Ligand source activities (1 row/activity)



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

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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

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

 Assay
Description		 Source

 Mol
weight		 Rot
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 DOI
9827294 80640 3 None - 1 Human 8.0 pEC50 = 8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL2018953 80640 3 None - 1 Human 8.0 pEC50 = 8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.ejmech.2016.02.058
127046612 146528 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3798452 146528 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127046614 146704 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799578 146704 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
127047356 146412 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 146412 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
44288958 175506 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL43698 175506 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
127047440 146385 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 542 7 2 8 4.4 COc1cc2nc(N3CCC(N(C)C(=O)[C@H]4CCCN4)CC3)nc(Nc3ccc(Cl)cc3F)c2cc1OC 10.1016/j.ejmech.2016.02.058
CHEMBL3797462 146385 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 542 7 2 8 4.4 COc1cc2nc(N3CCC(N(C)C(=O)[C@H]4CCCN4)CC3)nc(Nc3ccc(Cl)cc3F)c2cc1OC 10.1016/j.ejmech.2016.02.058
127047612 146670 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799393 146670 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
44288959 172086 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42334 172086 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
10238794 169614 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 473 7 2 6 4.3 O=S(=O)(Nc1ncc(Cl)nc1OCc1ccccc1CO)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172769 169614 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 473 7 2 6 4.3 O=S(=O)(Nc1ncc(Cl)nc1OCc1ccccc1CO)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10195057 169276 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 444 6 1 6 4.2 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4167445 169276 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 444 6 1 6 4.2 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
23585443 7330 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 7330 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 7330 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
145959198 168952 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 369 4 1 5 2.9 COc1nc(F)c(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4162364 168952 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 369 4 1 5 2.9 COc1nc(F)c(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10308720 7333 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 7333 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 7333 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
10309893 169467 2 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4170431 169467 2 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
11525206 142006 0 None - 1 Human 8.0 pIC50 = 8 Functional
Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPRCalcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL372399 142006 0 None - 1 Human 8.0 pIC50 = 8 Functional
Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPRCalcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44581043 194613 0 None 1 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496152 194613 0 None 1 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581068 194703 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496787 194703 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
25212472 199425 0 None -2 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL521737 199425 0 None -2 2 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
59456023 93931 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 516 8 2 7 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)=O)cccc32)c1 10.1021/jm301572h
CHEMBL2326612 93931 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 516 8 2 7 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)=O)cccc32)c1 10.1021/jm301572h
59456042 93933 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 532 8 3 7 4.5 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)(C)O)cccc32)c1 10.1021/jm301572h
CHEMBL2326614 93933 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 532 8 3 7 4.5 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)(C)O)cccc32)c1 10.1021/jm301572h
59456012 93934 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
CHEMBL2326615 93934 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
71584536 93948 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccnc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326628 93948 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccnc(CNC(C)=O)c1 10.1021/jm301572h
59168189 169206 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1 10.1021/acsmedchemlett.7b00315
CHEMBL4166246 169206 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1 10.1021/acsmedchemlett.7b00315
118706823 119753 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 5 2 5 4.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(C)C 10.1016/j.bmc.2014.05.021
CHEMBL3310832 119753 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 5 2 5 4.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(C)C 10.1016/j.bmc.2014.05.021
10309983 168892 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 417 4 1 6 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4161268 168892 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 417 4 1 6 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)c(Cl)s1 10.1021/acsmedchemlett.7b00315
145949792 169485 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 425 5 1 6 3.8 COc1nc(Br)cnc1NS(=O)(=O)c1sccc1-c1ccccc1 10.1021/acsmedchemlett.7b00315
CHEMBL4170786 169485 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 425 5 1 6 3.8 COc1nc(Br)cnc1NS(=O)(=O)c1sccc1-c1ccccc1 10.1021/acsmedchemlett.7b00315
137642528 165043 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1ccc2c(cnn2C)c1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
CHEMBL4088688 165043 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1ccc2c(cnn2C)c1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
137659242 165946 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 458 6 2 9 2.3 COc1nn(C)c2nc(NC3COC3)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4098333 165946 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 458 6 2 9 2.3 COc1nn(C)c2nc(NC3COC3)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
145955299 169368 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 368 4 1 6 2.6 COc1nc(Cl)cnc1NS(=O)(=O)c1ccnc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4168920 169368 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 368 4 1 6 2.6 COc1nc(Cl)cnc1NS(=O)(=O)c1ccnc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
