Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

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 DOI
9827294 73891 None 9 Human Functional pEC50 = 8 8.0 - 1
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 73891 None 9 Human Functional pEC50 = 8 8.0 - 1
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 139837 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 139837 None 0 Human Functional pEC50 = 7.9 7.9 - 1
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 140013 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 140013 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 139721 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 139721 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 168830 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 168830 None 0 Human Functional pEC50 = 5.7 5.7 - 1
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 139694 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 139694 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 139979 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 139979 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 165402 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 165402 None 0 Human Functional pEC50 = 6.2 6.2 - 1
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 162930 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 162930 None 0 Human Functional pIC50 = 9.5 9.5 - 1
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 162592 None 0 Human Functional pIC50 = 9.2 9.2 - 1
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 162592 None 0 Human Functional pIC50 = 9.2 9.2 - 1
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 None 16 Mouse Functional pIC50 = 9 9.0 3 3
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 None 16 Mouse Functional pIC50 = 9 9.0 3 3
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 None 16 Mouse Functional pIC50 = 9 9.0 3 3
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 162267 None 0 Human Functional pIC50 = 9 9.0 - 1
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 162267 None 0 Human Functional pIC50 = 9 9.0 - 1
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 None 41 Mouse Functional pIC50 = 8 8.0 2 3
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 None 41 Mouse Functional pIC50 = 8 8.0 2 3
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 None 41 Mouse Functional pIC50 = 8 8.0 2 3
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 162783 None 0 Human Functional pIC50 = 8 8.0 - 1
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 162783 None 0 Human Functional pIC50 = 8 8.0 - 1
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 135297 None 0 Human Functional pIC50 = 8 8.0 - 1
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 135297 None 0 Human Functional pIC50 = 8 8.0 - 1
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 187940 None 0 Human Functional pIC50 = 7 7.0 1 2
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 187940 None 0 Human Functional pIC50 = 7 7.0 1 2
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 188030 None 0 Human Functional pIC50 = 7 7.0 - 1
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 188030 None 0 Human Functional pIC50 = 7 7.0 - 1
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 192755 None 0 Human Functional pIC50 = 7 7.0 -2 2
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 192755 None 0 Human Functional pIC50 = 7 7.0 -2 2
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 87190 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87190 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87192 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87192 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87193 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87193 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87207 None 0 Human Functional pIC50 = 7 7.0 - 1
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 87207 None 0 Human Functional pIC50 = 7 7.0 - 1
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 162522 None 0 Human Functional pIC50 = 7 7.0 - 1
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 162522 None 0 Human Functional pIC50 = 7 7.0 - 1
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 113039 None 0 Human Functional pIC50 = 6 6.0 - 1
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 113039 None 0 Human Functional pIC50 = 6 6.0 - 1
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 162207 None 0 Human Functional pIC50 = 6 6.0 - 1
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 162207 None 0 Human Functional pIC50 = 6 6.0 - 1
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 162801 None 0 Human Functional pIC50 = 6 6.0 - 1
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 162801 None 0 Human Functional pIC50 = 6 6.0 - 1
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 158356 None 0 Human Functional pIC50 = 5 5.0 - 1
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 158356 None 0 Human Functional pIC50 = 5 5.0 - 1
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 159260 None 0 Human Functional pIC50 = 5 5.0 - 1
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 159260 None 0 Human Functional pIC50 = 5 5.0 - 1
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 162684 None 0 Human Functional pIC50 = 5 5.0 - 1
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 162684 None 0 Human Functional pIC50 = 5 5.0 - 1
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 170571 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 170571 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 84375 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 84375 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 185994 None 0 Human Functional pIC50 = 7.0 7.0 1 2
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 185994 None 0 Human Functional pIC50 = 7.0 7.0 1 2
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 185994 None 0 Human Functional pIC50 = 7.0 7.0 1 2
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 185994 None 0 Human Functional pIC50 = 7.0 7.0 1 2
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 113040 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 113040 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73907 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 73907 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 86836 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 86836 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 87209 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 87209 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 162254 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 162254 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 162501 None 4 Human Functional pIC50 = 7.9 7.9 - 1
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 162501 None 4 Human Functional pIC50 = 7.9 7.9 - 1
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 163132 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 163132 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 178313 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 178313 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 87208 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 87208 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 162069 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 162069 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 163186 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 163186 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 158853 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 158853 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 162869 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 162869 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 156483 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 156483 None 0 Human Functional pIC50 = 4.9 4.9 - 1
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 173296 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 173296 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73904 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 73904 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 176328 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 176328 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 189152 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 189152 None 0 Human Functional pIC50 = 7.9 7.9 - 1
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 186861 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 186861 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 185994 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 185994 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 186543 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 186543 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 185994 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 185994 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 186543 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 186543 None 0 Mouse Functional pIC50 = 6.9 6.9 -1 2
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 177312 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 177312 None 0 Human Functional pIC50 = 5.9 5.9 - 1
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 None 31 Human Functional pIC50 = 7.8 7.8 199 3
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 None 31 Human Functional pIC50 = 7.8 7.8 199 3
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 None 31 Human Functional pIC50 = 7.8 7.8 199 3
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 168830 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 168830 None 0 Human Functional pIC50 = 6.9 6.9 - 1
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 None 26 Human Functional pIC50 = 6.9 6.9 -1 2
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 None 26 Human Functional pIC50 = 6.9 6.9 -1 2
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 None 26 Human Functional pIC50 = 6.9 6.9 -1 2
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 187878 None 0 Mouse Functional pIC50 = 6.9 6.9 1 2
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 187878 None 0 Mouse Functional pIC50 = 6.9 6.9 1 2
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 177926 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 177926 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 87199 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87199 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87200 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87200 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87201 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87201 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87203 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87203 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87212 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87212 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87224 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 87224 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 None 41 Human Functional pIC50 = 7.8 7.8 -4 3
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 None 41 Human Functional pIC50 = 7.8 7.8 -4 3
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 None 41 Human Functional pIC50 = 7.8 7.8 -4 3
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 162279 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 162279 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 162805 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 162805 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 186834 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 186834 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 132880 None 0 Human Functional pIC50 = 5.8 5.8 -446 5
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 132880 None 0 Human Functional pIC50 = 5.8 5.8 -446 5
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 73895 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 73895 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 None 16 Human Functional pIC50 = 6.8 6.8 -16 3
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 None 16 Human Functional pIC50 = 6.8 6.8 -16 3
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 None 16 Human Functional pIC50 = 6.8 6.8 -16 3
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 87206 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 87206 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 156710 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 156710 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 162590 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 162590 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 163163 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 163163 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 113043 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 113043 None 0 Human Functional pIC50 = 5.8 5.8 - 1
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 158500 None 0 Human Functional pIC50 = 4.8 4.8 - 1
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 158500 None 0 Human Functional pIC50 = 4.8 4.8 - 1
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 175859 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 175859 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 175579 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 175579 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 178030 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 178030 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 None 26 Human Functional pIC50 = 7.8 7.8 -1 2
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 173083 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 173083 None 0 Human Functional pIC50 = 7.8 7.8 - 1
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 188370 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 188370 None 0 Human Functional pIC50 = 6.8 6.8 - 1
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 186543 None 0 Human Functional pIC50 = 7.7 7.7 1 2
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 186543 None 0 Human Functional pIC50 = 7.7 7.7 1 2
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 186543 None 0 Human Functional pIC50 = 7.7 7.7 1 2
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 186543 None 0 Human Functional pIC50 = 7.7 7.7 1 2
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 187968 None 2 Human Functional pIC50 = 7.7 7.7 2 2
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 187968 None 2 Human Functional pIC50 = 7.7 7.7 2 2
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 186543 None 0 Human Functional pIC50 = 7.7 7.7 1 2
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 186543 None 0 Human Functional pIC50 = 7.7 7.7 1 2
