 7 6.3 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN3OC4(CCCCC4)C[C@H]3[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00835-6
11988311 178472 0 CCR5 CCR5 Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 451 8 1 5 5.2 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CCCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
CHEMBL473558 178472 0 CCR5 CCR5 Human 9.9 pIC50 = 9.9 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 451 8 1 5 5.2 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CCCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
44590750 176045 0 CCR5 CCR5 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 490 10 2 3 5.1 CCN(C(=O)NCc1ccccc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
CHEMBL461687 176045 0 CCR5 CCR5 Human 9.8 pIC50 = 9.8 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 490 10 2 3 5.1 CCN(C(=O)NCc1ccccc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
71451877 81923 0 CCR5 CCR5 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 638 11 0 6 5.0 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 10.1021/jm300682j
CHEMBL2178577 81923 0 CCR5 CCR5 Human 9.8 pIC50 = 9.8 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 638 11 0 6 5.0 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 10.1021/jm300682j
11650548 102828 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 697 17 1 8 8.1 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4nncn4CCC)cc2)CCCN3CC(C)C)cc1 10.1021/jm0509703
CHEMBL3085308 102828 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 697 17 1 8 8.1 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4nncn4CCC)cc2)CCCN3CC(C)C)cc1 10.1021/jm0509703
44274043 75963 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 542 11 1 3 6.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL20622 75963 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 542 11 1 3 6.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00829-6
44273830 78964 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 574 11 1 3 7.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(C(F)(F)F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL21147 78964 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 574 11 1 3 7.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(C(F)(F)F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
15947119 68644 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 549 10 1 6 5.7 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(Cl)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1926893 68644 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 549 10 1 6 5.7 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(Cl)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1201187 14143 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1[C@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1021/jm100978n
CHEMBL1649926 56695 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 497 6 1 6 3.9 COC(=O)N[C@@H](CCN1[C@H]2CC[C@@H]1C[C@H](n1c(C)nc3c1CN(C(C)=O)CC3)C2)c1cccc(F)c1 10.1021/jm100978n
CHEMBL1649927 56696 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 513 6 1 7 4.1 COC(=O)N[C@@H](CCN1[C@H]2CC[C@@H]1C[C@H](n1c(C)nc3c1CN(C(=O)OC)CC3)C2)c1cccc(F)c1 10.1021/jm100978n
CHEMBL1201187 14143 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1[C@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1016/j.bmcl.2009.01.008
CHEMBL1201187 14143 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1[C@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1016/j.bmcl.2009.01.009
10414981 107416 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 542 10 2 6 5.3 OC1(CCCc2ccc(-c3nnn[nH]3)cc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(02)00605-4
CHEMBL319593 107416 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 542 10 2 6 5.3 OC1(CCCc2ccc(-c3nnn[nH]3)cc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(02)00605-4
44332341 108925 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 556 10 1 7 5.3 Cn1nnnc1-c1ccc(CCCC2(O)CCN(C[C@H]3CN(CC4CCCCC4)C[C@@H]3c3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00605-4
CHEMBL322422 108925 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 556 10 1 7 5.3 Cn1nnnc1-c1ccc(CCCC2(O)CCN(C[C@H]3CN(CC4CCCCC4)C[C@@H]3c3ccccc3)CC2)cc1 10.1016/s0960-894x(02)00605-4
44274043 75963 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 542 11 1 3 6.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL20622 75963 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 542 11 1 3 6.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
44273830 78964 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 574 11 1 3 7.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(C(F)(F)F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL21147 78964 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 574 11 1 3 7.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(C(F)(F)F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
10414981 107416 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 542 10 2 6 5.3 OC1(CCCc2ccc(-c3nnn[nH]3)cc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
CHEMBL319593 107416 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 542 10 2 6 5.3 OC1(CCCc2ccc(-c3nnn[nH]3)cc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
501063 201959 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 488 10 1 3 6.1 O=C(O)[C@@H](C1CCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL99909 201959 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 488 10 1 3 6.1 O=C(O)[C@@H](C1CCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
10414981 107416 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 542 10 2 6 5.3 OC1(CCCc2ccc(-c3nnn[nH]3)cc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(02)00606-6
CHEMBL319593 107416 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 542 10 2 6 5.3 OC1(CCCc2ccc(-c3nnn[nH]3)cc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(02)00606-6
501063 201959 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 488 10 1 3 6.1 O=C(O)[C@@H](C1CCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL99909 201959 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 488 10 1 3 6.1 O=C(O)[C@@H](C1CCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL1201187 14143 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of CCR5 in human TZM-bl cells infected with HIV1 Bal R5 assessed as antiviral activity by measuring reduction in viral infection pre-incubated with cells followed by viral infection measured after 3 days by luciferase reporter gene assayInhibition of CCR5 in human TZM-bl cells infected with HIV1 Bal R5 assessed as antiviral activity by measuring reduction in viral infection pre-incubated with cells followed by viral infection measured after 3 days by luciferase reporter gene assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1[C@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1016/j.bmc.2016.12.035
501055 4363 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assayInhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assay
ChEMBL 502 10 1 3 6.5 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2003.12.004
CHEMBL102826 4363 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assayInhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assay
ChEMBL 502 10 1 3 6.5 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2003.12.004
11285792 833 24 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cellsInhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 833 24 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cellsInhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 833 24 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cellsInhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 833 24 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cellsInhibition of replication of R5 HIV1 Ba-L in MOLT4/CCR5 cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
516310 59075 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 642 12 1 6 7.1 CCn1nc(Cc2ccc(OC3CC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL171958 59075 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 642 12 1 6 7.1 CCn1nc(Cc2ccc(OC3CC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516257 59445 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc5ccccc5c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL173400 59445 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc5ccccc5c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516288 59857 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 9 1 5 7.2 CCn1nc(Cc2cccc3ccccc23)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL174927 59857 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 9 1 5 7.2 CCn1nc(Cc2cccc3ccccc23)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516256 127863 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4cccc5ccccc45)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL366770 127863 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4cccc5ccccc45)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516289 130761 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 9 1 5 7.2 CCn1nc(Cc2ccc3ccccc3c2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL369235 130761 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 9 1 5 7.2 CCn1nc(Cc2ccc3ccccc3c2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
490023 111780 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 574 10 0 6 5.6 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN(C(=O)C3CCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
CHEMBL329893 111780 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 574 10 0 6 5.6 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN(C(=O)C3CCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
490019 167144 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 582 10 0 6 5.7 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN(C(=O)c3ccccc3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
CHEMBL431852 167144 1 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cellsInhibitory concentration, binding towards C-C chemokine receptor type 5 using [125I]-MIP-1 alpha as radioligand expressed on CHO cells
