Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

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 DOI
9827294 73865 3 None - 1 Human 8.0 pEC50 = 8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL2018953 73865 3 None - 1 Human 8.0 pEC50 = 8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.ejmech.2016.02.058
127046612 139750 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3798452 139750 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127046614 139926 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799578 139926 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
127047356 139634 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 139634 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
44288958 168727 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL43698 168727 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
127047440 139607 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 542 7 2 8 4.4 COc1cc2nc(N3CCC(N(C)C(=O)[C@H]4CCCN4)CC3)nc(Nc3ccc(Cl)cc3F)c2cc1OC 10.1016/j.ejmech.2016.02.058
CHEMBL3797462 139607 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 542 7 2 8 4.4 COc1cc2nc(N3CCC(N(C)C(=O)[C@H]4CCCN4)CC3)nc(Nc3ccc(Cl)cc3F)c2cc1OC 10.1016/j.ejmech.2016.02.058
127047612 139892 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799393 139892 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
44288959 165307 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42334 165307 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
10238794 162835 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 473 7 2 6 4.3 O=S(=O)(Nc1ncc(Cl)nc1OCc1ccccc1CO)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172769 162835 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 473 7 2 6 4.3 O=S(=O)(Nc1ncc(Cl)nc1OCc1ccccc1CO)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10195057 162497 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 444 6 1 6 4.2 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4167445 162497 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 444 6 1 6 4.2 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
23585443 542 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 542 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 542 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
145959198 162173 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 369 4 1 5 2.9 COc1nc(F)c(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4162364 162173 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 369 4 1 5 2.9 COc1nc(F)c(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10308720 545 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 545 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 545 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
10309893 162688 2 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4170431 162688 2 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
11525206 135228 0 None - 1 Human 8.0 pIC50 = 8 Functional
Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPRCalcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL372399 135228 0 None - 1 Human 8.0 pIC50 = 8 Functional
Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPRCalcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44581043 187834 0 None 1 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496152 187834 0 None 1 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581068 187924 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496787 187924 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
25212472 192646 0 None -2 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL521737 192646 0 None -2 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
59456023 87156 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 516 8 2 7 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)=O)cccc32)c1 10.1021/jm301572h
CHEMBL2326612 87156 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 516 8 2 7 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)=O)cccc32)c1 10.1021/jm301572h
59456042 87158 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 532 8 3 7 4.5 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)(C)O)cccc32)c1 10.1021/jm301572h
CHEMBL2326614 87158 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 532 8 3 7 4.5 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)(C)O)cccc32)c1 10.1021/jm301572h
59456012 87159 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
CHEMBL2326615 87159 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
71584536 87173 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccnc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326628 87173 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccnc(CNC(C)=O)c1 10.1021/jm301572h
59168189 162427 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1 10.1021/acsmedchemlett.7b00315
CHEMBL4166246 162427 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1 10.1021/acsmedchemlett.7b00315
118706823 112976 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 5 2 5 4.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(C)C 10.1016/j.bmc.2014.05.021
CHEMBL3310832 112976 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 5 2 5 4.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(C)C 10.1016/j.bmc.2014.05.021
10309983 162113 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 417 4 1 6 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4161268 162113 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 417 4 1 6 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.7b00315
145949792 162706 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 425 5 1 6 3.8 COc1nc(Br)cnc1NS(=O)(=O)c1sccc1-c1ccccc1 10.1021/acsmedchemlett.7b00315
CHEMBL4170786 162706 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 425 5 1 6 3.8 COc1nc(Br)cnc1NS(=O)(=O)c1sccc1-c1ccccc1 10.1021/acsmedchemlett.7b00315
137642528 158264 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1ccc2c(cnn2C)c1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
CHEMBL4088688 158264 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1ccc2c(cnn2C)c1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
137659242 159167 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 458 6 2 9 2.3 COc1nn(C)c2nc(NC3COC3)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4098333 159167 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 458 6 2 9 2.3 COc1nn(C)c2nc(NC3COC3)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
145955299 162589 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 368 4 1 6 2.6 COc1nc(Cl)cnc1NS(=O)(=O)c1ccnc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4168920 162589 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 368 4 1 6 2.6 COc1nc(Cl)cnc1NS(=O)(=O)c1ccnc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
155520262 170468 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 578 7 0 8 5.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(C)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4448901 170468 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 578 7 0 8 5.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(C)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
71461546 84341 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 640 11 2 5 6.3 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmc.2012.03.069
CHEMBL2216810 84341 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 640 11 2 5 6.3 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmc.2012.03.069
25141301 185888 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 185888 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 185888 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL486840 185888 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
118706824 112977 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 443 5 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1COC1 10.1016/j.bmc.2014.05.021
CHEMBL3310833 112977 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 443 5 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1COC1 10.1016/j.bmc.2014.05.021
59456067 73881 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018968 73881 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
136116031 86802 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
CHEMBL2321924 86802 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
59456019 87175 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326630 87175 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
10195081 162160 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 445 6 1 7 3.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cncnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4162097 162160 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 445 6 1 7 3.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cncnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10309206 162406 5 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4165939 162406 5 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
59168214 163037 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 6 1 6 3.0 CCOc1cnc(NS(=O)(=O)c2cccc(Cl)c2Cl)c(OC)n1 10.1021/acsmedchemlett.7b00315
CHEMBL4175972 163037 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 6 1 6 3.0 CCOc1cnc(NS(=O)(=O)c2cccc(Cl)c2Cl)c(OC)n1 10.1021/acsmedchemlett.7b00315
134210781 178208 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(C4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4649666 178208 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(C4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
71584537 87174 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)n1 10.1021/jm301572h
CHEMBL2326629 87174 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)n1 10.1021/jm301572h
10150948 161975 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4159115 161975 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1Cl 10.1021/acsmedchemlett.7b00315
10287210 163091 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.7b00315
CHEMBL4176859 163091 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.7b00315
137652824 158761 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 357 3 1 6 2.5 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
CHEMBL4093994 158761 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 357 3 1 6 2.5 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
10126022 162774 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1ccsc1 10.1021/acsmedchemlett.7b00315
CHEMBL4171873 162774 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1ccsc1 10.1021/acsmedchemlett.7b00315
137632634 156392 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 356 3 1 5 3.1 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ccnc21 10.1016/j.bmc.2017.07.052
CHEMBL4066451 156392 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 356 3 1 5 3.1 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ccnc21 10.1016/j.bmc.2017.07.052
155543648 173193 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn(C(C)c2ccc(Cl)cc2Cl)c2nc(N3CCC(N4CCCCC4)C(C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4522547 173193 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn(C(C)c2ccc(Cl)cc2Cl)c2nc(N3CCC(N4CCCCC4)C(C)C3)cnc12 10.1021/acs.jmedchem.9b00506
70685474 73878 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 518 8 1 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN(C)C(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018965 73878 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 518 8 1 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN(C)C(C)=O)c1 10.1016/j.bmcl.2012.02.104
44561334 176223 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
CHEMBL459464 176223 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
44561260 189044 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 384 6 2 6 5.1 COc1cc2nc(NC3CCCC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL509396 189044 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 384 6 2 6 5.1 COc1cc2nc(NC3CCCC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44562238 186755 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 524 8 1 8 5.0 COc1cc2nc(N3CCCN(CCN4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488855 186755 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 524 8 1 8 5.0 COc1cc2nc(N3CCCN(CCN4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 185888 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 185888 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 186437 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 186437 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 185888 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL486840 185888 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
16724339 186437 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL487635 186437 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
156013953 177207 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 418 5 0 6 4.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(CN(C)C)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4635359 177207 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 418 5 0 6 4.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(CN(C)C)C3)cnc12 10.1021/acs.jmedchem.0c00988
10416 1879 30 None 309 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
46861584 1879 30 None 309 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
CHEMBL2018969 1879 30 None 309 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
44288958 168727 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmc.2012.03.069
CHEMBL43698 168727 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmc.2012.03.069
25141190 1146 28 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
9478 1146 28 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
CHEMBL508207 1146 28 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
44581102 187772 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495736 187772 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
156017568 177821 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 494 5 0 8 4.3 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4643839 177821 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 494 5 0 8 4.3 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
59455988 87165 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
CHEMBL2326620 87165 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
59456014 87166 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
CHEMBL2326621 87166 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
59456103 87167 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
CHEMBL2326622 87167 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
58054368 87169 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326624 87169 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
59456058 87178 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326633 87178 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
56849395 87190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326926 87190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
10308720 545 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 545 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 545 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
10308963 162185 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(F)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4162555 162185 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(F)c1Cl 10.1021/acsmedchemlett.7b00315
145951541 162710 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 409 6 1 5 4.3 CC(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4170833 162710 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 409 6 1 5 4.3 CC(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44562237 186728 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 510 8 1 8 4.7 COc1cc2nc(N3CCCN(CCN4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488691 186728 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 510 8 1 8 4.7 COc1cc2nc(N3CCCN(CCN4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
71525425 132812 0 None -446 5 Human 5.8 pIC50 = 5.8 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 509 8 3 9 2.7 Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
CHEMBL3701196 132812 0 None -446 5 Human 5.8 pIC50 = 5.8 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 509 8 3 9 2.7 Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
59455992 73869 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018957 73869 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
23585443 542 12 None -16 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 542 12 None -16 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 542 12 None -16 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
71584535 87172 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cc(CNC(C)=O)ccn1 10.1021/jm301572h
CHEMBL2326627 87172 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cc(CNC(C)=O)ccn1 10.1021/jm301572h
137633709 156619 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 373 4 2 6 2.5 COc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4069103 156619 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 373 4 2 6 2.5 COc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
145955692 162495 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4167390 162495 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1Cl 10.1021/acsmedchemlett.7b00315
145971718 163068 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 453 7 1 5 4.5 CCCCOc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4176441 163068 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 453 7 1 5 4.5 CCCCOc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