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 192755 None 0 Mouse Functional pIC50 = 7.7 7.7 2 2
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 192755 None 0 Mouse Functional pIC50 = 7.7 7.7 2 2
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 87191 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 87191 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 87194 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 87194 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 162427 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 162427 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 162646 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 162646 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73152 None 1 Human Functional pIC50 = 6.7 6.7 -22 2
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 73152 None 1 Human Functional pIC50 = 6.7 6.7 -22 2
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 113035 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 113035 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 113045 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 113045 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 158317 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 158317 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 162272 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 162272 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 162477 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 162477 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 113037 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 113037 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 113042 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 113042 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 159174 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 159174 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 113036 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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 113036 None 0 Human Functional pIC50 = 4.7 4.7 - 1
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 None 16 Human Functional pIC50 = 8.6 8.6 -16 3
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 None 16 Human Functional pIC50 = 8.6 8.6 -16 3
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 None 16 Human Functional pIC50 = 8.6 8.6 -16 3
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 162140 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 162140 None 0 Human Functional pIC50 = 8.6 8.6 - 1
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 186543 None 0 Human Functional pIC50 = 6.7 6.7 1 2
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 186543 None 0 Human Functional pIC50 = 6.7 6.7 1 2
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 186543 None 0 Human Functional pIC50 = 6.7 6.7 1 2
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 186543 None 0 Human Functional pIC50 = 6.7 6.7 1 2
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 176330 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 176330 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 194661 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 194661 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 177611 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 177611 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 177430 None 13 Human Functional pIC50 = 7.7 7.7 1 2
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 177430 None 13 Human Functional pIC50 = 7.7 7.7 1 2
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 178149 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 178149 None 0 Human Functional pIC50 = 7.7 7.7 - 1
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 73897 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73897 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 186835 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 186835 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 189225 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 189225 None 0 Human Functional pIC50 = 6.7 6.7 - 1
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 171205 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 171205 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 171046 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 171046 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 177768 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 177768 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 171354 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 171354 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 187968 None 2 Human Functional pIC50 = 7.6 7.6 2 2
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 187968 None 2 Human Functional pIC50 = 7.6 7.6 2 2
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 193557 None 0 Mouse Functional pIC50 = 6.6 6.6 -3 2
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 193557 None 0 Mouse Functional pIC50 = 6.6 6.6 -3 2
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 172512 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 172512 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 177258 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 177258 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 185994 None 0 Human Functional pIC50 = 7.6 7.6 1 2
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 185994 None 0 Human Functional pIC50 = 7.6 7.6 1 2
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 185994 None 0 Human Functional pIC50 = 7.6 7.6 1 2
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 185994 None 0 Human Functional pIC50 = 7.6 7.6 1 2
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 177187 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 177187 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 186737 None 0 Human Functional pIC50 = 7.6 7.6 19 2
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 186737 None 0 Human Functional pIC50 = 7.6 7.6 19 2
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 113046 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 113046 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 87202 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 87202 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 162675 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 162675 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 175080 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 175080 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 87205 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 87205 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 87225 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 87225 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 157649 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 157649 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 159137 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 159137 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 159315 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 159315 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 170425 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 170425 None 0 Human Functional pIC50 = 5.6 5.6 - 1
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 186825 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 186825 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 174757 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 174757 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73906 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 73906 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 169777 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 169777 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 177213 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 177213 None 0 Human Functional pIC50 = 7.6 7.6 - 1
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 186862 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 186862 None 0 Human Functional pIC50 = 6.6 6.6 - 1
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 92697 None 0 Human Functional pIC50 = 6.6 6.6 -467 2
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 92697 None 0 Human Functional pIC50 = 6.6 6.6 -467 2
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 178154 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 178154 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87294 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 87294 None 0 Human Functional pIC50 = 8.5 8.5 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 73892 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 None 16 Human Functional pIC50 = 8.4 8.4 -16 3
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 None 16 Human Functional pIC50 = 8.4 8.4 -16 3
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 None 16 Human Functional pIC50 = 8.4 8.4 -16 3
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 162178 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 162178 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 162951 None 3 Human Functional pIC50 = 8.4 8.4 - 1
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 162951 None 3 Human Functional pIC50 = 8.4 8.4 - 1
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 163086 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 163086 None 0 Human Functional pIC50 = 8.4 8.4 - 1
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 192755 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
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 192755 None 0 Human Functional pIC50 = 7.5 7.5 -2 2
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 177410 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 177410 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 186681 None 0 Human Functional pIC50 = 7.5 7.5 7 2
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 186681 None 0 Human Functional pIC50 = 7.5 7.5 7 2
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 189987 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 189987 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 None 41 Human Functional pIC50 = 7.5 7.5 -4 3
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 None 41 Human Functional pIC50 = 7.5 7.5 -4 3
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 None 41 Human Functional pIC50 = 7.5 7.5 -4 3
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 73903 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73903 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73903 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73903 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87185 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87185 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87195 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87195 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87197 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 87197 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 113034 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 113034 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 None 16 Human Functional pIC50 = 6.5 6.5 -16 3
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 None 16 Human Functional pIC50 = 6.5 6.5 -16 3
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 None 16 Human Functional pIC50 = 6.5 6.5 -16 3
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 87188 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 87188 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 156624 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 156624 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 158407 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 158407 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 156438 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 156438 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 157486 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 157486 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 162341 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 162341 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 162976 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 162976 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 163060 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 163060 None 0 Human Functional pIC50 = 5.5 5.5 - 1
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 172288 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 172288 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 175136 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 175136 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 173814 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 173814 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73889 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 73889 None 0 Human Functional pIC50 = 7.5 7.5 - 1
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 186681 None 0 Human Functional pIC50 = 6.5 6.5 7 2
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 186681 None 0 Human Functional pIC50 = 6.5 6.5 7 2
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 73899 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 73899 None 0 Human Functional pIC50 = 6.5 6.5 - 1
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 172445 None 0 Human Functional pIC50 = 7.5 7.5 8 2
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 172445 None 0 Human Functional pIC50 = 7.5 7.5 8 2
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 178012 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 178012 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 170215 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 170215 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 185883 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 185883 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 177793 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 177793 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 175486 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 175486 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 177720 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 177720 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 92628 None 0 Human Functional pIC50 = 5.4 5.4 -4168 2
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 92628 None 0 Human Functional pIC50 = 5.4 5.4 -4168 2
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 135297 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 135297 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 174629 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 174629 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73893 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73893 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 None 26 Mouse Functional pIC50 = 7.4 7.4 1 2