ChEMBL 582 10 0 6 5.7 C=CCN(C(=O)OCc1ccc([N+](=O)[O-])cc1)C1CCN(C[C@H]2CN(C(=O)c3ccccc3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(01)00545-5
11513274 102829 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 734 17 1 9 8.0 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4cncn4CCC)cc2)CCCN3Cc2cnn(C)c2)cc1 10.1021/jm0509703
CHEMBL3085309 102829 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 734 17 1 9 8.0 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4cncn4CCC)cc2)CCCN3Cc2cnn(C)c2)cc1 10.1021/jm0509703
9916998 79340 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cells
ChEMBL 614 11 0 6 4.7 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cccc(F)c2)CC1 10.1016/j.bmcl.2006.03.089
CHEMBL212731 79340 0 CCR5 CCR5 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cells
ChEMBL 614 11 0 6 4.7 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cccc(F)c2)CC1 10.1016/j.bmcl.2006.03.089
3010274 186381 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 543 10 1 5 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL511493 186381 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 543 10 1 5 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010273 187410 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 529 10 1 5 5.9 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL520091 187410 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 529 10 1 5 5.9 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
44342962 110491 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 529 10 1 5 5.9 O=C(O)C(CC1CC1)N1CC(c2ccccc2)[C@@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL326487 110491 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 529 10 1 5 5.9 O=C(O)C(CC1CC1)N1CC(c2ccccc2)[C@@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)C1 10.1016/j.bmcl.2004.04.078
44342961 113797 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 543 10 1 5 6.3 O=C(O)C(CC1CCC1)N1CC(c2ccccc2)[C@@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL333619 113797 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 543 10 1 5 6.3 O=C(O)C(CC1CCC1)N1CC(c2ccccc2)[C@@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)C1 10.1016/j.bmcl.2004.04.078
3010274 186381 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 543 10 1 5 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL511493 186381 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 543 10 1 5 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010273 187410 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 529 10 1 5 5.9 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL520091 187410 1 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 529 10 1 5 5.9 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
9810893 102827 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 682 17 1 7 8.5 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4cncn4CCC)cc2)CCCN3CCC)cc1 10.1021/jm0509703
CHEMBL3085307 102827 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 682 17 1 7 8.5 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4cncn4CCC)cc2)CCCN3CCC)cc1 10.1021/jm0509703
11285792 833 24 CCR5 CCR5 Mouse 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1016/j.ejmech.2018.01.085
801 833 24 CCR5 CCR5 Mouse 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1016/j.ejmech.2018.01.085
CHEMBL2110727 833 24 CCR5 CCR5 Mouse 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1016/j.ejmech.2018.01.085
DB11758 833 24 CCR5 CCR5 Mouse 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1016/j.ejmech.2018.01.085
11614352 524 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 639 11 0 6 4.1 CCN(C(=O)Cc1ccc(cc1)S(=O)(=O)C)C1CCN(CC1)CC[C@@H](c1cc(F)cc(c1)F)C1CCN(CC1)S(=O)(=O)C 10.1016/j.bmcl.2011.12.117
7686 524 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 639 11 0 6 4.1 CCN(C(=O)Cc1ccc(cc1)S(=O)(=O)C)C1CCN(CC1)CC[C@@H](c1cc(F)cc(c1)F)C1CCN(CC1)S(=O)(=O)C 10.1016/j.bmcl.2011.12.117
CHEMBL1951914 524 0 CCR5 CCR5 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 639 11 0 6 4.1 CCN(C(=O)Cc1ccc(cc1)S(=O)(=O)C)C1CCN(CC1)CC[C@@H](c1cc(F)cc(c1)F)C1CCN(CC1)S(=O)(=O)C 10.1016/j.bmcl.2011.12.117
3010264 182926 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 557 9 1 5 6.7 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL480503 182926 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 557 9 1 5 6.7 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010264 182926 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 557 9 1 5 6.7 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL480503 182926 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 557 9 1 5 6.7 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010264 182926 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 557 9 1 5 6.7 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL480503 182926 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 557 9 1 5 6.7 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
10347790 77813 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 11 1 3 6.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL21117 77813 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 11 1 3 6.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44565720 173484 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 570 11 1 3 7.5 O=C(O)[C@@H](CC1CCCCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL455073 173484 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 570 11 1 3 7.5 O=C(O)[C@@H](CC1CCCCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
20672370 77442 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 531 11 1 4 6.1 N#Cc1ccc(CCCC2CCN(C[C@H]3CN([C@H](CC4CCC4)C(=O)O)C[C@@H]3c3cccc(F)c3)CC2)cc1 10.1016/s0960-894x(02)00829-6
CHEMBL20988 77442 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 531 11 1 4 6.1 N#Cc1ccc(CCCC2CCN(C[C@H]3CN([C@H](CC4CCC4)C(=O)O)C[C@@H]3c3cccc(F)c3)CC2)cc1 10.1016/s0960-894x(02)00829-6
10347790 77813 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 560 11 1 3 6.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL21117 77813 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 560 11 1 3 6.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
20672362 98734 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 556 10 1 3 7.2 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL282921 98734 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 556 10 1 3 7.2 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00829-6
44511934 68647 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 533 10 1 6 5.2 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(F)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1926896 68647 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 533 10 1 6 5.2 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(F)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
44512090 68649 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 540 10 1 7 5.0 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(C#N)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1926898 68649 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 540 10 1 7 5.0 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(C#N)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
44512058 68658 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 551 10 1 8 4.5 COc1ccc(N(Cc2cccc(C#N)n2)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(C#N)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1927008 68658 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 551 10 1 8 4.5 COc1ccc(N(Cc2cccc(C#N)n2)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(C#N)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
44511938 68659 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 560 10 1 7 5.3 COc1ccc(N(Cc2cccc(C#N)n2)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(Cl)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1927009 68659 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 560 10 1 7 5.3 COc1ccc(N(Cc2cccc(C#N)n2)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(Cl)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1649922 56692 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 479 6 1 6 3.8 COC(=O)N1CCc2nc(C)n([C@@H]3C[C@@H]4CC[C@H](C3)N4CC[C@H](NC(C)=O)c3ccccc3)c2C1 10.1021/jm100978n
62706110 81121 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 491 8 2 5 4.2 CNC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
CHEMBL2164203 81121 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 491 8 2 5 4.2 CNC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
15940799 81123 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 493 8 3 6 4.0 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)NO)CC1 10.1021/ml2002604
CHEMBL2164205 81123 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 493 8 3 6 4.0 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)NO)CC1 10.1021/ml2002604
57384005 81124 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 507 9 2 6 4.2 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
CHEMBL2164206 81124 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 507 9 2 6 4.2 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
57384006 81129 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 551 12 2 7 4.2 COCCONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
CHEMBL2164211 81129 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 551 12 2 7 4.2 COCCONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
10369469 69772 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 522 8 1 5 5.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4ccc(F)cn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
CHEMBL194497 69772 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 522 8 1 5 5.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4ccc(F)cn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
489315 106638 2 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes.Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes.
ChEMBL 474 9 1 3 6.1 OC1(CCCc2ccccc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(02)00605-4
CHEMBL317710 106638 2 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes.Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes.