118706827 112980 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 461 7 4 7 2.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(CO)CO 10.1016/j.bmc.2014.05.021
CHEMBL3310836 112980 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 461 7 4 7 2.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(CO)CO 10.1016/j.bmc.2014.05.021
137643503 158408 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 3 3 6 2.2 O=S(=O)(Nc1ncnc2[nH]nc(O)c12)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
CHEMBL4090166 158408 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 3 3 6 2.2 O=S(=O)(Nc1ncnc2[nH]nc(O)c12)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
155561858 175755 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4583503 175755 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134325276 175475 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4577319 175475 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134211225 177925 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4645325 177925 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
25141190 1146 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
9478 1146 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
CHEMBL508207 1146 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
25141190 1146 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
9478 1146 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
CHEMBL508207 1146 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
44561294 172980 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 481 7 1 7 5.6 COc1cc2nc(N3CCC(N(C)C4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL451783 172980 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 481 7 1 7 5.6 COc1cc2nc(N3CCC(N(C)C4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44581121 188263 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 553 10 2 8 5.0 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL499852 188263 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 553 10 2 8 5.0 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
16724339 186437 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 186437 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 186437 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL487635 186437 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
25212379 187862 1 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496356 187862 1 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
16724339 186437 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL487635 186437 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
25212472 192646 0 None 2 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL521737 192646 0 None 2 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
59455975 87157 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
CHEMBL2326613 87157 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
71583488 87160 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
CHEMBL2326616 87160 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
11244702 162333 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 339 4 1 6 2.7 COc1nccnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4164738 162333 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 339 4 1 6 2.7 COc1nccnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
59168158 162551 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C 10.1021/acsmedchemlett.7b00315
CHEMBL4168237 162551 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C 10.1021/acsmedchemlett.7b00315
10215932 73127 1 None -22 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR4 in human primary Th2 cells by chemotaxis assayAntagonist activity at CCR4 in human primary Th2 cells by chemotaxis assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL2011441 73127 1 None -22 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR4 in human primary Th2 cells by chemotaxis assayAntagonist activity at CCR4 in human primary Th2 cells by chemotaxis assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
118706818 112972 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C 10.1016/j.bmc.2014.05.021
CHEMBL3310827 112972 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C 10.1016/j.bmc.2014.05.021
118706829 112982 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 484 5 2 6 2.8 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CN(C(C)=O)C1 10.1016/j.bmc.2014.05.021
CHEMBL3310838 112982 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 484 5 2 6 2.8 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CN(C(C)=O)C1 10.1016/j.bmc.2014.05.021
137643926 158225 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 6 2 8 2.0 COc1nn(CC(=O)O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4088207 158225 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 6 2 8 2.0 COc1nn(CC(=O)O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
10194488 162178 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1021/acsmedchemlett.7b00315
CHEMBL4162503 162178 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1021/acsmedchemlett.7b00315
10194274 162383 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 1 6 3.2 CCOc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4165500 162383 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 1 6 3.2 CCOc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
118706820 112974 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 415 4 1 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)n(C)c(=O)n2C 10.1016/j.bmc.2014.05.021
CHEMBL3310829 112974 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 415 4 1 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)n(C)c(=O)n2C 10.1016/j.bmc.2014.05.021
118706826 112979 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 458 7 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CCN(C)C 10.1016/j.bmc.2014.05.021
CHEMBL3310835 112979 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 458 7 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CCN(C)C 10.1016/j.bmc.2014.05.021
137661320 159081 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2ccccc21 10.1016/j.bmc.2017.07.052
CHEMBL4097341 159081 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2ccccc21 10.1016/j.bmc.2017.07.052
118706819 112973 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2[nH]c(=O)n(C)c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310828 112973 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2[nH]c(=O)n(C)c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
23585443 542 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 542 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 542 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59168181 162046 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 391 5 1 5 3.3 C#CCOc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160218 162046 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 391 5 1 5 3.3 C#CCOc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
16724339 186437 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 186437 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 186437 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL487635 186437 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
44561335 176225 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 393 4 1 5 4.8 c1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
CHEMBL459465 176225 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 393 4 1 5 4.8 c1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
44561588 194553 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL529664 194553 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
134210933 177506 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639600 177506 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134225255 177325 10 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 177325 10 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134211098 178044 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647117 178044 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
58054516 73871 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
CHEMBL2018959 73871 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
44562156 186729 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488704 186729 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
44561217 189116 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL510375 189116 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
134324821 171102 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.5 CC1CN(c2cnc3c(C(N)=O)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4457732 171102 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.5 CC1CN(c2cnc3c(C(N)=O)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
134324770 170943 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
CHEMBL4455432 170943 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
134225247 177663 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641595 177663 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
134325106 171251 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4460062 171251 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
25212379 187862 1 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496356 187862 1 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581044 193448 0 None -3 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
CHEMBL526474 193448 0 None -3 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
134325169 172409 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 CC1CN(c2cnc3cnn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4476671 172409 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 CC1CN(c2cnc3cnn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
134211185 177153 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4634054 177153 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
25141301 185888 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 185888 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 185888 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL486840 185888 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
156010350 177082 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633133 177082 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44562155 186631 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488018 186631 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
102143549 112983 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310839 112983 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054475 87168 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326623 87168 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
58597374 162580 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 363 5 2 6 2.1 COc1nc(CO)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4168775 162580 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 363 5 2 6 2.1 COc1nc(CO)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
134335265 174976 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 497 4 0 7 5.3 CC1CN(c2cnc3c(C#N)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4566241 174976 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 497 4 0 7 5.3 CC1CN(c2cnc3c(C#N)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
71583704 87171 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 9 2 8 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC2COC2)c1 10.1021/jm301572h
CHEMBL2326626 87171 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 9 2 8 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC2COC2)c1 10.1021/jm301572h
71583039 87191 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 6 4.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3ccccc32)c1 10.1021/jm301572h
CHEMBL2326927 87191 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 6 4.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3ccccc32)c1 10.1021/jm301572h
137647817 157557 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 429 5 1 8 2.5 COc1nn(C2COC2)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4080352 157557 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 429 5 1 8 2.5 COc1nn(C2COC2)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137653647 159044 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 2.9 CCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4096860 159044 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 2.9 CCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
137661613 159222 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 415 5 1 7 3.5 COc1nn(C(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4098813 159222 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 415 5 1 7 3.5 COc1nn(C(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
155518637 170322 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.2 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(N3CCC(N4CCCCC4)CC3)nc21 10.1021/acs.jmedchem.9b00506
CHEMBL4446924 170322 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.2 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(N3CCC(N4CCCCC4)CC3)nc21 10.1021/acs.jmedchem.9b00506
44561137 186719 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL488640 186719 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
134325016 174653 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
CHEMBL4558456 174653 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
59456051 73880 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018967 73880 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
142450222 169674 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 484 4 1 6 4.5 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(C3=CCN(C(=O)[C@H]4CCCCN4)CC3)nc21 10.1021/acs.jmedchem.9b00506
CHEMBL4437594 169674 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 484 4 1 6 4.5 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(C3=CCN(C(=O)[C@H]4CCCCN4)CC3)nc21 10.1021/acs.jmedchem.9b00506
156010372 177108 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4633494 177108 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44562191 186756 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488857 186756 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
58834906 92644 0 None -467 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
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 92644 0 None -467 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
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
134210845 178049 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647188 178049 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44430312 87260 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL233046 87260 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
9959269 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
CHEMBL2018954 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
9959269 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
CHEMBL2018954 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
9959269 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2017.07.052
9959269 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
CHEMBL2018954 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2017.07.052
CHEMBL2018954 73866 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
23585443 542 12 None -16 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 542 12 None -16 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 542 12 None -16 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59168106 162084 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 2 6 2.7 COc1nc(CO)c(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160846 162084 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 2 6 2.7 COc1nc(CO)c(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
23585446 162856 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1ncc(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4173046 162856 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1ncc(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
59168165 162991 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 521 6 1 5 5.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccc(Br)c1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4175323 162991 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 521 6 1 5 5.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccc(Br)c1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
25212472 192646 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL521737 192646 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
134210626 177305 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4636749 177305 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44562189 186575 0 None 7 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487835 186575 0 None 7 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44561333 189878 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2c1 10.1016/j.bmc.2008.05.036
CHEMBL516936 189878 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2c1 10.1016/j.bmc.2008.05.036
10308720 545 42 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 545 42 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 545 42 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59456102 73877 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018964 73877 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