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 None 26 Mouse Functional pIC50 = 7.4 7.4 1 2
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 None 26 Mouse Functional pIC50 = 7.4 7.4 1 2
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 None 31 Human Functional pIC50 = 7.4 7.4 199 3
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 None 31 Human Functional pIC50 = 7.4 7.4 199 3
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 None 31 Human Functional pIC50 = 7.4 7.4 199 3
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 87196 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87196 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87210 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87210 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87211 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 87211 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 162134 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 162134 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 162150 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 162150 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 162917 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 162917 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 187879 None 0 Mouse Functional pIC50 = 6.4 6.4 -6 2
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 187879 None 0 Mouse Functional pIC50 = 6.4 6.4 -6 2
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 113044 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 113044 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 87221 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 87221 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 87223 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 87223 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 113041 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 113041 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 159820 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 159820 None 0 Human Functional pIC50 = 5.4 5.4 - 1
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 None 9 Human Functional pIC50 = 7.4 7.4 3 2
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 None 9 Human Functional pIC50 = 7.4 7.4 3 2
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 None 9 Human Functional pIC50 = 7.4 7.4 3 2
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 173098 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 173098 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 73902 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 73902 None 0 Human Functional pIC50 = 6.4 6.4 - 1
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 177674 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 177674 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 171710 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 171710 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 187940 None 0 Mouse Functional pIC50 = 6.4 6.4 -1 2
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 187940 None 0 Mouse Functional pIC50 = 6.4 6.4 -1 2
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 186862 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 186862 None 0 Human Functional pIC50 = 7.4 7.4 - 1
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 187939 None 0 Mouse Functional pIC50 = 6.4 6.4 -6 2
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 187939 None 0 Mouse Functional pIC50 = 6.4 6.4 -6 2
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 187878 None 0 Human Functional pIC50 = 6.4 6.4 -1 2
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 187878 None 0 Human Functional pIC50 = 6.4 6.4 -1 2
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 133392 None 0 Human Functional pIC50 = 6.4 6.4 -234 5
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 133392 None 0 Human Functional pIC50 = 6.4 6.4 -234 5
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 177807 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 177807 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 113038 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 113038 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 177600 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 177600 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 170490 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 170490 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73446 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73446 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 187939 None 0 Human Functional pIC50 = 7.3 7.3 6 2
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 187939 None 0 Human Functional pIC50 = 7.3 7.3 6 2
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 179107 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 179107 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 73152 None 1 Mouse Functional pIC50 = 8.3 8.3 22 2
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 73152 None 1 Mouse Functional pIC50 = 8.3 8.3 22 2
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 73891 None 9 Human Functional pIC50 = 8.3 8.3 - 1
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 113048 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 113048 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 87222 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 87222 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 162390 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 162390 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 11870 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 11870 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 11870 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 71108 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 71108 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 None 41 Human Functional pIC50 = 6.3 6.3 -4 3
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 None 41 Human Functional pIC50 = 6.3 6.3 -4 3
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 None 41 Human Functional pIC50 = 6.3 6.3 -4 3
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 None 41 Human Functional pIC50 = 6.3 6.3 -4 3
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 None 41 Human Functional pIC50 = 6.3 6.3 -4 3
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 None 41 Human Functional pIC50 = 6.3 6.3 -4 3
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 156962 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 156962 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 162245 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 162245 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 162492 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 162492 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 162561 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 162561 None 0 Human Functional pIC50 = 5.3 5.3 - 1
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 177974 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 177974 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 187940 None 0 Human Functional pIC50 = 6.3 6.3 1 2
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 187940 None 0 Human Functional pIC50 = 6.3 6.3 1 2
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 189793 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 189793 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 193557 None 0 Human Functional pIC50 = 7.3 7.3 3 2
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 193557 None 0 Human Functional pIC50 = 7.3 7.3 3 2
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 77148 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 77148 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 172617 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 172617 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 173291 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 173291 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73890 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 73890 None 0 Human Functional pIC50 = 7.3 7.3 - 1
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 186566 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 186566 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 176327 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 176327 None 0 Human Functional pIC50 = 6.3 6.3 - 1
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 92696 None 0 Human Functional pIC50 = 6.3 6.3 -398 2
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 92696 None 0 Human Functional pIC50 = 6.3 6.3 -398 2
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 174671 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 174671 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 187968 None 2 Mouse Functional pIC50 = 7.2 7.2 -2 2
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 187968 None 2 Mouse Functional pIC50 = 7.2 7.2 -2 2
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 177881 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 177881 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 177730 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 177730 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 87189 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 87189 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 87204 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 87204 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 113033 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 113033 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 113033 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 113033 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 185883 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 185883 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 187879 None 0 Human Functional pIC50 = 7.2 7.2 6 2
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 187879 None 0 Human Functional pIC50 = 7.2 7.2 6 2
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 188030 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 188030 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 155964 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 155964 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 73152 None 1 Human Functional pIC50 = 7.2 7.2 -22 2
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 73152 None 1 Human Functional pIC50 = 7.2 7.2 -22 2
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 162184 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 162184 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 162847 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 162847 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 156528 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 156528 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 158824 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 158824 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 158997 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 158997 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 163023 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 163023 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 163038 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 163038 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 193557 None 0 Human Functional pIC50 = 7.2 7.2 3 2
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 193557 None 0 Human Functional pIC50 = 7.2 7.2 3 2
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 141450 None 14 Human Functional pIC50 = 5.2 5.2 - 1
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 141450 None 14 Human Functional pIC50 = 5.2 5.2 - 1
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 170794 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 170794 None 0 Human Functional pIC50 = 6.2 6.2 - 1
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 177559 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 177559 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 175082 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 175082 None 0 Human Functional pIC50 = 7.2 7.2 - 1
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 186737 None 0 Human Functional pIC50 = 7.2 7.2 19 2
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 186737 None 0 Human Functional pIC50 = 7.2 7.2 19 2
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 87294 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 87294 None 0 Human Functional pIC50 = 8.2 8.2 - 1
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 135297 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 135297 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 139721 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 139721 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 139956 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 139956 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 140013 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 140013 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 162472 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 162472 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 162998 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 162998 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 186681 None 0 Mouse Functional pIC50 = 6.2 6.2 -7 2
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 186681 None 0 Mouse Functional pIC50 = 6.2 6.2 -7 2
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 177243 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 177243 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 113047 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 113047 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73901 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 73901 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 87186 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 87186 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 87213 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 87213 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 156769 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 156769 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 156922 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 156922 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 163138 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 163138 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 156019 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 156019 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 156568 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 156568 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 157833 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 157833 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 158587 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 158587 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 163079 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 163079 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 155909 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 155909 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 162707 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 162707 None 0 Human Functional pIC50 = 5.1 5.1 - 1