ChEMBL 474 9 1 3 6.1 OC1(CCCc2ccccc2)CCN(C[C@H]2CN(CC3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/s0960-894x(02)00605-4
10347790 77813 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 11 1 3 6.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL21117 77813 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 11 1 3 6.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44565720 173484 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 570 11 1 3 7.5 O=C(O)[C@@H](CC1CCCCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL455073 173484 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 570 11 1 3 7.5 O=C(O)[C@@H](CC1CCCCC1)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
72712598 91967 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 5 0 4 6.6 Cc1cc(Cl)nc(C)c1C(=O)N1CCC(C)(N2CCC(N3C(=O)N(C4CCCCC4)C[C@H]3c3ccccc3)CC2)CC1 10.1021/jm401101p
CHEMBL2435848 91967 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 591 5 0 4 6.6 Cc1cc(Cl)nc(C)c1C(=O)N1CCC(C)(N2CCC(N3C(=O)N(C4CCCCC4)C[C@H]3c3ccccc3)CC2)CC1 10.1021/jm401101p
516231 59317 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc5ccccc5c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL172894 59317 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc5ccccc5c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516245 59324 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 13 1 6 6.6 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC5CC5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL172916 59324 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 13 1 6 6.6 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC5CC5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516235 59679 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 636 12 1 5 7.7 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(-c5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL174004 59679 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 636 12 1 5 7.7 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(-c5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516224 61104 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 626 13 1 6 6.6 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL177127 61104 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 626 13 1 6 6.6 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516234 98300 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 11 1 5 7.3 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(C)(C)C)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL279992 98300 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 11 1 5 7.3 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(C)(C)C)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516233 127896 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 602 12 1 5 7.2 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(C)C)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL366868 127896 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 602 12 1 5 7.2 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(C)C)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516202 129498 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 11 1 5 7.3 CCn1nc(Cc2ccc(-c3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL367987 129498 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 11 1 5 7.3 CCn1nc(Cc2ccc(-c3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516314 129900 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 662 11 1 5 8.2 CCn1nc(Cc2ccc(-c3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL368329 129900 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 662 11 1 5 8.2 CCn1nc(Cc2ccc(-c3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516216 130652 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 13 1 6 6.6 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC5CC5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL369059 130652 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 13 1 6 6.6 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC5CC5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516262 165538 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 628 9 1 5 7.0 CCn1nc(Cc2ccc(C(F)(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL427493 165538 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 628 9 1 5 7.0 CCn1nc(Cc2ccc(C(F)(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516232 167693 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 574 11 1 5 6.3 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL435472 167693 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 574 11 1 5 6.3 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
16007088 79330 8 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 632 11 0 6 4.8 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cc(F)cc(F)c2)CC1 10.1021/jm300682j
CHEMBL212689 79330 8 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 632 11 0 6 4.8 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cc(F)cc(F)c2)CC1 10.1021/jm300682j
16007088 79330 8 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cells
ChEMBL 632 11 0 6 4.8 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2006.03.089
CHEMBL212689 79330 8 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cells
ChEMBL 632 11 0 6 4.8 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2006.03.089
16007088 79330 8 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 632 11 0 6 4.8 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.12.117
CHEMBL212689 79330 8 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 632 11 0 6 4.8 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@H](c2ccc(S(C)(=O)=O)cc2)c2cc(F)cc(F)c2)CC1 10.1016/j.bmcl.2011.12.117
3010271 182965 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 527 10 1 5 5.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)o3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL480693 182965 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 527 10 1 5 5.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)o3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
44590633 175356 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 509 10 1 3 5.6 CCN(C(=O)Cc1ccc(Cl)cc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
CHEMBL459384 175356 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 509 10 1 3 5.6 CCN(C(=O)Cc1ccc(Cl)cc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
3010271 182965 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 527 10 1 5 5.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)o3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL480693 182965 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 527 10 1 5 5.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)o3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010271 182965 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 527 10 1 5 5.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)o3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL480693 182965 1 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 527 10 1 5 5.8 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)o3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
44401488 69500 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 532 9 1 5 5.6 CCc1ccn2c(C3CCN(C[C@H]4CN([C@H](CC5CCC5)C(=O)O)C[C@@H]4c4cccc(F)c4)CC3)cnc2c1 10.1016/j.bmcl.2005.02.030
CHEMBL193984 69500 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 532 9 1 5 5.6 CCc1ccn2c(C3CCN(C[C@H]4CN([C@H](CC5CCC5)C(=O)O)C[C@@H]4c4cccc(F)c4)CC3)cnc2c1 10.1016/j.bmcl.2005.02.030
CHEMBL1784385 62312 0 CCR5 CCR5 Human 9.5 pIC50 = 9.5 Binding
Displacement of 125I-MIP-1beta from human CCR5 receptor after 4 hrs by scintillation countingDisplacement of 125I-MIP-1beta from human CCR5 receptor after 4 hrs by scintillation counting
ChEMBL 512 5 0 4 6.5 Cc1nc2ccccc2n1[C@@H]1C[C@@H]2CC[C@H](C1)N2CCC1(c2ccccc2)CCN(C(=O)C(C)(C)C)CC1 10.1021/jm200279v
CHEMBL1201187 14143 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 MGC26-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assayAntagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 MGC26-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1[C@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1021/ml400370w
44565038 184180 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 473 8 1 5 5.0 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CC(F)(F)C2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
CHEMBL489513 184180 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 473 8 1 5 5.0 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CC(F)(F)C2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
CHEMBL491679 184180 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 473 8 1 5 5.0 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CC(F)(F)C2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
3010268 78073 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 526 10 2 4 5.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3c[nH]c(Cc4ccccc4)n3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL2112559 78073 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 526 10 2 4 5.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3c[nH]c(Cc4ccccc4)n3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