59456102 73877 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2018964 73877 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
58054384 87151 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
CHEMBL2326608 87151 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
71583489 87161 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCO2)c1 10.1021/jm301572h
CHEMBL2326617 87161 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCO2)c1 10.1021/jm301572h
59456010 87163 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
CHEMBL2326619 87163 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
118706817 112971 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310826 112971 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
23585443 542 12 None -16 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 542 12 None -16 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 542 12 None -16 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59456021 87154 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 7 2 7 4.1 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C#N)cccc32)c1 10.1021/jm301572h
CHEMBL2326610 87154 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 7 2 7 4.1 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C#N)cccc32)c1 10.1021/jm301572h
137632888 156533 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.6 COCCn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
CHEMBL4068045 156533 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.6 COCCn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
137644457 158315 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 402 4 2 8 2.1 COc1nn(C)c2nc(N)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4089151 158315 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 402 4 2 8 2.1 COc1nn(C)c2nc(N)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137632974 156347 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 3.3 COc1nn(C)c2nc(NC(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4065904 156347 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 3.3 COc1nn(C)c2nc(NC(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137652382 157394 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)cccc21 10.1016/j.bmc.2017.07.052
CHEMBL4078359 157394 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)cccc21 10.1016/j.bmc.2017.07.052
10173173 162247 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)ccc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4163571 162247 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)ccc1Cl 10.1021/acsmedchemlett.7b00315
145950145 162881 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 279 6 1 5 1.7 CCCCS(=O)(=O)Nc1ncc(Cl)nc1OC 10.1021/acsmedchemlett.7b00315
CHEMBL4173424 162881 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 279 6 1 5 1.7 CCCCS(=O)(=O)Nc1ncc(Cl)nc1OC 10.1021/acsmedchemlett.7b00315
145950218 162965 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 399 4 1 6 3.5 CSc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4174872 162965 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 399 4 1 6 3.5 CSc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
134325076 172185 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4473604 172185 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134325041 175032 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4567398 175032 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44561172 173710 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 485 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCC(F)CC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL453594 173710 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 485 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCC(F)CC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
70685473 73863 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018951 73863 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
44562189 186575 0 None 7 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487835 186575 0 None 7 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
70681287 73873 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
CHEMBL2018960 73873 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
134335394 172342 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
CHEMBL4475665 172342 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
156018849 177907 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4645037 177907 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134335393 170112 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4443688 170112 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44562192 185777 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486656 185777 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
134211221 177688 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4641873 177688 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
134325003 175382 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4575089 175382 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
156015374 177615 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4640909 177615 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
16041411 92576 0 None -4168 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 572 8 1 6 5.6 O=C(O)c1ccc(Sc2ccc(CN3CCC(N4C(=O)N(C5CCOCC5)C[C@H]4c4ccccc4)CC3)cn2)cc1 10.1021/jm401101p
CHEMBL2434978 92576 0 None -4168 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 572 8 1 6 5.6 O=C(O)c1ccc(Sc2ccc(CN3CCC(N4C(=O)N(C5CCOCC5)C[C@H]4c4ccccc4)CC3)cn2)cc1 10.1021/jm401101p
11525206 135228 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of chemotaxis of murine CCR4 transfected L1.2 cellsInhibition of chemotaxis of murine CCR4 transfected L1.2 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL372399 135228 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of chemotaxis of murine CCR4 transfected L1.2 cellsInhibition of chemotaxis of murine CCR4 transfected L1.2 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
155557193 174525 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
CHEMBL4555534 174525 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
70689680 73867 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018955 73867 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
25141190 1146 28 None 1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
9478 1146 28 None 1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
CHEMBL508207 1146 28 None 1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
10416 1879 30 None 309 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
46861584 1879 30 None 309 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
CHEMBL2018969 1879 30 None 309 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
59456111 87162 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
CHEMBL2326618 87162 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
59456026 87176 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326631 87176 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59455990 87177 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326632 87177 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
10288569 162040 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 461 4 1 6 3.5 COc1nc(Br)cnc1NS(=O)(=O)c1sc(Cl)cc1Br 10.1021/acsmedchemlett.7b00315
CHEMBL4160139 162040 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 461 4 1 6 3.5 COc1nc(Br)cnc1NS(=O)(=O)c1sc(Cl)cc1Br 10.1021/acsmedchemlett.7b00315
10287192 162056 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 5 2 6 2.4 COc1nc(CO)c(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160463 162056 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 5 2 6 2.4 COc1nc(CO)c(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10193586 162822 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(C)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172568 162822 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(C)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44581103 187773 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495737 187773 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
118706828 112981 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 442 5 3 6 2.6 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CNC1 10.1016/j.bmc.2014.05.021
CHEMBL3310837 112981 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 442 5 3 6 2.6 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CNC1 10.1016/j.bmc.2014.05.021
56848673 87187 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)c(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326923 87187 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)c(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
56848670 87189 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326925 87189 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
118706825 112978 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 6 2 5 3.9 CCCn1c(=O)[nH]c2cc(NS(=O)(=O)c3cccc(Cl)c3Cl)c(OC)cc21 10.1016/j.bmc.2014.05.021
CHEMBL3310834 112978 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 6 2 5 3.9 CCCn1c(=O)[nH]c2cc(NS(=O)(=O)c3cccc(Cl)c3Cl)c(OC)cc21 10.1016/j.bmc.2014.05.021
137656805 159726 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 7 1 8 2.5 COc1nn(CCN(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4104585 159726 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 7 1 8 2.5 COc1nn(CCN(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
10417 1069 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
134324842 1069 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
CHEMBL4459231 1069 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
155541406 172995 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4518040 172995 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
58054487 73876 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018963 73876 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
134211126 177569 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4640439 177569 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
155531126 171607 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4465359 171607 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44581043 187834 0 None -1 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496152 187834 0 None -1 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44562191 186756 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488857 186756 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44581042 187833 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496151 187833 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581102 187772 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495736 187772 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
71555361 133324 0 None -234 5 Human 6.4 pIC50 = 6.4 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 564 8 3 10 2.4 Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
CHEMBL3704573 133324 0 None -234 5 Human 6.4 pIC50 = 6.4 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 564 8 3 10 2.4 Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
134210778 177702 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4642090 177702 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
118706821 112975 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 444 6 3 6 1.9 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CC(N)=O 10.1016/j.bmc.2014.05.021
CHEMBL3310830 112975 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 444 6 3 6 1.9 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CC(N)=O 10.1016/j.bmc.2014.05.021
134336138 177495 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639418 177495 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134324973 170387 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4447900 170387 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
70693879 73421 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2016602 73421 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
44581042 187833 0 None 6 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496151 187833 0 None 6 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44561561 179001 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL470962 179001 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
10215932 73127 1 None 22 2 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL2011441 73127 1 None 22 2 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
9827294 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
CHEMBL2018953 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
9827294 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
CHEMBL2018953 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
9827294 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2017.07.052
9827294 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
CHEMBL2018953 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2017.07.052
CHEMBL2018953 73865 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
118706831 112985 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310841 112985 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
56848674 87188 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 542 9 3 7 3.9 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326924 87188 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 542 9 3 7 3.9 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59168115 162296 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1ncc(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4164247 162296 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1ncc(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44430315 11866 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL1182360 11866 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233047 11866 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
11223594 71084 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195298 71084 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
10308720 545 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 545 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 545 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
10308720 545 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 545 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 545 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
137638825 156870 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 1.4 COc1nn(CC(N)=O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4071815 156870 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 1.4 COc1nn(CC(N)=O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
59168213 162151 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 5 1 7 2.0 COc1nc(S(C)(=O)=O)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4161922 162151 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 5 1 7 2.0 COc1nc(S(C)(=O)=O)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
145955410 162397 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 381 4 1 5 3.3 CCc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4165828 162397 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 381 4 1 5 3.3 CCc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
10309892 162466 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1021/acsmedchemlett.7b00315
CHEMBL4167021 162466 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1021/acsmedchemlett.7b00315
156018931 177869 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 540 6 0 6 6.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4644412 177869 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 540 6 0 6 6.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44581043 187834 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496152 187834 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44561363 189684 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 466 6 1 6 6.3 COc1cc2nc(C3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL515355 189684 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 466 6 1 6 6.3 COc1cc2nc(C3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44581044 193448 0 None 3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
CHEMBL526474 193448 0 None 3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
11496063 77119 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
CHEMBL207642 77119 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
155540774 172514 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
CHEMBL4483537 172514 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
155543069 173188 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 459 5 2 5 4.7 C[C@@H](Nc1cncc(C2=CCN(C(=O)[C@H]3CCCCN3)CC2)n1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.9b00506
CHEMBL4522437 173188 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 459 5 2 5 4.7 C[C@@H](Nc1cncc(C2=CCN(C(=O)[C@H]3CCCCN3)CC2)n1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.9b00506
59456003 73864 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018952 73864 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
44562235 186460 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 495 6 1 7 5.9 COc1cc2nc(N3CCCN(C4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487665 186460 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 495 6 1 7 5.9 COc1cc2nc(N3CCCN(C4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44561332 176222 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL459463 176222 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