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 177849 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 177849 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 11870 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 11870 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 11870 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 173891 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 173891 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 186737 None 0 Mouse Functional pIC50 = 6.1 6.1 -19 2
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 186737 None 0 Mouse Functional pIC50 = 6.1 6.1 -19 2
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 171846 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 171846 None 0 Human Functional pIC50 = 6.1 6.1 - 1
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 177915 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 177915 None 0 Human Functional pIC50 = 7.1 7.1 - 1
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 187939 None 0 Human Functional pIC50 = 7.1 7.1 6 2
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 187939 None 0 Human Functional pIC50 = 7.1 7.1 6 2
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 187878 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
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 187878 None 0 Human Functional pIC50 = 7.1 7.1 -1 2
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 177469 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 177469 None 0 Human Functional pIC50 = 8.1 8.1 - 1
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 177888 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 177888 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73900 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73900 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 186833 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 186833 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 186682 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 186682 None 0 Human Functional pIC50 = 7.0 7.0 - 1
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 73900 None 0 Human Functional pKd = 6 6.0 - 1
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 73900 None 0 Human Functional pKd = 6 6.0 - 1
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 73903 None 0 Human Functional pKd = 6 6.0 - 1
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 73903 None 0 Human Functional pKd = 6 6.0 - 1
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 73890 None 0 Human Functional pKd = 5.8 5.8 - 1
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 73890 None 0 Human Functional pKd = 5.8 5.8 - 1
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 73906 None 0 Human Functional pKd = 5.7 5.7 - 1
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 73906 None 0 Human Functional pKd = 5.7 5.7 - 1
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 73892 None 0 Human Functional pKd = 6.6 6.6 - 1
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 73892 None 0 Human Functional pKd = 6.6 6.6 - 1
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 73897 None 0 Human Functional pKd = 5.6 5.6 - 1
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 73897 None 0 Human Functional pKd = 5.6 5.6 - 1
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 73891 None 9 Human Functional pKd = 7.3 7.3 - 1
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 73891 None 9 Human Functional pKd = 7.3 7.3 - 1
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 None 31 Human Functional pKd = 6.2 6.2 199 3
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 None 31 Human Functional pKd = 6.2 6.2 199 3
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 None 31 Human Functional pKd = 6.2 6.2 199 3
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 73907 None 0 Human Functional pKd = 6.2 6.2 - 1
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 73907 None 0 Human Functional pKd = 6.2 6.2 - 1
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 73889 None 0 Human Functional pKd = 5.2 5.2 - 1
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 73889 None 0 Human Functional pKd = 5.2 5.2 - 1
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 73893 None 0 Human Functional pKd = 5.2 5.2 - 1
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 73893 None 0 Human Functional pKd = 5.2 5.2 - 1
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 10697 None 0 Human Functional pKi = 5.9 5.9 - 0
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 10697 None 0 Human Functional pKi = 5.9 5.9 - 0
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 10562 None 0 Human Functional pKi = 5.8 5.8 - 0
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 10562 None 0 Human Functional pKi = 5.8 5.8 - 0
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 10795 None 0 Human Functional pKi = 6.4 6.4 - 1
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 10795 None 0 Human Functional pKi = 6.4 6.4 - 1
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 10733 None 0 Human Functional pKi = 6.1 6.1 - 1
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 10733 None 0 Human Functional pKi = 6.1 6.1 - 1
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 None 0 Human Functional pIC50 < 7 7.0 - 1
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 None 0 Human Functional pIC50 < 7 7.0 - 1
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
139344142.0 4140 None 0 Human Functional pIC50 < 7 7.0 - 1
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
CHEMBL5314496 4140 None 0 Human Functional pIC50 < 7 7.0 - 1
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 188382 None 69 Human Functional pIC50 = 8.3 8.3 -16 12
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 188382 None 69 Human Functional pIC50 = 8.3 8.3 -16 12
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 188382 None 69 Human Functional pIC50 = 8.3 8.3 -16 12
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 4781 None 63 Human Functional pIC50 = 8.2 8.2 3 44
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 4781 None 63 Human Functional pIC50 = 8.2 8.2 3 44
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 None 64 Human Functional pIC50 = 8.2 8.2 -18 6
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 3137 None 64 Human Functional pIC50 = 8.2 8.2 -18 6
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015.0 3137 None 64 Human Functional pIC50 = 8.2 8.2 -18 6
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 3137 None 64 Human Functional pIC50 = 8.2 8.2 -18 6
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 3137 None 64 Human Functional pIC50 = 8.2 8.2 -18 6
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 3137 None 64 Human Functional pIC50 = 8.2 8.2 -18 6
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
3793 205667 None 50 Human Functional pIC50 = 8.2 8.2 -1 4
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 205667 None 50 Human Functional pIC50 = 8.2 8.2 -1 4
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 205667 None 50 Human Functional pIC50 = 8.2 8.2 -1 4
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 None 0 Human Functional pIC50 = 7 7.0 - 1
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 None 0 Human Functional pIC50 = 7 7.0 - 1
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
134210715.0 1665 None 0 Human Functional pIC50 = 7 7.0 - 1
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
CHEMBL5314490 1665 None 0 Human Functional pIC50 = 7 7.0 - 1
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
DB15570 1665 None 0 Human Functional pIC50 = 7 7.0 - 1
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 None 9 Human Functional pIC50 = 7.4 7.4 3 2
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 None 9 Human Functional pIC50 = 7.4 7.4 3 2
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 None 9 Human Functional pIC50 = 7.4 7.4 3 2
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 None 41 Dog Functional pIC50 = 7.6 7.6 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 545 None 41 Dog Functional pIC50 = 7.6 7.6 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 545 None 41 Dog Functional pIC50 = 7.6 7.6 -2 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
25141190 1146 None 26 Human Functional pIC50 = 7.7 7.7 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
9478 1146 None 26 Human Functional pIC50 = 7.7 7.7 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
CHEMBL508207 1146 None 26 Human Functional pIC50 = 7.7 7.7 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
10308720 545 None 41 Human Functional pIC50 = 7.8 7.8 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 545 None 41 Human Functional pIC50 = 7.8 7.8 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 545 None 41 Human Functional pIC50 = 7.8 7.8 -4 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
10308720 545 None 41 Mouse Functional pIC50 = 8 8.0 2 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 545 None 41 Mouse Functional pIC50 = 8 8.0 2 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 545 None 41 Mouse Functional pIC50 = 8 8.0 2 3
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
23585443 542 None 16 Dog Functional pIC50 = 8.5 8.5 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 542 None 16 Dog Functional pIC50 = 8.5 8.5 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 542 None 16 Dog Functional pIC50 = 8.5 8.5 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
23585443 542 None 16 Human Functional pIC50 = 8.6 8.6 -16 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 542 None 16 Human Functional pIC50 = 8.6 8.6 -16 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 542 None 16 Human Functional pIC50 = 8.6 8.6 -16 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
797 832 None 0 Human Functional pIC50 = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724
23585443 542 None 16 Mouse Functional pIC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 542 None 16 Mouse Functional pIC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 542 None 16 Mouse Functional pIC50 = 9 9.0 3 3
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
798 846 None 0 Human Functional pIC50 = 9.2 9.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44410965 77087 None 0 Human Binding pIC50 = 6 6.0 - 0
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 77087 None 0 Human Binding pIC50 = 6 6.0 - 0
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 73960 None 0 Human Binding pIC50 = 6 6.0 - 0
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 73960 None 0 Human Binding pIC50 = 6 6.0 - 0
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 101223 None 0 Human Binding pIC50 = 6 6.0 - 0
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 101223 None 0 Human Binding pIC50 = 6 6.0 - 0
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 165156 None 0 Human Binding pIC50 = 6 6.0 - 0
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 165156 None 0 Human Binding pIC50 = 6 6.0 - 0
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 166067 None 0 Human Binding pIC50 = 6 6.0 - 0
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 166067 None 0 Human Binding pIC50 = 6 6.0 - 0
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 169879 None 0 Human Binding pIC50 = 6 6.0 - 0
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 169879 None 0 Human Binding pIC50 = 6 6.0 - 0
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 208281 None 0 Human Binding pIC50 = 5 5.0 - 0
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 208281 None 0 Human Binding pIC50 = 5 5.0 - 0
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 188382 None 69 Human Binding pIC50 = 5 5.0 - 32
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 188382 None 69 Human Binding pIC50 = 5 5.0 - 32
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 188382 None 69 Human Binding pIC50 = 5 5.0 - 32
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 87041 None 0 Human Binding pIC50 = 5 5.0 - 0
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 87041 None 0 Human Binding pIC50 = 5 5.0 - 0
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 163891 None 0 Human Binding pIC50 = 5 5.0 - 0
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 163891 None 0 Human Binding pIC50 = 5 5.0 - 0
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 71259 None 0 Human Binding pIC50 = 5 5.0 - 0
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 71259 None 0 Human Binding pIC50 = 5 5.0 - 0
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 188382 None 69 Human Binding pIC50 = 4 4.0 - 32
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 188382 None 69 Human Binding pIC50 = 4 4.0 - 32
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 188382 None 69 Human Binding pIC50 = 4 4.0 - 32
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 101319 None 0 Human Binding pIC50 = 4 4.0 - 0
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 101319 None 0 Human Binding pIC50 = 4 4.0 - 0
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 162165 None 0 Human Binding pIC50 = 4 4.0 - 0
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 162165 None 0 Human Binding pIC50 = 4 4.0 - 0
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 168294 None 0 Human Binding pIC50 = 4 4.0 - 0
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 168294 None 0 Human Binding pIC50 = 4 4.0 - 0
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 170387 None 0 Human Binding pIC50 = 4 4.0 - 0
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 170387 None 0 Human Binding pIC50 = 4 4.0 - 0
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 188382 None 69 Human Binding pIC50 = 5.0 5.0 - 32
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 188382 None 69 Human Binding pIC50 = 5.0 5.0 - 32
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 188382 None 69 Human Binding pIC50 = 5.0 5.0 - 32