44273996 74972 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 526 11 2 4 5.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(O)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL20453 74972 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 526 11 2 4 5.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(O)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44565673 176790 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 556 10 1 7 5.3 Cn1nnc(-c2ccc(CCCC3(O)CCN(C[C@H]4CN(CC5CCCCC5)C[C@@H]4c4ccccc4)CC3)cc2)n1 10.1016/j.ejmech.2008.01.040
CHEMBL464132 176790 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 556 10 1 7 5.3 Cn1nnc(-c2ccc(CCCC3(O)CCN(C[C@H]4CN(CC5CCCCC5)C[C@@H]4c4ccccc4)CC3)cc2)n1 10.1016/j.ejmech.2008.01.040
44273996 74972 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 526 11 2 4 5.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(O)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL20453 74972 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 526 11 2 4 5.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(O)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
44273888 98070 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 558 11 1 4 5.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CC[S+]([O-])c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL278117 98070 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 558 11 1 4 5.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CC[S+]([O-])c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
50915506 18669 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 in HOS cells assessed as inhibition of HIV-1 Ba-L infectionAntagonist activity at CCR5 in HOS cells assessed as inhibition of HIV-1 Ba-L infection
ChEMBL 848 11 2 6 8.2 CC(C)(C)NS(=O)(=O)c1cc(C(=O)N2CCC(CCN3CCC(N(C(=O)NCc4ccc(C#N)cc4)c4cccc(F)c4)CC3)(c3cccc(F)c3)CC2)c(Cl)cc1F 10.1016/j.bmcl.2010.10.033
CHEMBL1288663 18669 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 in HOS cells assessed as inhibition of HIV-1 Ba-L infectionAntagonist activity at CCR5 in HOS cells assessed as inhibition of HIV-1 Ba-L infection
ChEMBL 848 11 2 6 8.2 CC(C)(C)NS(=O)(=O)c1cc(C(=O)N2CCC(CCN3CCC(N(C(=O)NCc4ccc(C#N)cc4)c4cccc(F)c4)CC3)(c3cccc(F)c3)CC2)c(Cl)cc1F 10.1016/j.bmcl.2010.10.033
CHEMBL257000 94735 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor by [35S]GTP-gamma-S binding assayAntagonist activity at CCR5 receptor by [35S]GTP-gamma-S binding assay
ChEMBL 608 7 1 5 6.4 CC(=O)N1CCc2c(nc(C)n2[C@H]2C[C@@H]3CC[C@H](C2)N3CCCN(C(=O)Nc2ccc(C(F)(F)F)cc2)c2ccccc2)C1 10.1016/j.bmcl.2007.12.058
CHEMBL1649919 56688 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 463 6 1 5 3.5 CC(=O)N[C@@H](CCN1[C@H]2CC[C@@H]1C[C@H](n1c(C)nc3c1CN(C(C)=O)CC3)C2)c1ccccc1 10.1021/jm100978n
CHEMBL1649920 56690 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 477 7 1 5 3.9 CCC(=O)N1CCc2nc(C)n([C@@H]3C[C@@H]4CC[C@H](C3)N4CC[C@H](NC(C)=O)c3ccccc3)c2C1 10.1021/jm100978n
CHEMBL1649921 56691 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 491 7 1 5 4.2 CC(=O)N[C@@H](CCN1[C@H]2CC[C@@H]1C[C@H](n1c(C)nc3c1CN(C(=O)C(C)C)CC3)C2)c1ccccc1 10.1021/jm100978n
59458228 81126 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 558 11 3 7 3.6 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(C(=O)NC(C)C)nc2C)CC1 10.1021/ml2002604
CHEMBL2164208 81126 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 558 11 3 7 3.6 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(C(=O)NC(C)C)nc2C)CC1 10.1021/ml2002604
59458061 81127 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 543 9 2 6 3.7 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)[n+]([O-])c2Cl)CC1 10.1021/ml2002604
CHEMBL2164209 81127 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 543 9 2 6 3.7 CONC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)[n+]([O-])c2Cl)CC1 10.1021/ml2002604
15941083 81137 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 506 10 1 6 4.1 COCC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
CHEMBL2164219 81137 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 506 10 1 6 4.1 COCC(=O)N(Cc1ccsc1)C1CCN([C@H](C)CCNC(=O)c2c(C)cc(Cl)nc2C)CC1 10.1021/ml2002604
15940801 81138 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 501 9 1 6 4.3 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)CC#N)CC1 10.1021/ml2002604
CHEMBL2164220 81138 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 501 9 1 6 4.3 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)CC#N)CC1 10.1021/ml2002604
44357079 118591 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranesDisplacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranes
ChEMBL 541 11 1 6 4.8 CCCN(c1ncc(F)cn1)C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/s0960-894x(02)00988-5
CHEMBL344261 118591 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranesDisplacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranes
ChEMBL 541 11 1 6 4.8 CCCN(c1ncc(F)cn1)C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/s0960-894x(02)00988-5
3001322 423 12 CCR5 CCR5 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 577 10 3 6 4.6 CCCCN1C(=O)[C@H](NC(=O)C21CCN(CC2)Cc1ccc(cc1)Oc1ccc(cc1)C(=O)O)[C@@H](C1CCCCC1)O 10.1016/j.ejmech.2018.01.085
805 423 12 CCR5 CCR5 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 577 10 3 6 4.6 CCCCN1C(=O)[C@H](NC(=O)C21CCN(CC2)Cc1ccc(cc1)Oc1ccc(cc1)C(=O)O)[C@@H](C1CCCCC1)O 10.1016/j.ejmech.2018.01.085
CHEMBL1255794 423 12 CCR5 CCR5 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 577 10 3 6 4.6 CCCCN1C(=O)[C@H](NC(=O)C21CCN(CC2)Cc1ccc(cc1)Oc1ccc(cc1)C(=O)O)[C@@H](C1CCCCC1)O 10.1016/j.ejmech.2018.01.085
DB06497 423 12 CCR5 CCR5 Mouse 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hrDisplacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr
ChEMBL 577 10 3 6 4.6 CCCCN1C(=O)[C@H](NC(=O)C21CCN(CC2)Cc1ccc(cc1)Oc1ccc(cc1)C(=O)O)[C@@H](C1CCCCC1)O 10.1016/j.ejmech.2018.01.085
44332489 4505 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 557 10 2 5 4.7 C[n+]1n[nH]c(-c2ccc(CCCC3(O)CCN(C[C@H]4CN(CC5CCCCC5)C[C@@H]4c4ccccc4)CC3)cc2)n1 10.1016/s0960-894x(02)00605-4
CHEMBL103790 4505 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 557 10 2 5 4.7 C[n+]1n[nH]c(-c2ccc(CCCC3(O)CCN(C[C@H]4CN(CC5CCCCC5)C[C@@H]4c4ccccc4)CC3)cc2)n1 10.1016/s0960-894x(02)00605-4
44273996 74972 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 526 11 2 4 5.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(O)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL20453 74972 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 526 11 2 4 5.5 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(CCC(O)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44565673 176790 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 556 10 1 7 5.3 Cn1nnc(-c2ccc(CCCC3(O)CCN(C[C@H]4CN(CC5CCCCC5)C[C@@H]4c4ccccc4)CC3)cc2)n1 10.1016/j.ejmech.2008.01.040
CHEMBL464132 176790 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 556 10 1 7 5.3 Cn1nnc(-c2ccc(CCCC3(O)CCN(C[C@H]4CN(CC5CCCCC5)C[C@@H]4c4ccccc4)CC3)cc2)n1 10.1016/j.ejmech.2008.01.040
58834969 91976 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 586 8 1 6 5.9 Cc1nc(Sc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
CHEMBL2435857 91976 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 586 8 1 6 5.9 Cc1nc(Sc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
516292 59739 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 9 1 5 7.3 CCn1nc(Cc2ccc(C(C)(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL174214 59739 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 9 1 5 7.3 CCn1nc(Cc2ccc(C(C)(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516201 59919 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 608 12 1 6 6.2 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
CHEMBL175348 59919 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 608 12 1 6 6.2 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
516246 60525 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 630 13 1 6 7.0 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC5CCC5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL176459 60525 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 630 13 1 6 7.0 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC5CCC5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516255 60732 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 13 1 6 6.6 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)[C@H](C)CC)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
CHEMBL176669 60732 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 13 1 6 6.6 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)[C@H](C)CC)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
516279 95792 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 652 11 1 6 7.8 CCn1nc(Cc2ccc(Oc3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL262402 95792 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 652 11 1 6 7.8 CCn1nc(Cc2ccc(Oc3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516230 127685 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4cccc5ccccc45)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL366611 127685 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 610 11 1 5 7.2 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4cccc5ccccc45)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516274 127899 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 11 1 6 6.6 CCn1nc(Cc2ccc(OC3CC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL366873 127899 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 11 1 6 6.6 CCn1nc(Cc2ccc(OC3CC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516221 131786 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 652 13 1 6 7.8 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(Oc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL369812 131786 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 652 13 1 6 7.8 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(Oc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516271 167423 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 11 1 6 6.4 CCOc1cccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)c1 10.1016/j.bmcl.2003.12.006