58835024 92643 0 None -398 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 570 8 1 6 5.5 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
CHEMBL2435852 92643 0 None -398 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 570 8 1 6 5.5 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
134324891 174567 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4556507 174567 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
25212379 187862 1 None -2 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496356 187862 1 None -2 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
134210775 177776 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 7 0 8 4.8 CCOC(=O)CN1CCCC(C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4643066 177776 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 7 0 8 4.8 CCOC(=O)CN1CCCC(C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
134211057 177625 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641127 177625 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
59455976 87155 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
CHEMBL2326611 87155 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
59456050 87170 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
CHEMBL2326625 87170 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
118706816 112970 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2014.05.021
CHEMBL3310825 112970 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2014.05.021
118706816 112970 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2017.07.052
CHEMBL3310825 112970 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2017.07.052
44562192 185777 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486656 185777 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44581103 187773 0 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495737 187773 0 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581068 187924 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496787 187924 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
137636569 155874 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 4 1 7 2.5 COc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4060413 155874 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 4 1 7 2.5 COc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
10215932 73127 1 None -22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL2011441 73127 1 None -22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
145958908 162090 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 401 4 1 5 3.6 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(C(F)(F)F)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160965 162090 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 401 4 1 5 3.6 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(C(F)(F)F)c1Cl 10.1021/acsmedchemlett.7b00315
145951136 162752 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 358 4 1 6 2.5 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C#N 10.1021/acsmedchemlett.7b00315
CHEMBL4171579 162752 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 358 4 1 6 2.5 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C#N 10.1021/acsmedchemlett.7b00315
137632086 156437 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 401 4 1 7 2.8 COc1nn(C)c2nc(C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4066934 156437 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 401 4 1 7 2.8 COc1nn(C)c2nc(C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137654717 158732 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 5 1 8 2.5 COc1nn(C)c2nc(N(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4093509 158732 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 5 1 8 2.5 COc1nn(C)c2nc(N(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137652889 158905 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 1.7 CNC(=O)Cn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
CHEMBL4095437 158905 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 1.7 CNC(=O)Cn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
145951247 162928 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1c(Cl)cccc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4174254 162928 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1c(Cl)cccc1Cl 10.1021/acsmedchemlett.7b00315
10193603 162943 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1cccs1 10.1021/acsmedchemlett.7b00315
CHEMBL4174488 162943 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1cccs1 10.1021/acsmedchemlett.7b00315
44581044 193448 0 None 3 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
CHEMBL526474 193448 0 None 3 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
692856 141363 19 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL383736 141363 19 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
134325269 170691 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 516 5 1 7 4.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(=O)O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4451802 170691 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 516 5 1 7 4.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(=O)O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134210768 177454 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4638846 177454 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
134325215 174978 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4566304 174978 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44562155 186631 0 None 19 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488018 186631 0 None 19 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
44430312 87260 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL233046 87260 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
11525206 135228 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL372399 135228 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
127047356 139634 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 139634 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
127045756 139869 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799266 139869 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127046614 139926 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799578 139926 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
10287052 162378 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1ncc(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4165356 162378 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1ncc(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
11234202 162903 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 373 4 1 6 3.3 COc1nc(Cl)cnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4173861 162903 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 373 4 1 6 3.3 COc1nc(Cl)cnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44562189 186575 0 None -7 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487835 186575 0 None -7 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
156010600 177138 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633920 177138 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
118706830 112984 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310840 112984 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054532 73875 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018962 73875 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
58054387 87152 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
CHEMBL2326609 87152 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
59456098 87179 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1ccc(F)c2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326634 87179 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1ccc(F)c2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
137639968 156677 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 416 5 2 8 2.5 CNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4069639 156677 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 416 5 2 8 2.5 CNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
137639432 156830 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 4 1 8 1.9 COc1nn(C)c2ncnc(NS(=O)(=O)c3ccc(Cl)s3)c12 10.1016/j.bmc.2017.07.052
CHEMBL4071299 156830 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 4 1 8 1.9 COc1nn(C)c2ncnc(NS(=O)(=O)c3ccc(Cl)s3)c12 10.1016/j.bmc.2017.07.052
10308962 163043 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1F 10.1021/acsmedchemlett.7b00315
CHEMBL4176082 163043 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1F 10.1021/acsmedchemlett.7b00315
137634526 155929 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 8 2.5 COc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4060967 155929 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 8 2.5 COc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
137632304 156477 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1nn(C)c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4067451 156477 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1nn(C)c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137647898 157741 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.5 COCCOc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4082318 157741 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.5 COCCOc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137644970 158495 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 5 2 6 2.9 CCOc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4091069 158495 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 5 2 6 2.9 CCOc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
59168178 162984 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 343 4 1 5 2.0 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.7b00315
CHEMBL4175259 162984 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 343 4 1 5 2.0 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.7b00315
137637450 155819 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 460 8 2 9 2.5 COCCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4059913 155819 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 460 8 2 9 2.5 COCCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
145955548 162612 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 423 5 1 5 4.7 CC(C)(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169258 162612 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 423 5 1 5 4.7 CC(C)(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
134225259 177744 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4642563 177744 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44430315 11866 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL1182360 11866 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233047 11866 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
155548141 173787 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@@H](N4CCCCC4)[C@@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4537681 173787 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@@H](N4CCCCC4)[C@@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44562155 186631 0 None -19 2 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488018 186631 0 None -19 2 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
134324996 171743 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 540 4 0 6 6.5 CC1CN(c2cnc3c(C(F)(F)F)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4467274 171743 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 540 4 0 6 6.5 CC1CN(c2cnc3c(C(F)(F)F)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
134210954 177810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643609 177810 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44581042 187833 0 None 6 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496151 187833 0 None 6 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581102 187772 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495736 187772 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
156012782 177364 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637695 177364 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134210898 177783 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643158 177783 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
59455974 73874 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018961 73874 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
44562236 186727 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 512 10 1 8 4.9 CCN(CC)CCN1CCCN(c2nc(Nc3ccc(Cl)cc3)c3cc(OC)c(OC)cc3n2)CC1 10.1016/j.bmc.2008.07.062
CHEMBL488690 186727 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 512 10 1 8 4.9 CCN(CC)CCN1CCCN(c2nc(Nc3ccc(Cl)cc3)c3cc(OC)c(OC)cc3n2)CC1 10.1016/j.bmc.2008.07.062
44562190 186576 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 471 8 2 8 3.9 COc1cc2nc(N3CCC(N(C)CCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487836 186576 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 471 8 2 8 3.9 COc1cc2nc(N3CCC(N(C)CCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
59455974 73874 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018961 73874 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
59456102 73877 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018964 73877 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
59456003 73864 0 None - 1 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018952 73864 0 None - 1 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
59456051 73880 0 None - 1 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018967 73880 0 None - 1 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
9959269 73866 0 None - 1 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
CHEMBL2018954 73866 0 None - 1 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
58054516 73871 0 None - 1 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
CHEMBL2018959 73871 0 None - 1 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
9827294 73865 3 None - 1 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
CHEMBL2018953 73865 3 None - 1 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
10416 1879 30 None 309 2 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
46861584 1879 30 None 309 2 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
CHEMBL2018969 1879 30 None 309 2 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
59456067 73881 0 None - 1 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018968 73881 0 None - 1 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
70685473 73863 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018951 73863 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
70689680 73867 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018955 73867 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
49798461 10693 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170725 10693 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798437 10559 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169660 10559 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798349 10791 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171786 10791 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
16124598 10729 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171008 10729 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
12893 4140 0 None - 1 Human 7.0 pIC50 < 7 Functional
Binned value from patentBinned value from patent
Guide to Pharmacology 565 7 2 6 6.3 CC1=C(C(=NC(=N1)N2CC(C2)[C@H]3CCCN(C3)C4CC(C4)(C)C(=O)O)N[C@H](C)C5=C(C=C(C=C5)Cl)Cl)Cl None
139344142 4140 0 None - 1 Human 7.0 pIC50 < 7 Functional
Binned value from patentBinned value from patent
Guide to Pharmacology 565 7 2 6 6.3 CC1=C(C(=NC(=N1)N2CC(C2)[C@H]3CCCN(C3)C4CC(C4)(C)C(=O)O)N[C@H](C)C5=C(C=C(C=C5)Cl)Cl)Cl None
5280343 188275 124 None -16 12 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 188275 124 None -16 12 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 188275 124 None -16 12 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 4779 101 None 3 44 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4779 101 None 3 44 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
4410 3137 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 3137 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 3137 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 3137 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 3137 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
3793 203209 77 None -1 4 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
45039617 203209 77 None -1 4 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
CHEMBL64391 203209 77 None -1 4 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
12153 1665 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patentAntagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patent
Guide to Pharmacology 542 6 1 7 4.9 C[C@H](c1c(cc(cc1)Cl)Cl)n1c2nc(cnc2c(n1)C(F)(F)F)N1CC(C1)[C@H]1CCCN(C1)CCO None
134210715 1665 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patentAntagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patent
Guide to Pharmacology 542 6 1 7 4.9 C[C@H](c1c(cc(cc1)Cl)Cl)n1c2nc(cnc2c(n1)C(F)(F)F)N1CC(C1)[C@H]1CCCN(C1)CCO None
10417 1069 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.
Guide to Pharmacology 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 31259550
134324842 1069 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.
Guide to Pharmacology 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 31259550
CHEMBL4459231 1069 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.