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 177793 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 177793 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 203165 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 203165 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 165402 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 165402 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 152211 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 152211 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 None 32 Human Binding pIC50 = 6.0 6.0 - 0
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 None 32 Human Binding pIC50 = 6.0 6.0 - 0
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 None 32 Human Binding pIC50 = 6.0 6.0 - 0
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 None 32 Human Binding pIC50 = 6.0 6.0 - 0
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 100528 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 100528 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 155632 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 155632 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 155721 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 155721 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 157395 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 157395 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 166414 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 166414 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 170442 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 170442 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 171083 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 171083 None 0 Human Binding pIC50 = 5.0 5.0 - 0
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 203375 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 203375 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 177410 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 177410 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 174629 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 174629 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 194661 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 194661 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 141284 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 141284 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 79023 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 79023 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 101568 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 101568 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 163598 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 163598 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 169443 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 169443 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 76828 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 76828 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 205667 None 50 Human Binding pIC50 = 4.9 4.9 - 1
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 163754 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 163754 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 171034 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 171034 None 0 Human Binding pIC50 = 4.9 4.9 - 0
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 203192 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 203192 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 204168 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 204168 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 177768 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 177768 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 178154 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 178154 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 172617 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 172617 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 138512 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 138512 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 152469 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 152469 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 168830 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 168830 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 165652 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 165652 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 185994 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 185994 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 177720 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 177720 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 138983 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 138983 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 164724 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 164724 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 169393 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 169393 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 70576 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 70576 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 175136 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 175136 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 203176 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203176 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203193 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 203193 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 203689 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203689 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203166 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203166 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 4781 None 63 Human Binding pIC50 = 5.8 5.8 - 34
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 4781 None 63 Human Binding pIC50 = 5.8 5.8 - 34
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 87041 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 87041 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203552 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 203552 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 None 9 Mouse Binding pIC50 = 6.8 6.8 - 0
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 None 9 Mouse Binding pIC50 = 6.8 6.8 - 0
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 None 9 Mouse Binding pIC50 = 6.8 6.8 - 0
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 77140 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 77140 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 141450 None 14 Human Binding pIC50 = 5.8 5.8 - 0
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 141450 None 14 Human Binding pIC50 = 5.8 5.8 - 0
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 79021 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 79021 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 170215 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 170215 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 77148 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 77148 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 168839 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 168839 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 168904 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 168904 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 79030 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 79030 None 0 Human Binding pIC50 = 4.8 4.8 - 0
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 179107 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 179107 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 100250 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 100250 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 87258 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 87258 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 171354 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 171354 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 203175 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 203175 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 87294 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 87294 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 101613 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 101613 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 205667 None 50 Human Binding pIC50 = 6.7 6.7 - 1
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 205667 None 50 Human Binding pIC50 = 6.7 6.7 - 1
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 205667 None 50 Human Binding pIC50 = 6.7 6.7 - 1
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 168981 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 168981 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 169446 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 169446 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 70731 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 70731 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 126483 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 126483 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 163941 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 163941 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 79027 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 79027 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 202857 None 16 Human Binding pIC50 = 7.7 7.7 - 0
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 202857 None 16 Human Binding pIC50 = 7.7 7.7 - 0
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 77333 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 77333 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 77378 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 77378 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 87152 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 87152 None 0 Human Binding pIC50 = 5.7 5.7 - 0
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 169383 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 169383 None 0 Human Binding pIC50 = 4.7 4.7 - 0
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 None 47 Human Binding pIC50 = 4.7 4.7 -6 31
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 None 47 Human Binding pIC50 = 4.7 4.7 -6 31
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
2157.0 398 None 47 Human Binding pIC50 = 4.7 4.7 -6 31
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 None 47 Human Binding pIC50 = 4.7 4.7 -6 31
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 None 47 Human Binding pIC50 = 4.7 4.7 -6 31
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 None 47 Human Binding pIC50 = 4.7 4.7 -6 31
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 174671 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 174671 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 165854 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 165854 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 165177 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 165177 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 98485 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 98485 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 155502 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 155502 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 70607 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 70607 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 166180 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 166180 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 177674 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 177674 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 None 41 Dog Binding pIC50 = 7.6 7.6 - 0
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 None 41 Dog Binding pIC50 = 7.6 7.6 - 0
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 None 41 Dog Binding pIC50 = 7.6 7.6 - 0
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 100468 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 100468 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 169463 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 169463 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 100297 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 100297 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 101301 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 101301 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 168027 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 168027 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 71341 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 71341 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 68672 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 68672 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 71429 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 71429 None 0 Human Binding pIC50 = 4.6 4.6 - 0
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 203306 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 203306 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 172288 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 172288 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 178149 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 178149 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 76786 None 9 Human Binding pIC50 = 6.6 6.6 - 0
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 76786 None 9 Human Binding pIC50 = 6.6 6.6 - 0
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 87155 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 87155 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 71108 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 71108 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 11870 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 11870 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 11870 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 152214 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 152214 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 70864 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 70864 None 0 Human Binding pIC50 = 5.6 5.6 - 0
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 163540 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 163540 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 166667 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 166667 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 None 16 Dog Binding pIC50 = 8.5 8.5 - 0
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 None 16 Dog Binding pIC50 = 8.5 8.5 - 0
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 None 16 Dog Binding pIC50 = 8.5 8.5 - 0