CHEMBL433793 167423 1 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 11 1 6 6.4 CCOc1cccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)c1 10.1016/j.bmcl.2003.12.006
20664161 78361 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 504 8 1 5 5.0 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4ccccn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
CHEMBL2113086 78361 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 504 8 1 5 5.0 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4ccccn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
5275766 3510 25 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 552 9 1 4 4.7 CC(=O)N1CCC(CC1)C(=O)N(c1ccc(c(c1)Cl)C)CCCN1CCC(CC1)Cc1ccc(cc1)C(=O)N 10.1021/jm051034q
800 3510 25 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 552 9 1 4 4.7 CC(=O)N1CCC(CC1)C(=O)N(c1ccc(c(c1)Cl)C)CCCN1CCC(CC1)Cc1ccc(cc1)C(=O)N 10.1021/jm051034q
CHEMBL207004 3510 25 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 552 9 1 4 4.7 CC(=O)N1CCC(CC1)C(=O)N(c1ccc(c(c1)Cl)C)CCCN1CCC(CC1)Cc1ccc(cc1)C(=O)N 10.1021/jm051034q
CHEMBL1201187 14143 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Antagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 YU2-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assayAntagonist activity against CCR5 receptor in human TZM-bl cells assessed as inhibition of HIV-1 YU2-induced cell-cell fusion between viral envelope protein expressing human HEK293 cells to TZM-bl cells after 48 hrs by luciferase reporter gene assay
ChEMBL 513 8 1 5 6.0 Cc1nnc(C(C)C)n1[C@H]1C[C@@H]2CC[C@H](C1)N2CC[C@H](NC(=O)C1CCC(F)(F)CC1)c1ccccc1 10.1021/ml400370w
57391721 70487 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 617 11 0 6 4.1 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cccc(C)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
CHEMBL1951913 70487 0 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 617 11 0 6 4.1 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cccc(C)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
3009355 3742 14 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 533 6 0 6 4.5 COC[C@H](N1CCN(C[C@@H]1C)C1(C)CCN(CC1)C(=O)c1c(C)ncnc1C)c1ccc(cc1)C(F)(F)F 10.1021/jm300682j
807 3742 14 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 533 6 0 6 4.5 COC[C@H](N1CCN(C[C@@H]1C)C1(C)CCN(CC1)C(=O)c1c(C)ncnc1C)c1ccc(cc1)C(F)(F)F 10.1021/jm300682j
CHEMBL82301 3742 14 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 533 6 0 6 4.5 COC[C@H](N1CCN(C[C@@H]1C)C1(C)CCN(CC1)C(=O)c1c(C)ncnc1C)c1ccc(cc1)C(F)(F)F 10.1021/jm300682j
DB06652 3742 14 CCR5 CCR5 Human 9.4 pIC50 = 9.4 Binding
Binding affinity to CCR5Binding affinity to CCR5
ChEMBL 533 6 0 6 4.5 COC[C@H](N1CCN(C[C@@H]1C)C1(C)CCN(CC1)C(=O)c1c(C)ncnc1C)c1ccc(cc1)C(F)(F)F 10.1021/jm300682j
44590634 173960 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 543 10 1 3 6.0 CCN(C(=O)Cc1ccc(C(F)(F)F)cc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
CHEMBL456226 173960 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 543 10 1 3 6.0 CCN(C(=O)Cc1ccc(C(F)(F)F)cc1)C1CCN(C(C)C[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.009
44565080 184407 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 473 8 1 5 5.0 Cc1nnc(C(C)C)n1C1CCN([C@H](C)C[C@H](NC(=O)C2CC(F)(F)C2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
CHEMBL491319 184407 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 473 8 1 5 5.0 Cc1nnc(C(C)C)n1C1CCN([C@H](C)C[C@H](NC(=O)C2CC(F)(F)C2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
11700429 102831 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 710 17 1 7 9.1 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4cncn4CCC)cc2)CCCCN3CC(C)C)cc1 10.1021/jm0509703
CHEMBL3085311 102831 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5Inhibition of membrane fusion between HIV1 JR-FL Env-expressing COS7 cells and MOLT4/CCR5
ChEMBL 710 17 1 7 9.1 CCCCOCCOc1ccc(-c2ccc3c(c2)/C=C(/C(=O)Nc2ccc([S@@+]([O-])Cc4cncn4CCC)cc2)CCCCN3CC(C)C)cc1 10.1021/jm0509703
20672360 76727 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 534 10 1 3 6.4 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL20831 76727 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 534 10 1 3 6.4 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
20672386 98059 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 506 11 1 3 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL278085 98059 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 506 11 1 3 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
44273888 98070 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 558 11 1 4 5.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CC[S+]([O-])c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL278117 98070 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 558 11 1 4 5.5 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CC[S+]([O-])c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL1649913 56682 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 416 6 1 4 4.8 CC(=O)N[C@@H](CCN1[C@H]2CC[C@@H]1C[C@H](n1c(C)nc3ccccc31)C2)c1ccccc1 10.1021/jm100978n
15940498 81130 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 611 11 3 6 5.5 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)NCc2ccc(C(=O)O)cc2)CC1 10.1021/ml2002604
CHEMBL2164212 81130 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 611 11 3 6 5.5 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)NCc2ccc(C(=O)O)cc2)CC1 10.1021/ml2002604
44590440 178339 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 487 6 0 3 5.2 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(Cc3ccccc3)C(=O)C3CC3)CC2)CC1 10.1016/j.bmcl.2009.01.012
CHEMBL472464 178339 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 487 6 0 3 5.2 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(Cc3ccccc3)C(=O)C3CC3)CC2)CC1 10.1016/j.bmcl.2009.01.012
457871 100016 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Antagonistic activity against monkey C-C chemokine receptor type 5.Antagonistic activity against monkey C-C chemokine receptor type 5.
ChEMBL 483 4 1 3 5.6 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(Nc3ccc(Br)cc3)CC2)CC1 10.1021/jm031046g
CHEMBL292625 100016 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Functional
Antagonistic activity against monkey C-C chemokine receptor type 5.Antagonistic activity against monkey C-C chemokine receptor type 5.
ChEMBL 483 4 1 3 5.6 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(Nc3ccc(Br)cc3)CC2)CC1 10.1021/jm031046g
44357078 118651 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranesDisplacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranes
ChEMBL 591 11 1 6 5.7 CCCN(c1ncc(C(F)(F)F)cn1)C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/s0960-894x(02)00988-5
CHEMBL344641 118651 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranesDisplacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranes
ChEMBL 591 11 1 6 5.7 CCCN(c1ncc(C(F)(F)F)cn1)C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/s0960-894x(02)00988-5
44401956 132791 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 572 8 1 5 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4c(Cl)cc(Cl)cn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
CHEMBL371177 132791 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 572 8 1 5 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4c(Cl)cc(Cl)cn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
20672386 98059 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 506 11 1 3 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL278085 98059 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 506 11 1 3 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44565742 178255 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 548 11 1 3 6.8 CC(C)C[C@H](C(=O)O)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL471920 178255 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 548 11 1 3 6.8 CC(C)C[C@H](C(=O)O)N1C[C@H](CN2CCC(CCC(F)(F)c3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
10163007 94414 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]RANTES from human CCR5 expressed in CHO cellsDisplacement of [125I]RANTES from human CCR5 expressed in CHO cells
ChEMBL 482 5 0 4 6.0 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(c3ccccc3)c3cccnc3)CC2)CC1 10.1016/j.bmcl.2008.01.108
CHEMBL255429 94414 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]RANTES from human CCR5 expressed in CHO cellsDisplacement of [125I]RANTES from human CCR5 expressed in CHO cells
ChEMBL 482 5 0 4 6.0 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(c3ccccc3)c3cccnc3)CC2)CC1 10.1016/j.bmcl.2008.01.108
501046 108948 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 518 10 2 4 5.6 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(O)(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL322603 108948 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 518 10 2 4 5.6 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(O)(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
72714079 92005 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 565 8 1 4 6.1 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@H](C)N1CCC(N2C(=O)N(C3CCCCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