Guide to Pharmacology 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 31259550
10308720 545 42 None -2 3 Dog 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 545 42 None -2 3 Dog 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 545 42 None -2 3 Dog 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
25141190 1146 28 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
9478 1146 28 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
CHEMBL508207 1146 28 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
10308720 545 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 545 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 545 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
10308720 545 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 545 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 545 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
23585443 542 12 None -3 3 Dog 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 542 12 None -3 3 Dog 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 542 12 None -3 3 Dog 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
23585443 542 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 542 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 542 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
797 832 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724
23585443 542 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 542 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 542 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
798 846 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
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selectivity		 # Tested
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Type		 Assay
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 DOI
44410965 77059 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 5 2 4 4.1 CCNCc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207290 77059 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 5 2 4 4.1 CCNCc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44406335 73934 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL202085 73934 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44288732 101169 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(F)cc2F)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL295560 101169 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(F)cc2F)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288854 165061 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42266 165061 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
44288730 165972 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(F)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42523 165972 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(F)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289282 169776 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 617 11 3 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc2[nH]ccc2c1 10.1016/j.bmcl.2004.01.072
CHEMBL44390 169776 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 617 11 3 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc2[nH]ccc2c1 10.1016/j.bmcl.2004.01.072
5481702 205823 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 205823 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
5280343 188275 124 None - 32 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 188275 124 None - 32 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 188275 124 None - 32 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
71720517 87007 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 87007 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
44288960 163796 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42060 163796 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1Cl 10.1016/j.bmcl.2004.01.072
44400830 71235 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 10 1 4 5.1 CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195665 71235 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 10 1 4 5.1 CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
5280343 188275 124 None - 32 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 188275 124 None - 32 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 188275 124 None - 32 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
44288899 101265 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 13 2 6 3.6 O=C(C[C@H]1S[C@H](CCc2ccccc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL296245 101265 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 13 2 6 3.6 O=C(C[C@H]1S[C@H](CCc2ccccc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288863 162071 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 6 3.5 O=C(C[C@H]1S[C@H](C2CCCCC2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL416069 162071 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 6 3.5 O=C(C[C@H]1S[C@H](C2CCCCC2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289207 168191 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 633 9 1 5 6.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(Cc2cccc(CN3CCOCC3)c2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43330 168191 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 633 9 1 5 6.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(Cc2cccc(CN3CCOCC3)c2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288557 170284 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccoc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44463 170284 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccoc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
5280343 188275 124 None - 32 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 188275 124 None - 32 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 188275 124 None - 32 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
134211221 177688 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4641873 177688 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
45104526 200709 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 479 3 3 7 3.8 Cc1c(N2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL599995 200709 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 479 3 3 7 3.8 Cc1c(N2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
44288959 165307 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42334 165307 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44430304 152122 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2c(ncn2CC)n1 10.1016/j.bmcl.2006.10.091
CHEMBL396786 152122 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2c(ncn2CC)n1 10.1016/j.bmcl.2006.10.091
11285792 879 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO 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
801 879 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO 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 879 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO 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 879 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO 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
44288962 100474 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 10 2 5 4.5 CN(C)CC(=O)NCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL290845 100474 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 10 2 5 4.5 CN(C)CC(=O)NCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44288985 155542 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 668 14 2 9 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1OC 10.1016/j.bmcl.2004.01.072
CHEMBL40427 155542 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 668 14 2 9 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1OC 10.1016/j.bmcl.2004.01.072
44288961 155631 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1ccccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL40468 155631 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1ccccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
44289214 157303 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40771 157303 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288776 166319 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 10 2 8 3.3 O=C(CN1C(=O)[C@@H](CC(=O)Nc2nccs2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL42722 166319 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 10 2 8 3.3 O=C(CN1C(=O)[C@@H](CC(=O)Nc2nccs2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44288731 170339 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 11 2 6 3.9 Cc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(C)c1 10.1016/j.bmcl.2004.01.072
CHEMBL44472 170339 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 11 2 6 3.9 Cc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(C)c1 10.1016/j.bmcl.2004.01.072
44288963 170980 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 11 2 7 3.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccs1 10.1016/j.bmcl.2004.01.072
CHEMBL44561 170980 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 11 2 7 3.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccs1 10.1016/j.bmcl.2004.01.072
45104751 200918 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 1 1 5 1.9 Cc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL601651 200918 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 1 1 5 1.9 Cc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
3793 203209 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
134210626 177305 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4636749 177305 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
155557193 174525 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
CHEMBL4555534 174525 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
44561588 194553 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL529664 194553 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44406247 141197 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 463 5 0 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(OCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
CHEMBL382826 141197 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 463 5 0 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(OCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
71454500 78992 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113068 78992 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2005.02.084
44289275 101513 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL298035 101513 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
44289277 163503 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)ccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42021 163503 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)ccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289072 169340 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.3 O=C(C[C@H]1S[C@H](c2cccc(C(F)(F)F)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44187 169340 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.3 O=C(C[C@H]1S[C@H](c2cccc(C(F)(F)F)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44411038 76800 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 471 8 1 4 7.6 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)no2)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL206921 76800 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 471 8 1 4 7.6 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)no2)c1C 10.1016/j.bmcl.2006.01.126
3793 203209 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44289062 163659 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42044 163659 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.072
44289064 170931 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 660 12 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2004.01.072
CHEMBL44553 170931 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 660 12 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2004.01.072
45104634 200736 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 2 6 1.7 CCN1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
CHEMBL600196 200736 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 2 6 1.7 CCN1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
45104523 201711 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 437 3 3 6 4.0 Cc1c(N2CCN(C(=O)Nc3ccc(C(C)C)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL606421 201711 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 437 3 3 6 4.0 Cc1c(N2CCN(C(=O)Nc3ccc(C(C)C)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
134225247 177663 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641595 177663 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
134210845 178049 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647188 178049 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
155540774 172514 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
CHEMBL4483537 172514 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
44411321 138425 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 509 8 1 4 8.6 FC(F)(F)c1ccccc1CN(Cc1csc(Nc2cccc3ccccc23)n1)CC1CCCCC1 10.1016/j.bmcl.2006.01.126
CHEMBL377421 138425 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 509 8 1 4 8.6 FC(F)(F)c1ccccc1CN(Cc1csc(Nc2cccc3ccccc23)n1)CC1CCCCC1 10.1016/j.bmcl.2006.01.126
44430311 152380 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 460 11 2 6 5.9 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2cccnc2n1 10.1016/j.bmcl.2006.10.091
CHEMBL397028 152380 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 460 11 2 6 5.9 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2cccnc2n1 10.1016/j.bmcl.2006.10.091
44288958 168727 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL43698 168727 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
44288981 165557 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 7 2 5 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42419 165557 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 7 2 5 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
25141301 185888 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 185888 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
156015374 177615 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4640909 177615 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44411492 138896 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3cnccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL378272 138896 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3cnccc23)n1 10.1016/j.bmcl.2006.01.126
44288943 164629 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42162 164629 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2004.01.072
44288913 169290 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(F)c1 10.1016/j.bmcl.2004.01.072
CHEMBL44143 169290 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(F)c1 10.1016/j.bmcl.2004.01.072
44401027 70552 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL194775 70552 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
134325041 175032 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4567398 175032 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
45104946 200720 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 371 5 0 6 2.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCC3)ccc12 10.1021/jm901652p
CHEMBL600018 200720 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 371 5 0 6 2.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCC3)ccc12 10.1021/jm901652p
45104635 200737 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 420 2 2 6 3.9 Cc1c(N2CCN(c3cccc(C(F)(F)F)c3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL600197 200737 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 420 2 2 6 3.9 Cc1c(N2CCN(c3cccc(C(F)(F)F)c3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
45104422 201232 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 406 3 2 6 2.9 Cc1c(N2CCN(C(=O)/C=C/c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL603701 201232 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 406 3 2 6 2.9 Cc1c(N2CCN(C(=O)/C=C/c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
45104527 200710 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 409 3 3 6 2.5 Cc1c(N2CCN(C(=O)NCc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL599996 200710 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 409 3 3 6 2.5 Cc1c(N2CCN(C(=O)NCc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
2812 4779 101 None - 34 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 4779 101 None - 34 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
71720517 87007 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 87007 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
45104848 201095 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 3 0 5 2.3 CCOc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL602887 201095 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 3 0 5 2.3 CCOc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
10417 1069 9 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
134324842 1069 9 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
CHEMBL4459231 1069 9 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
9814022 77111 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 268 3 1 3 5.2 CC(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207589 77111 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 268 3 1 3 5.2 CC(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
692856 141363 19 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL383736 141363 19 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
71461653 78990 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccccc2Cl)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113066 78990 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccccc2Cl)c1 10.1016/j.bmcl.2005.02.084
134335393 170112 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4443688 170112 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
11496063 77119 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
CHEMBL207642 77119 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
44288978 168736 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 585 10 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43706 168736 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 585 10 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288827 168801 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43758 168801 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
71458049 78999 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 359 11 1 4 4.7 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(F)cc2)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113075 78999 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 359 11 1 4 4.7 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(F)cc2)c1 10.1016/j.bmcl.2005.02.084
44561561 179001 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL470962 179001 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44288791 100196 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 12 2 6 3.3 CC(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL288256 100196 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 12 2 6 3.3 CC(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
44430309 87224 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ccccc12 10.1016/j.bmcl.2006.10.091
CHEMBL232841 87224 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ccccc12 10.1016/j.bmcl.2006.10.091
134325106 171251 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4460062 171251 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
45104945 200719 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 385 5 0 6 2.7 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCCC3)ccc12 10.1021/jm901652p
CHEMBL600017 200719 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 385 5 0 6 2.7 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCCC3)ccc12 10.1021/jm901652p
44430312 87260 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL233046 87260 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
44288880 101558 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 5 5.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL298454 101558 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 5 5.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
3793 203209 77 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44411325 168878 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1 10.1016/j.bmcl.2006.01.126
CHEMBL438248 168878 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1 10.1016/j.bmcl.2006.01.126
44288879 169343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL44188 169343 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44400833 70707 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 392 11 1 5 5.1 CCN(CC)CCCC(C)Nc1nc(COc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195061 70707 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 392 11 1 5 5.1 CCN(CC)CCCC(C)Nc1nc(COc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