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 77190 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 77190 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 133605 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 133605 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 141450 None 14 Human Binding pIC50 = 5.5 5.5 - 0
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 141450 None 14 Human Binding pIC50 = 5.5 5.5 - 0
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 169446 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 169446 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 71346 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 71346 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 77148 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 77148 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 166476 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 166476 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 204980 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 204980 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 203494 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 203494 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 101441 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 101441 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 172445 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
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 172445 None 0 Mouse Binding pIC50 = 6.5 6.5 - 0
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 177430 None 13 Human Binding pIC50 = 7.5 7.5 - 0
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 177430 None 13 Human Binding pIC50 = 7.5 7.5 - 0
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 101286 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 101286 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 101468 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 101468 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 163201 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 163201 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 165621 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 165621 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 77175 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 77175 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 168029 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 168029 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 169542 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 169542 None 0 Human Binding pIC50 = 4.5 4.5 - 0
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 87041 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 87041 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 101435 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 101435 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 169952 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 169952 None 0 Human Binding pIC50 = 5.5 5.5 - 0
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 175486 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 175486 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 177849 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177849 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 164763 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 164763 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 169538 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 169538 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 87376 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 87376 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 168791 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 168791 None 0 Human Binding pIC50 = 4.4 4.4 - 0
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 171710 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 171710 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 75992 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 75992 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177888 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177888 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 140326 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 140326 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177469 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177469 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 170637 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 170637 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 170490 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 170490 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203377 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203377 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177430 None 13 Mouse Binding pIC50 = 7.4 7.4 - 0
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 177430 None 13 Mouse Binding pIC50 = 7.4 7.4 - 0
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 87041 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 87041 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 177730 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 177730 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 163568 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 163568 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 163763 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 163763 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 169173 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 169173 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 79024 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 79024 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 177600 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177600 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 204040 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 204040 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 203376 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 203376 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 203177 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 203177 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 203336 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 203336 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 172445 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 172445 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 76785 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 76785 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 166207 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 166207 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177187 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 177187 None 0 Human Binding pIC50 = 6.4 6.4 - 0
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 77096 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 77096 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 76566 None 1 Human Binding pIC50 = 5.4 5.4 - 0
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 76566 None 1 Human Binding pIC50 = 5.4 5.4 - 0
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 203218 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 203218 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 201630 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 201630 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 77118 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 77118 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 87154 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 87154 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 177430 None 13 Human Binding pIC50 = 7.3 7.3 - 0
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 177430 None 13 Human Binding pIC50 = 7.3 7.3 - 0
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 135297 None 0 Human Binding pIC50 = 7.3 7.3 - 1
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 135297 None 0 Human Binding pIC50 = 7.3 7.3 - 1
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 135297 None 0 Human Binding pIC50 = 7.3 7.3 - 1
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 135297 None 0 Human Binding pIC50 = 7.3 7.3 - 1
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 87293 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 87293 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 205667 None 50 Human Binding pIC50 = 6.3 6.3 - 1
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 205667 None 50 Human Binding pIC50 = 6.3 6.3 - 1
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 205667 None 50 Human Binding pIC50 = 6.3 6.3 - 1
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 205667 None 50 Human Binding pIC50 = 6.3 6.3 - 1
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 205667 None 50 Human Binding pIC50 = 6.3 6.3 - 1
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 205667 None 50 Human Binding pIC50 = 6.3 6.3 - 1
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 186835 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 186835 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 202892 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 202892 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 177213 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177213 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 203581 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 203581 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 203264 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 203264 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 77376 None 1 Human Binding pIC50 = 5.3 5.3 - 0
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 77376 None 1 Human Binding pIC50 = 5.3 5.3 - 0
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 177559 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 177559 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 73051 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 73051 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 101541 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 101541 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 100314 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 100314 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 177243 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 177243 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 174757 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 174757 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 203472 None 0 Human Binding pIC50 = 4.2 4.2 - 0
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 203472 None 0 Human Binding pIC50 = 4.2 4.2 - 0
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 178030 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 178030 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 72947 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 72947 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 166527 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 166527 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 203799 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 203799 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 101308 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 101308 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 162065 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 162065 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 178730 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 178730 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 204311 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 204311 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 71094 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 71094 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 171046 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 171046 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 177430 None 13 Human Binding pIC50 = 7.2 7.2 - 0
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 177430 None 13 Human Binding pIC50 = 7.2 7.2 - 0
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 189225 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 189225 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 165437 None 0 Human Binding pIC50 = 4.2 4.2 - 0
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 165437 None 0 Human Binding pIC50 = 4.2 4.2 - 0
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 101157 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 101157 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 203174 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 203174 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 101587 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 101587 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 None 9 Human Binding pIC50 = 7.2 7.2 - 0
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 None 9 Human Binding pIC50 = 7.2 7.2 - 0
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 None 9 Human Binding pIC50 = 7.2 7.2 - 0
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 186543 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 186543 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 186543 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 186543 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 72729 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 72729 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 100414 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 100414 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 155272 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 155272 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 169196 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 169196 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 177915 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 177915 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 205667 None 50 Human Binding pIC50 = 5.1 5.1 - 1
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 205667 None 50 Human Binding pIC50 = 5.1 5.1 - 1
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 205667 None 50 Human Binding pIC50 = 5.1 5.1 - 1
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 None 26 Human Binding pIC50 = 7.1 7.1 - 0
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 None 26 Human Binding pIC50 = 7.1 7.1 - 0
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 None 26 Human Binding pIC50 = 7.1 7.1 - 0
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 186825 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 186825 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 203553 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 203553 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 177258 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 177258 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 178012 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 178012 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 203374 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 203374 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 165956 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 165956 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 205667 None 50 Human Binding pIC50 = 5.1 5.1 - 1