CHEMBL2435886 92005 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 565 8 1 4 6.1 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@H](C)N1CCC(N2C(=O)N(C3CCCCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
516311 59373 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 11 1 6 7.7 CCn1nc(Cc2ccc(OC(C)(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL173091 59373 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 11 1 6 7.7 CCn1nc(Cc2ccc(OC(C)(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516312 59464 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 678 12 1 6 8.4 CCn1nc(Cc2ccc(Oc3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL173479 59464 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 678 12 1 6 8.4 CCn1nc(Cc2ccc(Oc3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516192 59491 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 618 14 1 6 6.8 CCCCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1 10.1016/j.bmcl.2003.12.006
CHEMBL173583 59491 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 618 14 1 6 6.8 CCCCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1 10.1016/j.bmcl.2003.12.006
516282 59863 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 626 11 1 6 6.6 CCn1nc(Cc2ccc(OC(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL174996 59863 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 626 11 1 6 6.6 CCn1nc(Cc2ccc(OC(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516228 59877 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 615 12 1 7 5.9 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC)c(C#N)c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL175079 59877 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 615 12 1 7 5.9 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC)c(C#N)c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516227 59917 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 11 1 7 5.8 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc5c(c4)OCO5)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL175341 59917 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 11 1 7 5.8 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc5c(c4)OCO5)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516313 60585 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 602 10 2 6 6.3 CCn1nc(Cc2ccc(O)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL176528 60585 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 602 10 2 6 6.3 CCn1nc(Cc2ccc(O)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
44385583 60950 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 578 9 1 5 6.2 CCn1nc(Cc2ccccc2F)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL177071 60950 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 578 9 1 5 6.2 CCn1nc(Cc2ccccc2F)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516251 96204 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 13 1 6 7.0 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCC(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL265723 96204 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 13 1 6 7.0 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCC(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516205 127684 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 628 11 1 5 7.0 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL366610 127684 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 628 11 1 5 7.0 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516259 128947 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 636 12 1 5 7.7 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(-c5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL367416 128947 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 636 12 1 5 7.7 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(-c5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
44384782 129411 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 589 12 2 6 6.1 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4cccc(NC)c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL367897 129411 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 589 12 2 6 6.1 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4cccc(NC)c4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516248 129502 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 666 14 1 6 7.6 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL368000 129502 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 666 14 1 6 7.6 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516198 131039 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 612 12 1 6 6.2 CCn1nc(Cc2ccc(OC(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL369398 131039 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 612 12 1 6 6.2 CCn1nc(Cc2ccc(OC(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516237 131116 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 628 11 1 5 7.0 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL369478 131116 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 628 11 1 5 7.0 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(C(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516249 131323 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 652 13 1 6 7.8 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(Oc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL369593 131323 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 652 13 1 6 7.8 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(Oc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
3010272 186606 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 517 9 1 5 5.7 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL513564 186606 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 517 9 1 5 5.7 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010272 186606 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 517 9 1 5 5.7 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL513564 186606 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 517 9 1 5 5.7 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
3010272 186606 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 517 9 1 5 5.7 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL513564 186606 1 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 517 9 1 5 5.7 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)s3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
44564930 178498 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 465 8 1 5 5.6 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CCCCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
CHEMBL473759 178498 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assayAntagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
ChEMBL 465 8 1 5 5.6 Cc1nnc(C(C)C)n1C1CCN(C(C)C[C@H](NC(=O)C2CCCCC2)c2ccccc2)CC1 10.1016/j.bmcl.2009.01.008
57391722 70489 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 637 11 0 6 4.4 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cccc(Cl)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
CHEMBL1951917 70489 0 CCR5 CCR5 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 637 11 0 6 4.4 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cccc(Cl)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
44565761 185638 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 554 11 2 4 6.1 CCc1nc(Cc2ccccc2)[nH]c1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
CHEMBL500631 185638 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 554 11 2 4 6.1 CCc1nc(Cc2ccccc2)[nH]c1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
3010275 78072 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 572 11 2 4 6.2 CCc1[nH]c(Cc2ccccc2)nc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2004.04.078
CHEMBL2112558 78072 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 572 11 2 4 6.2 CCc1[nH]c(Cc2ccccc2)nc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2004.04.078
44565761 185638 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 554 11 2 4 6.1 CCc1nc(Cc2ccccc2)[nH]c1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
CHEMBL500631 185638 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 554 11 2 4 6.1 CCc1nc(Cc2ccccc2)[nH]c1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
44565762 178330 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 10 2 4 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL472412 178330 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 10 2 4 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
44511935 68651 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 593 13 1 7 5.8 COCCOc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(Cl)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1926900 68651 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 593 13 1 7 5.8 COCCOc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(Cl)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1649925 56694 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in HeLa-P4 cells co-expressing CD4 assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat10 cells after 20 hrs by cell-cell fusion assay
ChEMBL 479 6 1 6 3.8 COC(=O)N[C@@H](CCN1[C@H]2CC[C@@H]1C[C@H](n1c(C)nc3c1CN(C(C)=O)CC3)C2)c1ccccc1 10.1021/jm100978n
3008904 193552 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonistic activity against human C-C chemokine receptor type 5.Antagonistic activity against human C-C chemokine receptor type 5.