44401066 126415 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CN(C)CCCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL365155 126415 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CN(C)CCCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44289208 163846 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 7 1 5 4.6 CN1CCN(C(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
CHEMBL42065 163846 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 7 1 5 4.6 CN1CCN(C(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
71452724 78996 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113072 78996 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2005.02.084
45104633 200401 22 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 290 1 2 6 1.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL598070 200401 22 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 290 1 2 6 1.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
9943773 77304 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 286 2 1 3 5.1 CC(C)(C)c1csc(Nc2cccc3c2CCCC3)n1 10.1016/j.bmcl.2006.01.126
CHEMBL208249 77304 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 286 2 1 3 5.1 CC(C)(C)c1csc(Nc2cccc3c2CCCC3)n1 10.1016/j.bmcl.2006.01.126
44411033 77349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 299 3 1 4 5.2 CCn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
CHEMBL208458 77349 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 299 3 1 4 5.2 CCn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
44430302 87118 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2nc[nH]c12 10.1016/j.bmcl.2006.10.091
CHEMBL232639 87118 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2nc[nH]c12 10.1016/j.bmcl.2006.10.091
44289116 169280 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 11 2 6 3.7 CC(C)(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL44134 169280 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 11 2 6 3.7 CC(C)(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
176 398 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
134324891 174567 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4556507 174567 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
9922232 165759 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 296 3 1 3 5.6 CC(C)(C)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL424689 165759 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 296 3 1 3 5.6 CC(C)(C)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44289186 165082 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42270 165082 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1 10.1016/j.bmcl.2004.01.072
44289105 98432 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 656 13 2 6 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL275593 98432 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 656 13 2 6 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288818 155412 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40366 155412 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44400899 70583 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 390 11 1 4 5.3 CCN(CC)CCCC(C)Nc1nc(CCc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL194930 70583 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 390 11 1 4 5.3 CCN(CC)CCCC(C)Nc1nc(CCc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
44288912 166085 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 678 13 2 7 4.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCNS(=O)(=O)CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42586 166085 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 678 13 2 7 4.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCNS(=O)(=O)CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134211126 177569 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4640439 177569 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
10308720 545 42 None - 0 Dog 7.6 pIC50 = 7.6 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 545 42 None - 0 Dog 7.6 pIC50 = 7.6 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 545 42 None - 0 Dog 7.6 pIC50 = 7.6 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
44289241 100414 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL290201 100414 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288996 169360 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL44198 169360 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
44289039 100243 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.01.072
CHEMBL288655 100243 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.01.072
44289340 101247 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 664 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2004.01.072
CHEMBL296152 101247 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 664 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2004.01.072
44288911 167924 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 595 11 2 7 3.1 Cc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)n1C 10.1016/j.bmcl.2004.01.072
CHEMBL43143 167924 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 595 11 2 7 3.1 Cc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)n1C 10.1016/j.bmcl.2004.01.072
44400829 71317 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 412 9 1 4 6.4 CCN(CC)CCCC(C)Nc1nc(-c2ccc3ccccc3c2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195751 71317 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 412 9 1 4 6.4 CCN(CC)CCCC(C)Nc1nc(-c2ccc3ccccc3c2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
44400922 68650 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 11 1 5 4.6 CCN(CC)CCCC(C)Nc1ccnc(COc2cccc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
CHEMBL191915 68650 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 11 1 5 4.6 CCN(CC)CCCC(C)Nc1ccnc(COc2cccc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
44400881 71405 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(COc2cc(Cl)cc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195893 71405 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(COc2cc(Cl)cc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
45104427 200849 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 473 4 3 8 2.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)cc1 10.1021/jm901652p
CHEMBL601217 200849 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 473 4 3 8 2.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)cc1 10.1021/jm901652p
134325076 172185 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4473604 172185 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134211098 178044 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647117 178044 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
9856506 76758 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 260 2 1 3 4.8 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL206789 76758 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 260 2 1 3 4.8 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1C 10.1016/j.bmcl.2006.01.126
44430305 87121 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ncn(CC)c12 10.1016/j.bmcl.2006.10.091
CHEMBL232641 87121 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ncn(CC)c12 10.1016/j.bmcl.2006.10.091
11223594 71084 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195298 71084 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44430315 11866 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL1182360 11866 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233047 11866 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
44430308 152125 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 433 10 1 5 5.7 CCN(CC)CCCC(C)Nc1ccc2cnn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
CHEMBL396787 152125 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 433 10 1 5 5.7 CCN(CC)CCCC(C)Nc1ccc2cnn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
44401007 70840 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195103 70840 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44289401 163445 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 604 10 2 6 4.0 O=C(CN1C(=O)[C@@H](CC(=O)N[C@@H]2CCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL41983 163445 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 604 10 2 6 4.0 O=C(CN1C(=O)[C@@H](CC(=O)N[C@@H]2CCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44289082 166572 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccco2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42799 166572 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccco2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
23585443 542 12 None - 0 Dog 8.5 pIC50 = 8.5 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 542 12 None - 0 Dog 8.5 pIC50 = 8.5 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 542 12 None - 0 Dog 8.5 pIC50 = 8.5 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9900444 77161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3ncccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207857 77161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3ncccc23)n1 10.1016/j.bmcl.2006.01.126
44406309 133536 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3ccnc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
CHEMBL370861 133536 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3ccnc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
692856 141363 19 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL383736 141363 19 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44288879 169343 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL44188 169343 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44400947 71322 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 396 11 1 5 4.9 CCN(CC)CCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195764 71322 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 396 11 1 5 4.9 CCN(CC)CCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
11496063 77119 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
CHEMBL207642 77119 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
44288903 166381 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 5 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42757 166381 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 5 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
45104849 202523 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 4 0 5 4.2 CCC1CCC(Oc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)CC1 10.1021/jm901652p
CHEMBL611508 202523 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 4 0 5 4.2 CCC1CCC(Oc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)CC1 10.1021/jm901652p
45104748 201037 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 3.5 Cc1cccc(N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)c1C 10.1021/jm901652p
CHEMBL602474 201037 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 3.5 Cc1cccc(N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)c1C 10.1021/jm901652p
44289098 101386 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 13 2 8 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1 10.1016/j.bmcl.2004.01.072
CHEMBL297173 101386 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 13 2 8 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1 10.1016/j.bmcl.2004.01.072
134335394 172342 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
CHEMBL4475665 172342 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
134225255 177325 10 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 177325 10 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44289027 101232 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 652 8 1 5 6.3 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL296067 101232 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 652 8 1 5 6.3 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288779 101413 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 9 1 5 5.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL297335 101413 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 9 1 5 5.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289036 163106 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2cccs2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL417712 163106 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2cccs2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289106 165526 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 620 13 2 8 3.3 COc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(OC)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42411 165526 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 620 13 2 8 3.3 COc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(OC)c1 10.1016/j.bmcl.2004.01.072
21866580 77146 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 481 8 1 3 8.0 Cc1cccc(Nc2cccc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)n2)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL207780 77146 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 481 8 1 3 8.0 Cc1cccc(Nc2cccc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)n2)c1C 10.1016/j.bmcl.2006.01.126
44289276 167926 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 634 11 2 7 4.7 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1csc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43144 167926 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 634 11 2 7 4.7 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1csc2ccccc12 10.1016/j.bmcl.2004.01.072
44288726 169439 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 561 11 2 7 2.7 O=C(C[C@H]1S[C@H](c2ccncc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44262 169439 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 561 11 2 7 2.7 O=C(C[C@H]1S[C@H](c2ccncc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
71720517 87007 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 87007 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
44289235 101380 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 8 2 5 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL297145 101380 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 8 2 5 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289204 169849 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 614 10 2 6 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44401 169849 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 614 10 2 6 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134325003 175382 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4575089 175382 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134225259 177744 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4642563 177744 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44288904 164668 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 586 11 2 5 4.9 CN(C)CCCNC(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42168 164668 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 586 11 2 5 4.9 CN(C)CCCNC(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44289227 169435 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 600 11 1 5 5.2 CN(C)CCCN(C)C(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL44259 169435 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 600 11 1 5 5.2 CN(C)CCCN(C)C(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44430317 87342 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 439 12 3 7 4.8 CCN(CC)CCCC(C)Nc1nc(NC)nc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233261 87342 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 439 12 3 7 4.8 CCN(CC)CCCC(C)Nc1nc(NC)nc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
44288898 168688 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 515 8 1 4 5.4 CN(C)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL43661 168688 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 515 8 1 4 5.4 CN(C)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
155531126 171607 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4465359 171607 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
21866577 75965 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 285 2 1 4 4.7 Cn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
CHEMBL205279 75965 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 285 2 1 4 4.7 Cn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
134210898 177783 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643158 177783 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44411191 140239 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 484 8 1 4 7.4 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)nn2C)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL380537 140239 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 484 8 1 4 7.4 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)nn2C)c1C 10.1016/j.bmcl.2006.01.126
156012782 177364 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637695 177364 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44289203 170534 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 12 2 6 5.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44498 170534 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 12 2 6 5.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134324973 170387 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4447900 170387 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
45104844 200920 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 1 6 1.6 COc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL601653 200920 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 1 6 1.6 COc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
134225255 177325 10 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assayAntagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 177325 10 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assayAntagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
71720517 87007 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 87007 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
134211057 177625 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641127 177625 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
44289341 163473 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 6 4.4 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL42001 163473 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 6 4.4 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
44288923 163668 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)ccc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42046 163668 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)ccc1Cl 10.1016/j.bmcl.2004.01.072
44288683 169070 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 578 11 2 6 3.5 O=C(C[C@H]1S[C@H](c2ccc(F)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43969 169070 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 578 11 2 6 3.5 O=C(C[C@H]1S[C@H](c2ccc(F)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
71449124 78993 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113069 78993 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.02.084
134336138 177495 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639418 177495 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
45104752 201583 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 1 0 6 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc3c(cc12)OCO3 10.1021/jm901652p
CHEMBL605581 201583 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 1 0 6 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc3c(cc12)OCO3 10.1021/jm901652p
45104423 200919 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 330 2 2 6 1.3 C=CC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
CHEMBL601652 200919 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 330 2 2 6 1.3 C=CC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
45104321 200721 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 276 1 3 6 0.9 Cc1c(N2CCNCC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL600019 200721 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 276 1 3 6 0.9 Cc1c(N2CCNCC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
45104425 200879 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 2.5 Cc1c(N2CCN(C(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL601424 200879 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 2.5 Cc1c(N2CCN(C(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
134335394 172342 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
CHEMBL4475665 172342 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
44411266 76757 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 274 3 1 3 5.3 CC(C)c1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
CHEMBL206788 76757 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 274 3 1 3 5.3 CC(C)c1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
44289342 166112 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 606 11 2 6 4.1 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1C 10.1016/j.bmcl.2004.01.072
CHEMBL42600 166112 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 606 11 2 6 4.1 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1C 10.1016/j.bmcl.2004.01.072