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 205667 None 50 Human Binding pIC50 = 5.1 5.1 - 1
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 205667 None 50 Human Binding pIC50 = 5.1 5.1 - 1
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 149889 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 149889 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 76811 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 76811 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 139596 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 139596 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 169145 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 169145 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 72789 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 72789 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 100512 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 100512 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 155525 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 155525 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 163265 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 163265 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 169463 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 169463 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 71150 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 71150 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 87256 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 87256 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 87257 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 87257 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 155502 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 155502 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 166179 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 166179 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 210300 None 60 Human Binding pIC50 = 5.1 5.1 -4 16
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 210300 None 60 Human Binding pIC50 = 5.1 5.1 -4 16
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 203764 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 203764 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 173098 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 173098 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 76027 None 15 Human Binding pIC50 = 6.1 6.1 - 0
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 76027 None 15 Human Binding pIC50 = 6.1 6.1 - 0
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 141002 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 141002 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 101205 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 101205 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 166595 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 166595 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 167953 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 167953 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 135351 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 135351 None 0 Human Binding pIC50 = 5.1 5.1 - 0
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 164999 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 164999 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 177611 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 177611 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 87041 None 0 Human Binding pIC50 = 5 5.0 - 0
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 87041 None 0 Human Binding pIC50 = 5 5.0 - 0
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 139721 None 0 Human Binding pKd = 6 6.0 - 1
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 139721 None 0 Human Binding pKd = 6 6.0 - 1
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 73903 None 0 Human Binding pKd = 6 6.0 - 1
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 73903 None 0 Human Binding pKd = 6 6.0 - 1
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 87189 None 0 Human Binding pKd = 6 6.0 - 1
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 87189 None 0 Human Binding pKd = 6 6.0 - 1
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 87194 None 0 Human Binding pKd = 6 6.0 - 1
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 87194 None 0 Human Binding pKd = 6 6.0 - 1
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 87211 None 0 Human Binding pKd = 6 6.0 - 1
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 87211 None 0 Human Binding pKd = 6 6.0 - 1
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 87201 None 0 Human Binding pKd = 6.9 6.9 - 1
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 87201 None 0 Human Binding pKd = 6.9 6.9 - 1
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 87224 None 0 Human Binding pKd = 5.9 5.9 - 1
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 87224 None 0 Human Binding pKd = 5.9 5.9 - 1
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 87200 None 0 Human Binding pKd = 6.9 6.9 - 1
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 87200 None 0 Human Binding pKd = 6.9 6.9 - 1
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 135297 None 0 Human Binding pKd = 6.8 6.8 - 1
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 135297 None 0 Human Binding pKd = 6.8 6.8 - 1
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 139956 None 0 Human Binding pKd = 6.7 6.7 - 1
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 139956 None 0 Human Binding pKd = 6.7 6.7 - 1
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 87199 None 0 Human Binding pKd = 6.7 6.7 - 1
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 87199 None 0 Human Binding pKd = 6.7 6.7 - 1
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 73892 None 0 Human Binding pKd = 6.6 6.6 - 1
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 73892 None 0 Human Binding pKd = 6.6 6.6 - 1
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 73892 None 0 Human Binding pKd = 6.6 6.6 - 1
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 73892 None 0 Human Binding pKd = 6.6 6.6 - 1
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 73892 None 0 Human Binding pKd = 6.6 6.6 - 1
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 73892 None 0 Human Binding pKd = 6.6 6.6 - 1
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 87204 None 0 Human Binding pKd = 6.6 6.6 - 1
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 87204 None 0 Human Binding pKd = 6.6 6.6 - 1
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 113047 None 0 Human Binding pKd = 5.6 5.6 - 1
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 113047 None 0 Human Binding pKd = 5.6 5.6 - 1
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 87209 None 0 Human Binding pKd = 5.5 5.5 - 1
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 87209 None 0 Human Binding pKd = 5.5 5.5 - 1
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 73891 None 9 Human Binding pKd = 7.3 7.3 - 1
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 73891 None 9 Human Binding pKd = 7.3 7.3 - 1
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 73891 None 9 Human Binding pKd = 7.3 7.3 - 1
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 73891 None 9 Human Binding pKd = 7.3 7.3 - 1
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 87191 None 0 Human Binding pKd = 6.3 6.3 - 1
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 87191 None 0 Human Binding pKd = 6.3 6.3 - 1
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 87197 None 0 Human Binding pKd = 6.3 6.3 - 1
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 87197 None 0 Human Binding pKd = 6.3 6.3 - 1
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 113034 None 0 Human Binding pKd = 5.3 5.3 - 1
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 113034 None 0 Human Binding pKd = 5.3 5.3 - 1
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 87186 None 0 Human Binding pKd = 5.3 5.3 - 1
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 87186 None 0 Human Binding pKd = 5.3 5.3 - 1
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 87202 None 0 Human Binding pKd = 6.3 6.3 - 1
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 87202 None 0 Human Binding pKd = 6.3 6.3 - 1
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 None 31 Human Binding pKd = 6.2 6.2 - 1
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 None 31 Human Binding pKd = 6.2 6.2 - 1
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 None 31 Human Binding pKd = 6.2 6.2 - 1
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 None 31 Human Binding pKd = 6.2 6.2 - 1
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 None 31 Human Binding pKd = 6.2 6.2 - 1
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 None 31 Human Binding pKd = 6.2 6.2 - 1
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 87210 None 0 Human Binding pKd = 6.2 6.2 - 1
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 87210 None 0 Human Binding pKd = 6.2 6.2 - 1
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 87212 None 0 Human Binding pKd = 6.2 6.2 - 1
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 87212 None 0 Human Binding pKd = 6.2 6.2 - 1
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 113048 None 0 Human Binding pKd = 5.2 5.2 - 1
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 113048 None 0 Human Binding pKd = 5.2 5.2 - 1
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 87185 None 0 Human Binding pKd = 5.2 5.2 - 1
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 87185 None 0 Human Binding pKd = 5.2 5.2 - 1
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 87203 None 0 Human Binding pKd = 7.1 7.1 - 1
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 87203 None 0 Human Binding pKd = 7.1 7.1 - 1
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 113046 None 0 Human Binding pKd = 6.1 6.1 - 1
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 113046 None 0 Human Binding pKd = 6.1 6.1 - 1
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 86836 None 0 Human Binding pKd = 6.1 6.1 - 1
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 86836 None 0 Human Binding pKd = 6.1 6.1 - 1
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 87196 None 0 Human Binding pKd = 6.1 6.1 - 1
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 87196 None 0 Human Binding pKd = 6.1 6.1 - 1
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 87193 None 0 Human Binding pKd = 5.1 5.1 - 1
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 87193 None 0 Human Binding pKd = 5.1 5.1 - 1
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 73891 None 9 Human Binding pKi = 9.1 9.1 - 1
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 73891 None 9 Human Binding pKi = 9.1 9.1 - 1
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 139721 None 0 Human Binding pKi = 9 9.0 - 1
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 139721 None 0 Human Binding pKi = 9 9.0 - 1
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 139956 None 0 Human Binding pKi = 8.8 8.8 - 1
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 139956 None 0 Human Binding pKi = 8.8 8.8 - 1
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 82602 None 3 Human Binding pKi = 8 8.0 - 1
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 82602 None 3 Human Binding pKi = 8 8.0 - 1
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 None 31 Human Binding pKi = 8 8.0 - 1
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 None 31 Human Binding pKi = 8 8.0 - 1
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 None 31 Human Binding pKi = 8 8.0 - 1
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 139852 None 0 Human Binding pKi = 7 7.0 - 1
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 139852 None 0 Human Binding pKi = 7 7.0 - 1
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 140070 None 0 Human Binding pKi = 7 7.0 - 1
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 140070 None 0 Human Binding pKi = 7 7.0 - 1
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 73900 None 0 Human Binding pKi = 7 7.0 - 1
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 73900 None 0 Human Binding pKi = 7 7.0 - 1
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 93581 None 0 Human Binding pKi = 7 7.0 - 1
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 93581 None 0 Human Binding pKi = 7 7.0 - 1
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 84019 None 0 Human Binding pKi = 6 6.0 -19 3
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 84019 None 0 Human Binding pKi = 6 6.0 -19 3
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 84030 None 0 Human Binding pKi = 6 6.0 -79 3
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 84030 None 0 Human Binding pKi = 6 6.0 -79 3
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 93645 None 0 Human Binding pKi = 5 5.0 - 1
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 93645 None 0 Human Binding pKi = 5 5.0 - 1
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 166963 None 0 Human Binding pKi = 5 5.0 - 1
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 166963 None 0 Human Binding pKi = 5 5.0 - 1
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 None 47 Human Binding pKi = 4.9 4.9 -6 31
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 None 47 Human Binding pKi = 4.9 4.9 -6 31
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
2157.0 398 None 47 Human Binding pKi = 4.9 4.9 -6 31
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 None 47 Human Binding pKi = 4.9 4.9 -6 31
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 None 47 Human Binding pKi = 4.9 4.9 -6 31
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 None 47 Human Binding pKi = 4.9 4.9 -6 31
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 73903 None 0 Human Binding pKi = 7.9 7.9 - 1
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 73903 None 0 Human Binding pKi = 7.9 7.9 - 1
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 140203 None 0 Human Binding pKi = 6.9 6.9 - 1
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 140203 None 0 Human Binding pKi = 6.9 6.9 - 1
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 140203 None 0 Human Binding pKi = 6.9 6.9 - 1