ChEMBL 537 6 0 5 5.0 Cc1cc[n+]([O-])c(C)c1C(=O)N1CCC(C)(N2CCC(N(Cc3cccc(C#N)c3)c3ccccc3)CC2)CC1 10.1021/jm031046g
CHEMBL59511 193552 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonistic activity against human C-C chemokine receptor type 5.Antagonistic activity against human C-C chemokine receptor type 5.
ChEMBL 537 6 0 5 5.0 Cc1cc[n+]([O-])c(C)c1C(=O)N1CCC(C)(N2CCC(N(Cc3cccc(C#N)c3)c3ccccc3)CC2)CC1 10.1021/jm031046g
44401965 70742 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 549 9 1 7 4.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4ccc([N+](=O)[O-])cn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
CHEMBL195753 70742 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranesDisplacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
ChEMBL 549 9 1 7 4.9 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3cnc4ccc([N+](=O)[O-])cn34)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2005.02.030
44565762 178330 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 10 2 4 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL472412 178330 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 10 2 4 6.2 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3008904 193552 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]RANTES from human CCR5 expressed in CHO cellsDisplacement of [125I]RANTES from human CCR5 expressed in CHO cells
ChEMBL 537 6 0 5 5.0 Cc1cc[n+]([O-])c(C)c1C(=O)N1CCC(C)(N2CCC(N(Cc3cccc(C#N)c3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.01.108
CHEMBL59511 193552 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]RANTES from human CCR5 expressed in CHO cellsDisplacement of [125I]RANTES from human CCR5 expressed in CHO cells
ChEMBL 537 6 0 5 5.0 Cc1cc[n+]([O-])c(C)c1C(=O)N1CCC(C)(N2CCC(N(Cc3cccc(C#N)c3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.01.108
58834906 91972 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 604 8 1 6 6.2 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2cccc(Cl)c2)CC1 10.1021/jm401101p
CHEMBL2435853 91972 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 604 8 1 6 6.2 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2cccc(Cl)c2)CC1 10.1021/jm401101p
3010276 78071 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 578 10 2 4 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL2112557 78071 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 578 10 2 4 6.3 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2004.04.078
516337 129396 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assayInhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assay
ChEMBL 596 12 1 5 7.0 CCCn1ncc(CCc2ccccc2)c1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/j.bmcl.2003.12.004
CHEMBL367837 129396 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assayInhibition of human CX3C chemokine receptor 5 from GP120-membrane-based assay
ChEMBL 596 12 1 5 7.0 CCCn1ncc(CCc2ccccc2)c1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/j.bmcl.2003.12.004
516333 119576 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory activity against human CC chemokine receptor 5Inhibitory activity against human CC chemokine receptor 5
ChEMBL 582 11 1 5 6.6 CCn1ncc(CCc2ccccc2)c1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/j.bmcl.2003.12.004
CHEMBL352981 119576 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory activity against human CC chemokine receptor 5Inhibitory activity against human CC chemokine receptor 5
ChEMBL 582 11 1 5 6.6 CCn1ncc(CCc2ccccc2)c1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C3CCCCC3)C[C@@H]2c2ccccc2)CC1 10.1016/j.bmcl.2003.12.004
516293 59161 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 636 10 1 5 7.7 CCn1nc(Cc2ccc(-c3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL172296 59161 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 636 10 1 5 7.7 CCn1nc(Cc2ccc(-c3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516194 59412 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 12 1 6 6.6 CCn1nc(Cc2ccc(OC3CCC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL173254 59412 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 616 12 1 6 6.6 CCn1nc(Cc2ccc(OC3CCC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516280 60519 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 644 10 1 6 6.9 CCn1nc(Cc2ccc(OC(F)(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL176426 60519 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 644 10 1 6 6.9 CCn1nc(Cc2ccc(OC(F)(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516223 60828 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 13 1 6 7.0 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCC(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL176933 60828 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 13 1 6 7.0 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCC(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516199 95828 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 562 10 2 6 5.3 CCn1nc(Cc2ccc(O)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL262663 95828 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 562 10 2 6 5.3 CCn1nc(Cc2ccc(O)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516291 95949 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 602 10 1 5 7.2 CCn1nc(Cc2ccc(C(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL263529 95949 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 602 10 1 5 7.2 CCn1nc(Cc2ccc(C(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516252 129037 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 626 13 1 6 6.6 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL367560 129037 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 626 13 1 6 6.6 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516212 129301 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 13 1 6 6.4 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)[C@@H](C)CC)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1 10.1016/j.bmcl.2003.12.006
CHEMBL367700 129301 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 13 1 6 6.4 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)[C@@H](C)CC)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1 10.1016/j.bmcl.2003.12.006
516209 129931 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 700 13 1 7 6.9 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(S(=O)(=O)c5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL368467 129931 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 700 13 1 7 6.9 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(S(=O)(=O)c5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516290 131144 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 574 9 1 5 6.3 CCn1nc(Cc2ccc(C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL369494 131144 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 574 9 1 5 6.3 CCn1nc(Cc2ccc(C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516250 131347 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 644 12 1 6 6.9 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL369659 131347 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 644 12 1 6 6.9 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OC(F)(F)F)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516253 157386 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 576 11 2 6 5.7 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(O)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL408800 157386 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 576 11 2 6 5.7 CC[C@@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(O)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516196 165256 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 638 12 1 6 7.4 CCn1nc(Cc2ccc(Oc3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL425845 165256 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 638 12 1 6 7.4 CCn1nc(Cc2ccc(Oc3ccccc3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516281 165472 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 11 1 6 7.0 CCn1nc(Cc2ccc(OCC(F)(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL427122 165472 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 658 11 1 6 7.0 CCn1nc(Cc2ccc(OCC(F)(F)F)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
3010261 187493 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 540 9 2 4 5.9 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)[nH]3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL520755 187493 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 540 9 2 4 5.9 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)[nH]3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010261 187493 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 540 9 2 4 5.9 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)[nH]3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL520755 187493 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 540 9 2 4 5.9 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)[nH]3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3010261 187493 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 540 9 2 4 5.9 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)[nH]3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL520755 187493 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 540 9 2 4 5.9 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cnc(Cc4ccccc4)[nH]3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
57403932 70486 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 621 11 0 6 3.9 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cccc(F)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
CHEMBL1951912 70486 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 621 11 0 6 3.9 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cccc(F)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
11614352 524 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxisAntagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxis
ChEMBL 639 11 0 6 4.1 CCN(C(=O)Cc1ccc(cc1)S(=O)(=O)C)C1CCN(CC1)CC[C@@H](c1cc(F)cc(c1)F)C1CCN(CC1)S(=O)(=O)C 10.1016/j.bmcl.2011.12.117
7686 524 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxisAntagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxis
ChEMBL 639 11 0 6 4.1 CCN(C(=O)Cc1ccc(cc1)S(=O)(=O)C)C1CCN(CC1)CC[C@@H](c1cc(F)cc(c1)F)C1CCN(CC1)S(=O)(=O)C 10.1016/j.bmcl.2011.12.117
CHEMBL1951914 524 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxisAntagonist activity at CCR5 in allo T cells assessed as inhibition of MIP-1beta-induced chemotaxis
ChEMBL 639 11 0 6 4.1 CCN(C(=O)Cc1ccc(cc1)S(=O)(=O)C)C1CCN(CC1)CC[C@@H](c1cc(F)cc(c1)F)C1CCN(CC1)S(=O)(=O)C 10.1016/j.bmcl.2011.12.117
57396952 70488 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 655 11 0 6 4.6 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cc(F)cc(Cl)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
CHEMBL1951915 70488 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1alpha from human recombinant CCR5 expressed in CHO cells
ChEMBL 655 11 0 6 4.6 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2cc(F)cc(Cl)c2)C2CCN(S(C)(=O)=O)CC2)CC1 10.1016/j.bmcl.2011.12.117
501056 106748 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 462 10 1 3 5.5 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL318406 106748 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 462 10 1 3 5.5 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
57392303 68642 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 535 10 1 6 5.4 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)ccnc3Cl)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1926891 68642 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 535 10 1 6 5.4 COc1ccc(N(Cc2cnccc2C)C2CCN([C@H](C)CCNC(=O)c3c(C)ccnc3Cl)CC2)cc1 10.1016/j.bmcl.2011.09.133
44512001 68660 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 544 10 1 7 4.8 COc1ccc(N(Cc2cccc(C#N)n2)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(F)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
CHEMBL1927010 68660 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assayAntagonist activity against human CCR5 assessed as inhibition of HIV1 gp120-induced cell-cell fusion between human HeLa P4/R5 cells and CHO-tat10 cells expressing HIV-1JRFL viral envolop protein after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 544 10 1 7 4.8 COc1ccc(N(Cc2cccc(C#N)n2)C2CCN([C@H](C)CCNC(=O)c3c(C)cc(F)nc3C)CC2)cc1 10.1016/j.bmcl.2011.09.133
62706106 81133 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 560 10 1 6 5.2 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)CC2CCOCC2)CC1 10.1021/ml2002604
CHEMBL2164215 81133 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assayAntagonist activity at CCR5 receptor expressed in P4R5 cells co-expressing CD4, and LTR-beta-gal construct assessed as inhibition of infusion to HIV gp120 expressed in CHO-tat cells expressing HIV-1 JRFLenv and HIV-1 Tat by beta-galactosidase activity based cell-cell fusion assay
ChEMBL 560 10 1 6 5.2 Cc1cc(Cl)nc(C)c1C(=O)NCC[C@@H](C)N1CCC(N(Cc2ccsc2)C(=O)CC2CCOCC2)CC1 10.1021/ml2002604
3008917 196366 2 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonistic activity against monkey C-C chemokine receptor type 5.Antagonistic activity against monkey C-C chemokine receptor type 5.
ChEMBL 481 5 0 3 6.6 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(c3ccccc3)c3ccccc3)CC2)CC1 10.1021/jm031046g
CHEMBL62152 196366 2 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Functional
Antagonistic activity against monkey C-C chemokine receptor type 5.Antagonistic activity against monkey C-C chemokine receptor type 5.
ChEMBL 481 5 0 3 6.6 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(c3ccccc3)c3ccccc3)CC2)CC1 10.1021/jm031046g
501056 106748 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 462 10 1 3 5.5 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL318406 106748 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 462 10 1 3 5.5 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
3008917 196366 2 CCR5 CCR5 Crab-eating macaque 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled MIP-1alpha from cynomolgus monkey CCR5 expressed in CHO cellsDisplacement of radiolabeled MIP-1alpha from cynomolgus monkey CCR5 expressed in CHO cells
ChEMBL 481 5 0 3 6.6 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.01.108
CHEMBL62152 196366 2 CCR5 CCR5 Crab-eating macaque 9.2 pIC50 = 9.2 Binding
Displacement of radiolabeled MIP-1alpha from cynomolgus monkey CCR5 expressed in CHO cellsDisplacement of radiolabeled MIP-1alpha from cynomolgus monkey CCR5 expressed in CHO cells
ChEMBL 481 5 0 3 6.6 Cc1cccc(C)c1C(=O)N1CCC(C)(N2CCC(N(c3ccccc3)c3ccccc3)CC2)CC1 10.1016/j.bmcl.2008.01.108
501056 106748 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 462 10 1 3 5.5 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
CHEMBL318406 106748 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.In vitro binding affinity at CCR5 receptor in the presence of [125I]-MIP-1 alpha.