156010350 177082 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633133 177082 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
10133595 77068 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 367 8 1 4 6.2 CC(C)CN(Cc1csc(Nc2cccc3ccccc23)n1)CC(C)C 10.1016/j.bmcl.2006.01.126
CHEMBL207320 77068 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 367 8 1 4 6.2 CC(C)CN(Cc1csc(Nc2cccc3ccccc23)n1)CC(C)C 10.1016/j.bmcl.2006.01.126
9899450 76539 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 232 2 1 3 4.2 CC(C)(C)c1csc(Nc2ccccc2)n1 10.1016/j.bmcl.2006.01.126
CHEMBL206103 76539 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 232 2 1 3 4.2 CC(C)(C)c1csc(Nc2ccccc2)n1 10.1016/j.bmcl.2006.01.126
45104846 200762 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 301 2 0 5 1.9 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(N(C)C)ccc12 10.1021/jm901652p
CHEMBL600409 200762 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 301 2 0 5 1.9 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(N(C)C)ccc12 10.1021/jm901652p
45104845 199174 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 318 3 0 6 1.9 COc1cc(OC)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL589521 199174 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 318 3 0 6 1.9 COc1cc(OC)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
21866574 77090 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 271 2 2 3 4.7 CC(C)(C)c1csc(Nc2cccc3[nH]ccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207479 77090 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 271 2 2 3 4.7 CC(C)(C)c1csc(Nc2cccc3[nH]ccc23)n1 10.1016/j.bmcl.2006.01.126
44430303 87120 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2[nH]cnc2n1 10.1016/j.bmcl.2006.10.091
CHEMBL232640 87120 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2[nH]cnc2n1 10.1016/j.bmcl.2006.10.091
134225255 177325 10 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 177325 10 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
11525206 135228 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL372399 135228 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2006.10.091
11525206 135228 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL372399 135228 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44430310 87259 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2ccccc2n1 10.1016/j.bmcl.2006.10.091
CHEMBL233045 87259 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2ccccc2n1 10.1016/j.bmcl.2006.10.091
3793 203209 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 203209 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44562156 186729 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488704 186729 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
45104847 200436 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 2 0 5 1.9 COc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL598339 200436 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 2 0 5 1.9 COc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
156010372 177108 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4633494 177108 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
45104943 201124 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 5 0 6 3.5 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCc3cccs3)ccc12 10.1021/jm901652p
CHEMBL603104 201124 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 5 0 6 3.5 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCc3cccs3)ccc12 10.1021/jm901652p
45104524 200808 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 417 7 3 6 3.3 CCCCCCCNC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
CHEMBL600805 200808 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 417 7 3 6 3.3 CCCCCCCNC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
4015979 77347 3 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 302 3 1 3 5.7 c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
CHEMBL208452 77347 3 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 302 3 1 3 5.7 c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
134210768 177454 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4638846 177454 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44406246 73026 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 479 9 2 6 4.3 CC(C)[C@@H](CNc1nccc(OCc2ccc(Cl)cc2Cl)n1)NC(=O)C1CCCN(C)C1 10.1016/j.bmcl.2005.09.022
CHEMBL200966 73026 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 479 9 2 6 4.3 CC(C)[C@@H](CNc1nccc(OCc2ccc(Cl)cc2Cl)n1)NC(=O)C1CCCN(C)C1 10.1016/j.bmcl.2005.09.022
44288897 101486 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 529 9 1 4 5.7 CN(C)CCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL297854 101486 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 529 9 1 4 5.7 CN(C)CCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44288663 100260 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 641 11 2 6 4.5 CN1CCN(CCCNC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
CHEMBL288800 100260 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 641 11 2 6 4.5 CN1CCN(CCCNC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
156010600 177138 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633920 177138 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
134325016 174653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
CHEMBL4558456 174653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
45104747 201015 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 370 2 2 6 3.0 Cc1c(N2CCN(c3ccc(F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL602269 201015 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 370 2 2 6 3.0 Cc1c(N2CCN(c3ccc(F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
134211225 177925 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4645325 177925 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44406338 72922 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 434 5 2 6 2.8 O=C([C@H]1CCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL200465 72922 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 434 5 2 6 2.8 O=C([C@H]1CCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44288972 166432 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 8 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42774 166432 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 8 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
45104525 201342 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 487 4 3 7 4.7 Cc1c(N2CCN(C(=O)Nc3ccccc3Oc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL604330 201342 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 487 4 3 7 4.7 Cc1c(N2CCN(C(=O)Nc3ccccc3Oc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
44289283 101254 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(CN1C(=O)[C@@H](CC(=O)NC(c2ccccc2)c2ccccc2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL296192 101254 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(CN1C(=O)[C@@H](CC(=O)NC(c2ccccc2)c2ccccc2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44289063 161971 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL415902 161971 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.01.072
44289097 178625 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 680 11 2 6 5.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
CHEMBL46748 178625 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 680 11 2 6 5.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
45104426 201854 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 416 3 2 7 2.0 Cc1c(N2CCN(S(=O)(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL607137 201854 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 416 3 2 7 2.0 Cc1c(N2CCN(S(=O)(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
44401118 71070 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uMInhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uM
ChEMBL 388 10 1 4 5.7 CCN(CC)CCCC(C)Nc1nc(/C=C/c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195203 71070 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uMInhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uM
ChEMBL 388 10 1 4 5.7 CCN(CC)CCCC(C)Nc1nc(/C=C/c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
134324770 170943 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
CHEMBL4455432 170943 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
134225255 177325 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 177325 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44561217 189116 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL510375 189116 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44289057 165342 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2ccsc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42360 165342 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2ccsc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289281 101103 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 618 10 2 6 4.4 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL295057 101103 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 618 10 2 6 4.4 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
45104944 200718 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 387 5 0 7 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCOCC3)ccc12 10.1021/jm901652p
CHEMBL600016 200718 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 387 5 0 7 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCOCC3)ccc12 10.1021/jm901652p
44288799 101532 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL298230 101532 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
10417 1069 9 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
134324842 1069 9 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
CHEMBL4459231 1069 9 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
16724339 186437 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 186437 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 186437 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL487635 186437 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44406282 72704 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
CHEMBL199733 72704 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
44289055 100360 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 568 11 2 7 3.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccco1 10.1016/j.bmcl.2004.01.072
CHEMBL289661 100360 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 568 11 2 7 3.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccco1 10.1016/j.bmcl.2004.01.072
44288575 155182 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 10 2 6 3.6 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCCC2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL40238 155182 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 10 2 6 3.6 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCCC2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44288698 169093 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43988 169093 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134210954 177810 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643609 177810 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
3793 203209 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
25141190 1146 28 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
9478 1146 28 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
CHEMBL508207 1146 28 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
44561137 186719 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL488640 186719 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
45104850 201096 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 394 5 0 6 3.4 COc1ccc(COc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)cc1 10.1021/jm901652p
CHEMBL602888 201096 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 394 5 0 6 3.4 COc1ccc(COc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)cc1 10.1021/jm901652p
134211185 177153 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4634054 177153 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
156018849 177907 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4645037 177907 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
45104750 200917 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 274 1 1 5 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)ccc12 10.1021/jm901652p
CHEMBL601650 200917 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 274 1 1 5 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)ccc12 10.1021/jm901652p
44289343 165861 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42491 165861 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1Cl 10.1016/j.bmcl.2004.01.072
3793 203209 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 203209 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 203209 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44430313 149801 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 485 5 2 7 3.3 O=C([C@@H]1CCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL394859 149801 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 485 5 2 7 3.3 O=C([C@@H]1CCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
44411037 76783 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 266 2 1 3 4.9 CC(C)(C)c1coc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL206878 76783 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 266 2 1 3 4.9 CC(C)(C)c1coc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
9814340 139509 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 282 2 1 3 5.3 CC(C)(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL379460 139509 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 282 2 1 3 5.3 CC(C)(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44410966 169042 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 311 6 1 4 4.9 CCN(CC)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL439518 169042 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 311 6 1 4 4.9 CCN(CC)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44406355 72764 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.0 O=C(C1CCCNC1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL199913 72764 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.0 O=C(C1CCCNC1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44288828 100458 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2c(Cl)cccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL290678 100458 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2c(Cl)cccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289242 155435 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40377 155435 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289205 163170 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 598 8 2 5 5.0 CN1CCC(NC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
CHEMBL418072 163170 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 598 8 2 5 5.0 CN1CCC(NC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
44288996 169360 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL44198 169360 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
44401087 71126 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CCN(CC)CCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195484 71126 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CCN(CC)CCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44430306 87222 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2ncn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
CHEMBL232839 87222 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2ncn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
44430307 87223 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2c(ncn2Cc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL232840 87223 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2c(ncn2Cc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
44288818 155412 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40366 155412 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288682 166084 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42585 166084 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
3117 207841 103 None -4 16 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -4 16 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
45104424 201307 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 352 2 2 6 1.4 Cc1c(N2CCN(C(=O)CCl)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL604130 201307 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 352 2 2 6 1.4 Cc1c(N2CCN(C(=O)CCl)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
155541406 172995 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4518040 172995 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
5071677 76000 19 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 358 3 1 3 7.0 CC(C)(C)c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
CHEMBL205490 76000 19 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 358 3 1 3 7.0 CC(C)(C)c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
44411322 140915 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
CHEMBL382244 140915 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
44288481 101151 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 557 8 1 5 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL295405 101151 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 557 8 1 5 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288998 166500 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 10 3 5 4.3 NCCNC(=O)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42786 166500 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 10 3 5 4.3 NCCNC(=O)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44289278 167850 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)cc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43092 167850 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)cc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44401153 135282 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 368 9 1 5 4.1 CCN(CC)CCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL372670 135282 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 368 9 1 5 4.1 CCN(CC)CCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44288964 164904 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42226 164904 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1 10.1016/j.bmcl.2004.01.072
134210933 177506 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639600 177506 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
71720517 87007 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 87007 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
127047356 139634 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 139634 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
59456102 73877 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2018964 73877 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
59455976 87155 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
CHEMBL2326611 87155 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
71583488 87160 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
CHEMBL2326616 87160 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
59455990 87177 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326632 87177 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
59456103 87167 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
CHEMBL2326622 87167 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
56849395 87190 0 None - 1 Human 5.9 pKd = 5.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326926 87190 0 None - 1 Human 5.9 pKd = 5.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59456014 87166 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
CHEMBL2326621 87166 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
11525206 135228 0 None - 1 Human 6.8 pKd = 6.8 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL372399 135228 0 None - 1 Human 6.8 pKd = 6.8 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
127045756 139869 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799266 139869 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
59455988 87165 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
CHEMBL2326620 87165 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
9959269 73866 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
CHEMBL2018954 73866 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
9959269 73866 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
CHEMBL2018954 73866 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
9959269 73866 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
CHEMBL2018954 73866 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
59456050 87170 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
CHEMBL2326625 87170 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
118706830 112984 0 None - 1 Human 5.6 pKd = 5.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310840 112984 0 None - 1 Human 5.6 pKd = 5.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