155520262 177247 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 578 7 0 8 5.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(C)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4448901 177247 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 578 7 0 8 5.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(C)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
71461546 91116 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 640 11 2 5 6.3 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmc.2012.03.069
CHEMBL2216810 91116 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 640 11 2 5 6.3 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmc.2012.03.069
25141301 192667 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 192667 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 192667 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL486840 192667 0 None 1 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
118706824 119754 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 443 5 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1COC1 10.1016/j.bmc.2014.05.021
CHEMBL3310833 119754 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 443 5 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1COC1 10.1016/j.bmc.2014.05.021
59456067 80656 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018968 80656 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
136116031 93577 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
CHEMBL2321924 93577 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
59456019 93950 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326630 93950 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
10195081 168939 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 445 6 1 7 3.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cncnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4162097 168939 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 445 6 1 7 3.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cncnc1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10309206 169185 5 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4165939 169185 5 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
59168214 169816 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 6 1 6 3.0 CCOc1cnc(NS(=O)(=O)c2cccc(Cl)c2Cl)c(OC)n1 10.1021/acsmedchemlett.7b00315
CHEMBL4175972 169816 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 6 1 6 3.0 CCOc1cnc(NS(=O)(=O)c2cccc(Cl)c2Cl)c(OC)n1 10.1021/acsmedchemlett.7b00315
134210781 184987 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(C4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4649666 184987 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(C4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
71584537 93949 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)n1 10.1021/jm301572h
CHEMBL2326629 93949 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)n1 10.1021/jm301572h
10150948 168754 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4159115 168754 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1Cl 10.1021/acsmedchemlett.7b00315
10287210 169870 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.7b00315
CHEMBL4176859 169870 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)cc1 10.1021/acsmedchemlett.7b00315
137652824 165540 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 357 3 1 6 2.5 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
CHEMBL4093994 165540 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 357 3 1 6 2.5 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
10126022 169553 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1ccsc1 10.1021/acsmedchemlett.7b00315
CHEMBL4171873 169553 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1ccsc1 10.1021/acsmedchemlett.7b00315
137632634 163171 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 356 3 1 5 3.1 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ccnc21 10.1016/j.bmc.2017.07.052
CHEMBL4066451 163171 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 356 3 1 5 3.1 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ccnc21 10.1016/j.bmc.2017.07.052
155543648 179972 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn(C(C)c2ccc(Cl)cc2Cl)c2nc(N3CCC(N4CCCCC4)C(C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4522547 179972 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn(C(C)c2ccc(Cl)cc2Cl)c2nc(N3CCC(N4CCCCC4)C(C)C3)cnc12 10.1021/acs.jmedchem.9b00506
70685474 80653 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 518 8 1 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN(C)C(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018965 80653 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 518 8 1 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN(C)C(C)=O)c1 10.1016/j.bmcl.2012.02.104
44561334 183002 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
CHEMBL459464 183002 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
44561260 195823 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 384 6 2 6 5.1 COc1cc2nc(NC3CCCC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL509396 195823 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 384 6 2 6 5.1 COc1cc2nc(NC3CCCC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44562238 193534 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 524 8 1 8 5.0 COc1cc2nc(N3CCCN(CCN4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488855 193534 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 524 8 1 8 5.0 COc1cc2nc(N3CCCN(CCN4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 192667 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 192667 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 193216 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 193216 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 192667 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL486840 192667 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
16724339 193216 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL487635 193216 0 None -1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
156013953 183986 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 418 5 0 6 4.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(CN(C)C)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4635359 183986 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 418 5 0 6 4.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC(CN(C)C)C3)cnc12 10.1021/acs.jmedchem.0c00988
10416 8660 30 None 309 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
46861584 8660 30 None 309 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
CHEMBL2018969 8660 30 None 309 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
44288958 175506 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmc.2012.03.069