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 73895 None 0 Human Binding pKi = 6.9 6.9 - 1
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 73895 None 0 Human Binding pKi = 6.9 6.9 - 1
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 84015 None 0 Human Binding pKi = 5.9 5.9 -12 3
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 84015 None 0 Human Binding pKi = 5.9 5.9 -12 3
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 84016 None 0 Human Binding pKi = 5.9 5.9 -12 3
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 84016 None 0 Human Binding pKi = 5.9 5.9 -12 3
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 73902 None 0 Human Binding pKi = 5.9 5.9 - 1
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 73902 None 0 Human Binding pKi = 5.9 5.9 - 1
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 149703 None 0 Human Binding pKi = 5.9 5.9 - 1
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 149703 None 0 Human Binding pKi = 5.9 5.9 - 1
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 139918 None 0 Human Binding pKi = 7.8 7.8 - 1
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 139918 None 0 Human Binding pKi = 7.8 7.8 - 1
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 73906 None 0 Human Binding pKi = 7.8 7.8 - 1
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 73906 None 0 Human Binding pKi = 7.8 7.8 - 1
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 93581 None 0 Human Binding pKi = 6.8 6.8 - 1
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 93581 None 0 Human Binding pKi = 6.8 6.8 - 1
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 93589 None 0 Human Binding pKi = 4.8 4.8 - 1
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 93589 None 0 Human Binding pKi = 4.8 4.8 - 1
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 84026 None 0 Human Binding pKi = 6.8 6.8 -15 3
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 84026 None 0 Human Binding pKi = 6.8 6.8 -15 3
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 73894 None 0 Human Binding pKi = 6.8 6.8 - 1
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 73894 None 0 Human Binding pKi = 6.8 6.8 - 1
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 73905 None 0 Human Binding pKi = 6.8 6.8 - 1
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 73905 None 0 Human Binding pKi = 6.8 6.8 - 1
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 139708 None 0 Human Binding pKi = 7.7 7.7 - 1
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 139708 None 0 Human Binding pKi = 7.7 7.7 - 1
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 73897 None 0 Human Binding pKi = 7.7 7.7 - 1
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 73897 None 0 Human Binding pKi = 7.7 7.7 - 1
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 84027 None 0 Human Binding pKi = 5.7 5.7 -79 3
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 84027 None 0 Human Binding pKi = 5.7 5.7 -79 3
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 135297 None 0 Human Binding pKi = 8.6 8.6 - 1
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 135297 None 0 Human Binding pKi = 8.6 8.6 - 1
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 139703 None 0 Human Binding pKi = 8.6 8.6 - 1
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 139703 None 0 Human Binding pKi = 8.6 8.6 - 1
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 93388 None 0 Human Binding pKi = 4.7 4.7 - 1
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 93388 None 0 Human Binding pKi = 4.7 4.7 - 1
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 93450 None 0 Human Binding pKi = 6.6 6.6 - 1
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 93450 None 0 Human Binding pKi = 6.6 6.6 - 1
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 139769 None 0 Human Binding pKi = 7.6 7.6 - 1
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 139769 None 0 Human Binding pKi = 7.6 7.6 - 1
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 139817 None 0 Human Binding pKi = 7.6 7.6 - 1
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 139817 None 0 Human Binding pKi = 7.6 7.6 - 1
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 140003 None 0 Human Binding pKi = 7.6 7.6 - 1
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 140003 None 0 Human Binding pKi = 7.6 7.6 - 1
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 140060 None 0 Human Binding pKi = 7.6 7.6 - 1
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 140060 None 0 Human Binding pKi = 7.6 7.6 - 1
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 149591 None 0 Human Binding pKi = 4.6 4.6 - 1
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 149591 None 0 Human Binding pKi = 4.6 4.6 - 1
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 73893 None 0 Human Binding pKi = 6.6 6.6 - 1
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 73893 None 0 Human Binding pKi = 6.6 6.6 - 1
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 73896 None 0 Human Binding pKi = 6.6 6.6 - 1
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 73896 None 0 Human Binding pKi = 6.6 6.6 - 1
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 73899 None 0 Human Binding pKi = 6.6 6.6 - 1
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 73899 None 0 Human Binding pKi = 6.6 6.6 - 1
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 84010 None 0 Human Binding pKi = 5.6 5.6 -251 3
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 84010 None 0 Human Binding pKi = 5.6 5.6 -251 3
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 84025 None 0 Human Binding pKi = 5.6 5.6 -79 3
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 84025 None 0 Human Binding pKi = 5.6 5.6 -79 3
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 93582 None 0 Human Binding pKi = 6.6 6.6 - 1
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 93582 None 0 Human Binding pKi = 6.6 6.6 - 1
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 93646 None 0 Human Binding pKi = 4.6 4.6 - 1
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 93646 None 0 Human Binding pKi = 4.6 4.6 - 1
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 150900 None 0 Human Binding pKi = 6.6 6.6 - 1
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 150900 None 0 Human Binding pKi = 6.6 6.6 - 1
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 93577 None 0 Human Binding pKi = 5.6 5.6 - 1
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 93577 None 0 Human Binding pKi = 5.6 5.6 - 1
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 73892 None 0 Human Binding pKi = 8.5 8.5 - 1
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 73892 None 0 Human Binding pKi = 8.5 8.5 - 1
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 140013 None 0 Human Binding pKi = 8.5 8.5 - 1
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 140013 None 0 Human Binding pKi = 8.5 8.5 - 1
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 73892 None 0 Human Binding pKi = 8.5 8.5 - 1
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 73892 None 0 Human Binding pKi = 8.5 8.5 - 1
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 139837 None 0 Human Binding pKi = 8.4 8.4 - 1
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 139837 None 0 Human Binding pKi = 8.4 8.4 - 1
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 140201 None 0 Human Binding pKi = 6.5 6.5 - 1
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 140201 None 0 Human Binding pKi = 6.5 6.5 - 1
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 140201 None 0 Human Binding pKi = 6.5 6.5 - 1
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 73901 None 0 Human Binding pKi = 6.5 6.5 - 1
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 73901 None 0 Human Binding pKi = 6.5 6.5 - 1
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 84020 None 0 Human Binding pKi = 5.5 5.5 -1 3
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 84020 None 0 Human Binding pKi = 5.5 5.5 -1 3
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 84023 None 0 Human Binding pKi = 5.5 5.5 -50 3
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 84023 None 0 Human Binding pKi = 5.5 5.5 -50 3
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 73889 None 0 Human Binding pKi = 7.4 7.4 - 1
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 73889 None 0 Human Binding pKi = 7.4 7.4 - 1
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 73890 None 0 Human Binding pKi = 7.4 7.4 - 1
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 73890 None 0 Human Binding pKi = 7.4 7.4 - 1
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 84009 None 0 Human Binding pKi = 6.4 6.4 -2 3
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 84009 None 0 Human Binding pKi = 6.4 6.4 -2 3
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 84022 None 0 Human Binding pKi = 6.4 6.4 -15 3
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 84022 None 0 Human Binding pKi = 6.4 6.4 -15 3
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 84021 None 0 Human Binding pKi = 5.4 5.4 -79 3
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 84021 None 0 Human Binding pKi = 5.4 5.4 -79 3
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 151495 None 0 Human Binding pKi = 6.4 6.4 - 1
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 151495 None 0 Human Binding pKi = 6.4 6.4 - 1
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 93490 None 0 Human Binding pKi = 6.4 6.4 - 1
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 93490 None 0 Human Binding pKi = 6.4 6.4 - 1
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 210300 None 60 Human Binding pKi = 5.4 5.4 -4 16
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 210300 None 60 Human Binding pKi = 5.4 5.4 -4 16
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 93390 None 0 Human Binding pKi = 6.3 6.3 - 1
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 93390 None 0 Human Binding pKi = 6.3 6.3 - 1
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 93931 None 0 Human Binding pKi = 5.3 5.3 - 1
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 93931 None 0 Human Binding pKi = 5.3 5.3 - 1
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 93417 None 0 Human Binding pKi = 6.3 6.3 - 1
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 93417 None 0 Human Binding pKi = 6.3 6.3 - 1
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 139979 None 0 Human Binding pKi = 8.3 8.3 - 1
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 139979 None 0 Human Binding pKi = 8.3 8.3 - 1
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 139909 None 0 Human Binding pKi = 7.3 7.3 - 1
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 139909 None 0 Human Binding pKi = 7.3 7.3 - 1
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 140202 None 0 Human Binding pKi = 7.3 7.3 - 1
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 140202 None 0 Human Binding pKi = 7.3 7.3 - 1
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 140202 None 0 Human Binding pKi = 7.3 7.3 - 1
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 73446 None 0 Human Binding pKi = 7.3 7.3 - 1
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 73446 None 0 Human Binding pKi = 7.3 7.3 - 1
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 93581 None 0 Human Binding pKi = 6.3 6.3 - 1
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 93581 None 0 Human Binding pKi = 6.3 6.3 - 1
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 84017 None 0 Human Binding pKi = 6.3 6.3 -1 3
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 84017 None 0 Human Binding pKi = 6.3 6.3 -1 3
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 84029 None 0 Human Binding pKi = 6.3 6.3 -39 3
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 84029 None 0 Human Binding pKi = 6.3 6.3 -39 3
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 153448 None 0 Human Binding pKi = 6.3 6.3 - 1
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 153448 None 0 Human Binding pKi = 6.3 6.3 - 1
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 93748 None 0 Human Binding pKi = 6.2 6.2 - 1
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 93748 None 0 Human Binding pKi = 6.2 6.2 - 1
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 153442 None 0 Human Binding pKi = 6.2 6.2 - 1
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 153442 None 0 Human Binding pKi = 6.2 6.2 - 1
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 84011 None 0 Human Binding pKi = 6.2 6.2 -15 3
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 84011 None 0 Human Binding pKi = 6.2 6.2 -15 3
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 84013 None 0 Human Binding pKi = 6.2 6.2 -39 3
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 84013 None 0 Human Binding pKi = 6.2 6.2 -39 3
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 139707 None 0 Human Binding pKi = 6.2 6.2 - 1
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 139707 None 0 Human Binding pKi = 6.2 6.2 - 1
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 73907 None 0 Human Binding pKi = 8.1 8.1 - 1
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 73907 None 0 Human Binding pKi = 8.1 8.1 - 1
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 93391 None 0 Human Binding pKi = 6.1 6.1 - 1
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 93391 None 0 Human Binding pKi = 6.1 6.1 - 1
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 93387 None 0 Human Binding pKi = 6.1 6.1 - 1
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 93387 None 0 Human Binding pKi = 6.1 6.1 - 1
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 None 31 Human Binding pIC50 = 7.8 7.8 - 1
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 None 31 Human Binding pIC50 = 7.8 7.8 - 1
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 None 31 Human Binding pIC50 = 7.8 7.8 - 1
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 None 47 Human Binding pKi = 8.3 8.3 -6 31
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 None 47 Human Binding pKi = 8.3 8.3 -6 31
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
2157.0 398 None 47 Human Binding pKi = 8.3 8.3 -6 31
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 None 47 Human Binding pKi = 8.3 8.3 -6 31
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 None 47 Human Binding pKi = 8.3 8.3 -6 31
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 None 47 Human Binding pKi = 8.3 8.3 -6 31
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 210300 None 60 Human Binding pKi = 8.3 8.3 -4 16
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 210300 None 60 Human Binding pKi = 8.3 8.3 -4 16
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