59456019 87175 0 None - 1 Human 5.5 pKd = 5.5 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326630 87175 0 None - 1 Human 5.5 pKd = 5.5 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
9827294 73865 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
CHEMBL2018953 73865 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
9827294 73865 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
CHEMBL2018953 73865 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
59455975 87157 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
CHEMBL2326613 87157 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
59456010 87163 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
CHEMBL2326619 87163 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
118706817 112971 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310826 112971 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054387 87152 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
CHEMBL2326609 87152 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
58054475 87168 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326623 87168 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
10416 1879 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.ejmech.2016.02.058
46861584 1879 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.ejmech.2016.02.058
CHEMBL2018969 1879 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.ejmech.2016.02.058
10416 1879 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
46861584 1879 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
CHEMBL2018969 1879 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
59456026 87176 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326631 87176 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59456058 87178 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326633 87178 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
118706831 112985 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310841 112985 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054384 87151 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
CHEMBL2326608 87151 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
58054368 87169 0 None - 1 Human 7.1 pKd = 7.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326624 87169 0 None - 1 Human 7.1 pKd = 7.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
102143549 112983 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310839 112983 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
136116031 86802 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
CHEMBL2321924 86802 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
59456111 87162 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
CHEMBL2326618 87162 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
59456012 87159 0 None - 1 Human 5.1 pKd = 5.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
CHEMBL2326615 87159 0 None - 1 Human 5.1 pKd = 5.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
9827294 73865 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
CHEMBL2018953 73865 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
127047356 139634 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 139634 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
127045756 139869 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799266 139869 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
71462571 82570 3 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to CCR4Binding affinity to CCR4
ChEMBL 506 8 3 8 3.5 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(NC(=O)CO)c1 10.1021/jm300682j
CHEMBL2178575 82570 3 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to CCR4Binding affinity to CCR4
ChEMBL 506 8 3 8 3.5 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(NC(=O)CO)c1 10.1021/jm300682j
10416 1879 30 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
46861584 1879 30 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
CHEMBL2018969 1879 30 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
127047973 139765 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 496 5 1 6 4.9 O=C(c1ccccn1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798539 139765 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 496 5 1 6 4.9 O=C(c1ccccn1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127045977 139983 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3799904 139983 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59455974 73874 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018961 73874 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
16747697 93528 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246334 93528 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
71457815 83985 0 None -19 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207091 83985 0 None -19 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
71214976 83996 0 None -79 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207101 83996 0 None -79 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
44440045 93592 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 443 6 1 4 3.2 CC(C)CN1CCC(NC(=O)[C@@H]2CCCN2S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246584 93592 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 443 6 1 4 3.2 CC(C)CN1CCC(NC(=O)[C@@H]2CCCN2S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.03.030
44440043 166867 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 469 7 1 4 3.7 CC(C)c1ccc(S(=O)(=O)N2CCC[C@H]2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.030
CHEMBL428576 166867 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 469 7 1 4 3.7 CC(C)c1ccc(S(=O)(=O)N2CCC[C@H]2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.030
176 398 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
59456102 73877 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018964 73877 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
127046413 140116 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 6 2 6 3.4 CNCC(=O)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797946 140116 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 6 2 6 3.4 CNCC(=O)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3800702 140116 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 6 2 6 3.4 CNCC(=O)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59455992 73869 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018957 73869 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
71461439 83981 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207087 83981 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
71452487 83982 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207088 83982 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
58054487 73876 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018963 73876 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
44440051 149615 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL394714 149615 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
127045976 139831 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3799025 139831 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59456051 73880 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018967 73880 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
16747697 93528 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assayDisplacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246334 93528 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assayDisplacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
44440041 93536 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 441 7 1 4 2.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)Cc1ccccc1 10.1016/j.bmcl.2007.03.030
CHEMBL246384 93536 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 441 7 1 4 2.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)Cc1ccccc1 10.1016/j.bmcl.2007.03.030
71450658 83992 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207098 83992 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
59455973 73868 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccccc1Cn1nc(NS(=O)(=O)c2ccc(Cl)s2)c2c(OC)cccc21 10.1016/j.bmcl.2012.02.104
CHEMBL2018956 73868 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccccc1Cn1nc(NS(=O)(=O)c2ccc(Cl)s2)c2c(OC)cccc21 10.1016/j.bmcl.2012.02.104
58054491 73879 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CNC(C)=O)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018966 73879 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CNC(C)=O)cc1 10.1016/j.bmcl.2012.02.104
127046189 139621 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797567 139621 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
58054516 73871 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
CHEMBL2018959 73871 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
15604497 83993 0 None -79 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207099 83993 0 None -79 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
11525206 135228 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL372399 135228 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
127046247 139616 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 2 6 4.8 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3797537 139616 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 2 6 4.8 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
44440135 93335 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
CHEMBL245319 93335 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
44440081 93397 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 582 8 1 5 3.9 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(N)=O)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245730 93397 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 582 8 1 5 3.9 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(N)=O)CC1 10.1016/j.bmcl.2007.03.030
127045978 139682 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797980 139682 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127045975 139730 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798263 139730 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127046787 139916 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 1 6 4.0 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(C(=O)C4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3799514 139916 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 1 6 4.0 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(C(=O)C4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
127046613 139973 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 456 5 2 6 2.9 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(F)cc4F)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3799865 139973 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 456 5 2 6 2.9 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(F)cc4F)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
44440031 149503 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 427 6 1 3 4.6 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
CHEMBL394642 149503 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 427 6 1 3 4.6 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
70689680 73867 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018955 73867 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
59456072 73870 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018958 73870 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1 10.1016/j.bmcl.2012.02.104
70681287 73873 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
CHEMBL2018960 73873 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
71461438 83976 0 None -251 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207082 83976 0 None -251 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461440 83991 0 None -79 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207097 83991 0 None -79 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
44440072 93529 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 557 7 0 4 5.0 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2F)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246335 93529 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 557 7 0 4 5.0 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2F)CC1 10.1016/j.bmcl.2007.03.030
44440047 93593 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1cccc2ccccc12)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246585 93593 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1cccc2ccccc12)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
44440083 150811 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 554 7 1 5 4.4 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2N)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL395680 150811 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 554 7 1 5 4.4 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2N)CC1 10.1016/j.bmcl.2007.03.030
44440059 93524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 553 8 0 4 5.2 CCN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246328 93524 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 553 8 0 4 5.2 CCN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
9959269 73866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
CHEMBL2018954 73866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
127046614 139926 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799578 139926 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
9959269 73866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
CHEMBL2018954 73866 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
127046612 139750 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3798452 139750 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127046412 140114 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 391 4 2 5 4.0 Clc1ccc(CNc2ccnc(N3CCC4(CCNC4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3797678 140114 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 391 4 2 5 4.0 Clc1ccc(CNc2ccnc(N3CCC4(CCNC4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3800700 140114 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 391 4 2 5 4.0 Clc1ccc(CNc2ccnc(N3CCC4(CCNC4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
58054532 73875 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018962 73875 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
71456007 83986 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207092 83986 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
71456008 83989 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207095 83989 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
70685473 73863 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018951 73863 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
59456003 73864 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018952 73864 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
15985912 83975 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 83975 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71450657 83988 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207094 83988 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
71452488 83987 0 None -79 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207093 83987 0 None -79 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
44440076 151406 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL396166 151406 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.030
44440084 93437 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 607 7 0 4 5.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245931 93437 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 607 7 0 4 5.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.030
3117 207841 103 None -4 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 103 None -4 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44440075 93337 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245331 93337 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.030
44440028 93878 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
CHEMBL247976 93878 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
44440079 93364 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 569 8 0 5 4.8 COc1cccc(CCN2CCC(N(C)C(=O)[C@@H]3CCCN3S(=O)(=O)c3ccc4c(Cl)cccc4c3)CC2)c1 10.1016/j.bmcl.2007.03.030
CHEMBL245531 93364 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 569 8 0 5 4.8 COc1cccc(CCN2CCC(N(C)C(=O)[C@@H]3CCCN3S(=O)(=O)c3ccc4c(Cl)cccc4c3)CC2)c1 10.1016/j.bmcl.2007.03.030
127047612 139892 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799393 139892 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127047970 139822 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.2 O=C(C1CCCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798949 139822 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.2 O=C(C1CCCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127046191 140115 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 3.8 O=C(C1CCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798941 140115 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 3.8 O=C(C1CCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3800701 140115 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 3.8 O=C(C1CCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
70693879 73421 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2016602 73421 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
16747697 93528 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246334 93528 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
71454246 83983 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
CHEMBL2207089 83983 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
71454248 83995 0 None -39 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207100 83995 0 None -39 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
44440080 153359 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 583 8 1 5 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(=O)O)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL397848 153359 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 583 8 1 5 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(=O)O)CC1 10.1016/j.bmcl.2007.03.030
44440054 93695 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 505 7 0 4 4.2 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246986 93695 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 505 7 0 4 4.2 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
44440055 153353 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 519 8 0 4 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL397845 153353 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 519 8 0 4 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
71214725 83977 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207083 83977 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214710 83979 0 None -39 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207085 83979 0 None -39 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
127047972 139620 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 501 5 1 5 5.8 O=C(C1CCCCC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797555 139620 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 501 5 1 5 5.8 O=C(C1CCCCC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59456067 73881 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018968 73881 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
44440077 93338 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245332 93338 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.030
44440065 93334 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 523 7 0 4 4.3 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(F)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245313 93334 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 523 7 0 4 4.3 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(F)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
10416 1879 30 None - 1 Human 7.8 pIC50 = 7.8 Binding
IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.
Guide to Pharmacology 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 23409871
46861584 1879 30 None - 1 Human 7.8 pIC50 = 7.8 Binding
IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.
Guide to Pharmacology 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 23409871
CHEMBL2018969 1879 30 None - 1 Human 7.8 pIC50 = 7.8 Binding
IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.
Guide to Pharmacology 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 23409871
176 398 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 398 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 398 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 398 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 398 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3117 207841 103 None -4 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207841 103 None -4 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None