ChEMBL 462 10 1 3 5.5 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/s0960-894x(02)00606-6
58835217 91975 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 584 9 1 6 5.8 CCc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
CHEMBL2435856 91975 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assayInhibition of CCR5 (unknown origin) expressed in human HeLa cells assessed as inhibition of interaction of CHO cells expressing HIV-1 JRFLenv and HIV-1 Tat and human HeLa cells expressing CD4 after 20 hrs by beta-galactosidase reporter gene assay
ChEMBL 584 9 1 6 5.8 CCc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
44415755 137906 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]MIP-1beta binding to CCR5 expressed in HEK293 cellsInhibition of [125I]MIP-1beta binding to CCR5 expressed in HEK293 cells
ChEMBL 451 9 2 3 4.0 O=C(Cc1ccc(F)cc1)NC1CCN(CC[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2006.06.012
CHEMBL377914 137906 0 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]MIP-1beta binding to CCR5 expressed in HEK293 cellsInhibition of [125I]MIP-1beta binding to CCR5 expressed in HEK293 cells
ChEMBL 451 9 2 3 4.0 O=C(Cc1ccc(F)cc1)NC1CCN(CC[C@H](NC(=O)C2CCC2)c2ccccc2)CC1 10.1016/j.bmcl.2006.06.012
3010279 78066 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 564 10 2 4 5.9 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL2112552 78066 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 564 10 2 4 5.9 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3[nH]c(Cc4ccccc4)nc3Cl)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2004.04.078
516285 59169 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 9 1 7 5.8 CCn1nc(Cc2ccc3c(c2)OCO3)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL172322 59169 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 604 9 1 7 5.8 CCn1nc(Cc2ccc3c(c2)OCO3)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516229 59425 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 13 1 6 6.6 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)[C@@H](C)CC)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
CHEMBL173308 59425 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 13 1 6 6.6 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)[C@@H](C)CC)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
516308 59924 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 644 13 1 6 7.4 CCCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C5CCCCC5)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1 10.1016/j.bmcl.2003.12.006
CHEMBL175394 59924 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 644 13 1 6 7.4 CCCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C5CCCCC5)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1 10.1016/j.bmcl.2003.12.006
516275 60883 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 630 11 1 6 7.0 CCn1nc(Cc2ccc(OC3CCC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL177033 60883 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 630 11 1 6 7.0 CCn1nc(Cc2ccc(OC3CCC3)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516220 61572 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 666 14 1 6 7.6 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
CHEMBL177648 61572 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 666 14 1 6 7.6 CC[C@H](C)[C@H](C(=O)O)N1C[C@H](CN2CCC(c3cc(Cc4ccc(OCc5ccccc5)cc4)nn3CC)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.bmcl.2003.12.006
516287 119232 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 11 1 6 6.6 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
CHEMBL349974 119232 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 622 11 1 6 6.6 CCOc1ccc(Cc2cc(C3CCN(C[C@H]4CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]4c4cccc(F)c4)CC3)n(CC)n2)cc1F 10.1016/j.bmcl.2003.12.006
516276 129878 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 618 11 1 6 6.8 CCn1nc(Cc2ccc(OC(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL368204 129878 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 618 11 1 6 6.8 CCn1nc(Cc2ccc(OC(C)C)cc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
516269 167706 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 590 10 1 6 6.0 CCn1nc(Cc2cccc(OC)c2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
CHEMBL435554 167706 1 CCR5 CCR5 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cellInhibitory concentration for displacement of [125I]-MIP-1 alpha from recombinant human CC chemokine receptor 5 (CCR5) expressed in CHO cell
ChEMBL 590 10 1 6 6.0 CCn1nc(Cc2cccc(OC)c2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2003.12.006
3010267 78074 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 512 10 2 4 5.1 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3c[nH]c(Cc4ccccc4)n3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
CHEMBL2112560 78074 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 512 10 2 4 5.1 O=C(O)[C@@H](CC1CC1)N1C[C@H](CN2CCC(c3c[nH]c(Cc4ccccc4)n3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.bmcl.2004.04.078
44461741 167219 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]-MIP-1 alpha binding to human CCR5 receptor expressed in Chinese hamster ovary (CHO) cellsInhibition of [125I]-MIP-1 alpha binding to human CCR5 receptor expressed in Chinese hamster ovary (CHO) cells
ChEMBL 619 14 1 6 5.3 C=CCN(C(=O)NCc1ccc([N+](=O)[O-])cc1)C1CCN(CC[C@@H](CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(01)00492-9
CHEMBL432360 167219 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]-MIP-1 alpha binding to human CCR5 receptor expressed in Chinese hamster ovary (CHO) cellsInhibition of [125I]-MIP-1 alpha binding to human CCR5 receptor expressed in Chinese hamster ovary (CHO) cells
ChEMBL 619 14 1 6 5.3 C=CCN(C(=O)NCc1ccc([N+](=O)[O-])cc1)C1CCN(CC[C@@H](CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(01)00492-9
76330829 84949 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at Homo sapiens (human) CCR5 receptorAntagonist activity at Homo sapiens (human) CCR5 receptor
ChEMBL 605 13 1 6 5.6 C=CCN(C(=O)Nc1ccc([N+](=O)[O-])cc1)C1CCN(CCC(CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1007/s00044-012-0138-3
CHEMBL2282506 84949 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at Homo sapiens (human) CCR5 receptorAntagonist activity at Homo sapiens (human) CCR5 receptor
ChEMBL 605 13 1 6 5.6 C=CCN(C(=O)Nc1ccc([N+](=O)[O-])cc1)C1CCN(CCC(CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1007/s00044-012-0138-3
16073660 79132 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cells
ChEMBL 596 11 0 6 4.6 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2ccccc2)c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2006.03.089
CHEMBL211866 79132 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cellsDisplacement of [125I]MIP-1-alpha to human recombinant CCR5 expressed in CHO cells
ChEMBL 596 11 0 6 4.6 CCN(C(=O)Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CC[C@@H](c2ccccc2)c2ccc(S(C)(=O)=O)cc2)CC1 10.1016/j.bmcl.2006.03.089
44565853 178169 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 571 11 1 5 6.8 CCc1nc(Cc2ccccc2)sc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
CHEMBL471251 178169 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 571 11 1 5 6.8 CCc1nc(Cc2ccccc2)sc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
3010278 78067 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 589 11 1 5 7.0 CCc1nc(Cc2ccccc2)sc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2004.04.078
CHEMBL2112553 78067 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Inhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligandInhibition of human C-C chemokine receptor type 5 assayed using [125I]-MIP-1 alpha as radioligand
ChEMBL 589 11 1 5 7.0 CCc1nc(Cc2ccccc2)sc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.bmcl.2004.04.078
44565853 178169 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 571 11 1 5 6.8 CCc1nc(Cc2ccccc2)sc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
CHEMBL471251 178169 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 571 11 1 5 6.8 CCc1nc(Cc2ccccc2)sc1C1CCN(C[C@H]2CN([C@H](CC3CCC3)C(=O)O)C[C@@H]2c2ccccc2)CC1 10.1016/j.ejmech.2008.01.040
76327166 84952 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at Homo sapiens (human) CCR5 receptorAntagonist activity at Homo sapiens (human) CCR5 receptor
ChEMBL 620 14 1 6 5.1 CCCN(C(=O)OCc1cccc(C(N)=O)c1)C1CCN(CC[C@H](CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1007/s00044-012-0138-3
CHEMBL2282509 84952 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Antagonist activity at Homo sapiens (human) CCR5 receptorAntagonist activity at Homo sapiens (human) CCR5 receptor
ChEMBL 620 14 1 6 5.1 CCCN(C(=O)OCc1cccc(C(N)=O)c1)C1CCN(CC[C@H](CN(C)S(=O)(=O)c2ccccc2)c2ccccc2)CC1 10.1007/s00044-012-0138-3
501051 4238 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 512 10 2 4 5.4 O=C(O)[C@@H](c1ccccc1)N1C[C@H](CN2CCC(O)(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL101961 4238 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 512 10 2 4 5.4 O=C(O)[C@@H](c1ccccc1)N1C[C@H](CN2CCC(O)(CCCc3ccccc3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
516260 59305 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 9 1 5 6.0 CCn1nc(Cc2ccccc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.ejmech.2008.01.040
CHEMBL172854 59305 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 560 9 1 5 6.0 CCn1nc(Cc2ccccc2)cc1C1CCN(C[C@H]2CN([C@@H](C(=O)O)C(C)(C)C)C[C@@H]2c2cccc(F)c2)CC1 10.1016/j.ejmech.2008.01.040
44273960 98525 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 524 11 1 3 6.4 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL281607 98525 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 524 11 1 3 6.4 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
44565719 178253 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 530 11 1 4 6.4 CC(C)C[C@H](C(=O)O)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL471909 178253 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 530 11 1 4 6.4 CC(C)C[C@H](C(=O)O)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/j.ejmech.2008.01.040
516342 186398 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 541 9 1 5 6.2 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cc(Cc4ccccc4)no3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
CHEMBL511634 186398 1 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]MIP1alpha from human CCR5 expressed in CHO cellsDisplacement of [125I]MIP1alpha from human CCR5 expressed in CHO cells
ChEMBL 541 9 1 5 6.2 O=C(O)[C@@H](C1CCCCC1)N1C[C@H](CN2CCC(c3cc(Cc4ccccc4)no3)CC2)[C@@H](c2ccccc2)C1 10.1016/j.ejmech.2008.01.040
44274108 98454 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 516 10 1 4 6.0 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL281176 98454 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 516 10 1 4 6.0 CC(C)[C@H](C(=O)O)N1C[C@H](CN2CCC(CCSc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
44273960 98525 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 524 11 1 3 6.4 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
CHEMBL281607 98525 0 CCR5 CCR5 Human 9.1 pIC50 = 9.1 Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membraneAbility to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL 524 11 1 3 6.4 O=C(O)[C@@H](CC1CCC1)N1C[C@H](CN2CCC(CCCc3ccc(F)cc3)CC2)[C@@H](c2cccc(F)c2)C1 10.1016/s0960-894x(02)00829-6
490022 110865 1 CCR5 CCR5 Human 9.1