CHEMBL43698 175506 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmc.2012.03.069
25141190 7929 28 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
9478 7929 28 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
CHEMBL508207 7929 28 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
44581102 194551 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495736 194551 0 None 1 2 Mouse 6.9 pIC50 = 6.9 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
156017568 184600 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 494 5 0 8 4.3 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4643839 184600 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 494 5 0 8 4.3 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
59455988 93940 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
CHEMBL2326620 93940 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
59456014 93941 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
CHEMBL2326621 93941 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
59456103 93942 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
CHEMBL2326622 93942 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
58054368 93944 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326624 93944 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
59456058 93953 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326633 93953 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
56849395 93965 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326926 93965 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
10308720 7333 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 7333 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 7333 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
10308963 168964 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(F)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4162555 168964 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(F)c1Cl 10.1021/acsmedchemlett.7b00315
145951541 169489 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 409 6 1 5 4.3 CC(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4170833 169489 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 409 6 1 5 4.3 CC(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44562237 193507 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 510 8 1 8 4.7 COc1cc2nc(N3CCCN(CCN4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488691 193507 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 510 8 1 8 4.7 COc1cc2nc(N3CCCN(CCN4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
71525425 139590 0 None -446 5 Human 5.8 pIC50 = 5.8 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 509 8 3 9 2.7 Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
CHEMBL3701196 139590 0 None -446 5 Human 5.8 pIC50 = 5.8 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 509 8 3 9 2.7 Cc1ccc(C(Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
59455992 80644 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018957 80644 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
23585443 7330 12 None -16 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 7330 12 None -16 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 7330 12 None -16 3 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
71584535 93947 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cc(CNC(C)=O)ccn1 10.1021/jm301572h
CHEMBL2326627 93947 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 505 8 2 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cc(CNC(C)=O)ccn1 10.1021/jm301572h
137633709 163398 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 373 4 2 6 2.5 COc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4069103 163398 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 373 4 2 6 2.5 COc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
145955692 169274 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4167390 169274 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 4 1 5 2.7 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1Cl 10.1021/acsmedchemlett.7b00315
145971718 169847 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 453 7 1 5 4.5 CCCCOc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4176441 169847 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 453 7 1 5 4.5 CCCCOc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
118706827 119757 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 461 7 4 7 2.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(CO)CO 10.1016/j.bmc.2014.05.021
CHEMBL3310836 119757 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 461 7 4 7 2.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(CO)CO 10.1016/j.bmc.2014.05.021
137643503 165187 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 3 3 6 2.2 O=S(=O)(Nc1ncnc2[nH]nc(O)c12)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
CHEMBL4090166 165187 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 3 3 6 2.2 O=S(=O)(Nc1ncnc2[nH]nc(O)c12)c1cccc(Cl)c1Cl 10.1016/j.bmc.2017.07.052
155561858 182534 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4583503 182534 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134325276 182254 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4577319 182254 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134211225 184704 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4645325 184704 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
25141190 7929 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
9478 7929 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
CHEMBL508207 7929 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
25141190 7929 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
9478 7929 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
CHEMBL508207 7929 28 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
44561294 179759 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 481 7 1 7 5.6 COc1cc2nc(N3CCC(N(C)C4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL451783 179759 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 481 7 1 7 5.6 COc1cc2nc(N3CCC(N(C)C4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44581121 195042 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 553 10 2 8 5.0 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL499852 195042 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 553 10 2 8 5.0 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
16724339 193216 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 193216 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 193216 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL487635 193216 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
25212379 194641 1 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496356 194641 1 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
16724339 193216 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL487635 193216 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
25212472 199425 0 None 2 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL521737 199425 0 None 2 2 Mouse 7.7 pIC50 = 7.7 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
59455975 93932 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
CHEMBL2326613 93932 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
71583488 93935 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
CHEMBL2326616 93935 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
11244702 169112 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 339 4 1 6 2.7 COc1nccnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4164738 169112 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 339 4 1 6 2.7 COc1nccnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
59168158 169330 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C 10.1021/acsmedchemlett.7b00315
CHEMBL4168237 169330 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C 10.1021/acsmedchemlett.7b00315
10215932 79902 1 None -22 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR4 in human primary Th2 cells by chemotaxis assayAntagonist activity at CCR4 in human primary Th2 cells by chemotaxis assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL2011441 79902 1 None -22 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at CCR4 in human primary Th2 cells by chemotaxis assayAntagonist activity at CCR4 in human primary Th2 cells by chemotaxis assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
118706818 119749 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C 10.1016/j.bmc.2014.05.021
CHEMBL3310827 119749 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C 10.1016/j.bmc.2014.05.021
118706829 119759 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 484 5 2 6 2.8 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CN(C(C)=O)C1 10.1016/j.bmc.2014.05.021
CHEMBL3310838 119759 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 484 5 2 6 2.8 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CN(C(C)=O)C1 10.1016/j.bmc.2014.05.021
137643926 165004 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 6 2 8 2.0 COc1nn(CC(=O)O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4088207 165004 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 6 2 8 2.0 COc1nn(CC(=O)O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
10194488 168957 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1021/acsmedchemlett.7b00315
CHEMBL4162503 168957 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1021/acsmedchemlett.7b00315
10194274 169162 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 1 6 3.2 CCOc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4165500 169162 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 1 6 3.2 CCOc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
118706820 119751 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 415 4 1 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)n(C)c(=O)n2C 10.1016/j.bmc.2014.05.021
CHEMBL3310829 119751 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 415 4 1 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)n(C)c(=O)n2C 10.1016/j.bmc.2014.05.021
118706826 119756 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 458 7 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CCN(C)C 10.1016/j.bmc.2014.05.021
CHEMBL3310835 119756 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 458 7 2 6 3.0 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CCN(C)C 10.1016/j.bmc.2014.05.021
137661320 165860 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2ccccc21 10.1016/j.bmc.2017.07.052
CHEMBL4097341 165860 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2ccccc21 10.1016/j.bmc.2017.07.052
118706819 119750 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2[nH]c(=O)n(C)c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310828 119750 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 401 4 2 5 3.0 COc1cc2[nH]c(=O)n(C)c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
23585443 7330 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 7330 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 7330 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59168181 168825 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 391 5 1 5 3.3 C#CCOc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160218 168825 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 391 5 1 5 3.3 C#CCOc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
16724339 193216 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 193216 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 193216 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL487635 193216 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
44561335 183004 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 393 4 1 5 4.8 c1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
CHEMBL459465 183004 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 393 4 1 5 4.8 c1ccc2c(NC3CCCCCC3)nc(N3CCC(N4CCCC4)CC3)nc2c1 10.1016/j.bmc.2008.05.036
44561588 201332 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL529664 201332 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
134210933 184285 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639600 184285 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134225255 184104 10 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 184104 10 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134211098 184823 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647117 184823 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
58054516 80646 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
CHEMBL2018959 80646 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
44562156 193508 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488704 193508 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
44561217 195895 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL510375 195895 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
134324821 177881 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.5 CC1CN(c2cnc3c(C(N)=O)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4457732 177881 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 515 5 1 7 4.5 CC1CN(c2cnc3c(C(N)=O)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
134324770 177722 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
CHEMBL4455432 177722 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
134225247 184442 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641595 184442 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
134325106 178030 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4460062 178030 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
25212379 194641 1 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496356 194641 1 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581044 200227 0 None -3 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
CHEMBL526474 200227 0 None -3 2 Mouse 6.6 pIC50 = 6.6 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
134325169 179188 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 CC1CN(c2cnc3cnn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4476671 179188 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 CC1CN(c2cnc3cnn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
134211185 183932 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4634054 183932 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
25141301 192667 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 192667 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
25141301 192667 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL486840 192667 0 None 1 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
156010350 183861 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633133 183861 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44562155 193410 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488018 193410 0 None 19 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
102143549 119760 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310839 119760 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054475 93943 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326623 93943 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
58597374 169359 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 363 5 2 6 2.1 COc1nc(CO)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4168775 169359 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 363 5 2 6 2.1 COc1nc(CO)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
134335265 181755 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 497 4 0 7 5.3 CC1CN(c2cnc3c(C#N)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4566241 181755 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 497 4 0 7 5.3 CC1CN(c2cnc3c(C#N)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
71583704 93946 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 9 2 8 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC2COC2)c1 10.1021/jm301572h
CHEMBL2326626 93946 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 518 9 2 8 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC2COC2)c1 10.1021/jm301572h
71583039 93966 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 6 4.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3ccccc32)c1 10.1021/jm301572h
CHEMBL2326927 93966 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 474 7 2 6 4.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3ccccc32)c1 10.1021/jm301572h
137647817 164336 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 429 5 1 8 2.5 COc1nn(C2COC2)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4080352 164336 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 429 5 1 8 2.5 COc1nn(C2COC2)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137653647 165823 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 2.9 CCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4096860 165823 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 2.9 CCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
137661613 166001 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 415 5 1 7 3.5 COc1nn(C(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4098813 166001 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 415 5 1 7 3.5 COc1nn(C(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
155518637 177101 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.2 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(N3CCC(N4CCCCC4)CC3)nc21 10.1021/acs.jmedchem.9b00506
CHEMBL4446924 177101 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.2 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(N3CCC(N4CCCCC4)CC3)nc21 10.1021/acs.jmedchem.9b00506
44561137 193498 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL488640 193498 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
134325016 181432 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
CHEMBL4558456 181432 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
59456051 80655 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018967 80655 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
142450222 176453 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 484 4 1 6 4.5 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(C3=CCN(C(=O)[C@H]4CCCCN4)CC3)nc21 10.1021/acs.jmedchem.9b00506
CHEMBL4437594 176453 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 484 4 1 6 4.5 CC(c1ccc(Cl)cc1Cl)n1ncc2ncc(C3=CCN(C(=O)[C@H]4CCCCN4)CC3)nc21 10.1021/acs.jmedchem.9b00506
156010372 183887 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4633494 183887 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44562191 193535 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488857 193535 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
58834906 99419 0 None -467 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 604 8 1 6 6.2 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2cccc(Cl)c2)CC1 10.1021/jm401101p
CHEMBL2435853 99419 0 None -467 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 604 8 1 6 6.2 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2cccc(Cl)c2)CC1 10.1021/jm401101p
134210845 184828 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647188 184828 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44430312 94035 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL233046 94035 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
9959269 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
CHEMBL2018954 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
9959269 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
CHEMBL2018954 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
9959269 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2017.07.052
9959269 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
CHEMBL2018954 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2017.07.052
CHEMBL2018954 80641 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
23585443 7330 12 None -16 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 7330 12 None -16 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 7330 12 None -16 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59168106 168863 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 2 6 2.7 COc1nc(CO)c(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160846 168863 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 397 5 2 6 2.7 COc1nc(CO)c(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
23585446 169635 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1ncc(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4173046 169635 1 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1ncc(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
59168165 169770 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 521 6 1 5 5.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccc(Br)c1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4175323 169770 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 521 6 1 5 5.6 O=S(=O)(Nc1ncc(Cl)nc1OCc1cccc(Br)c1)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
25212472 199425 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL521737 199425 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 7 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.11.020
134210626 184084 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4636749 184084 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44562189 193354 0 None 7 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487835 193354 0 None 7 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44561333 196657 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2c1 10.1016/j.bmc.2008.05.036
CHEMBL516936 196657 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 6 4.8 COc1ccc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2c1 10.1016/j.bmc.2008.05.036
10308720 7333 42 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 7333 42 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 7333 42 None -4 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilizationAntagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59456102 80652 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018964 80652 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
59456102 80652 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2018964 80652 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
58054384 93926 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
CHEMBL2326608 93926 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
71583489 93936 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCO2)c1 10.1021/jm301572h
CHEMBL2326617 93936 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 546 9 2 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCO2)c1 10.1021/jm301572h
59456010 93938 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
CHEMBL2326619 93938 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
118706817 119748 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310826 119748 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
23585443 7330 12 None -16 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 7330 12 None -16 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 7330 12 None -16 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
59456021 93929 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 7 2 7 4.1 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C#N)cccc32)c1 10.1021/jm301572h
CHEMBL2326610 93929 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 7 2 7 4.1 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C#N)cccc32)c1 10.1021/jm301572h
137632888 163312 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.6 COCCn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
CHEMBL4068045 163312 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.6 COCCn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
137644457 165094 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 402 4 2 8 2.1 COc1nn(C)c2nc(N)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4089151 165094 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 402 4 2 8 2.1 COc1nn(C)c2nc(N)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137632974 163126 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 3.3 COc1nn(C)c2nc(NC(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4065904 163126 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 3.3 COc1nn(C)c2nc(NC(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137652382 164173 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)cccc21 10.1016/j.bmc.2017.07.052
CHEMBL4078359 164173 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 355 3 1 4 3.7 Cn1ncc2c(NS(=O)(=O)c3cccc(Cl)c3Cl)cccc21 10.1016/j.bmc.2017.07.052
10173173 169026 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)ccc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4163571 169026 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)ccc1Cl 10.1021/acsmedchemlett.7b00315
145950145 169660 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 279 6 1 5 1.7 CCCCS(=O)(=O)Nc1ncc(Cl)nc1OC 10.1021/acsmedchemlett.7b00315
CHEMBL4173424 169660 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 279 6 1 5 1.7 CCCCS(=O)(=O)Nc1ncc(Cl)nc1OC 10.1021/acsmedchemlett.7b00315
145950218 169744 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 399 4 1 6 3.5 CSc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4174872 169744 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 399 4 1 6 3.5 CSc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
134325076 178964 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4473604 178964 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134325041 181811 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4567398 181811 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44561172 180489 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 485 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCC(F)CC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL453594 180489 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 485 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCC(F)CC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
70685473 80638 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018951 80638 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
44562189 193354 0 None 7 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487835 193354 0 None 7 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
70681287 80648 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
CHEMBL2018960 80648 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
134335394 179121 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
CHEMBL4475665 179121 0 None 8 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
156018849 184686 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4645037 184686 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134335393 176891 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4443688 176891 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44562192 192556 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486656 192556 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
134211221 184467 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4641873 184467 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
134325003 182161 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4575089 182161 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
156015374 184394 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4640909 184394 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
16041411 99351 0 None -4168 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 572 8 1 6 5.6 O=C(O)c1ccc(Sc2ccc(CN3CCC(N4C(=O)N(C5CCOCC5)C[C@H]4c4ccccc4)CC3)cn2)cc1 10.1021/jm401101p
CHEMBL2434978 99351 0 None -4168 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 572 8 1 6 5.6 O=C(O)c1ccc(Sc2ccc(CN3CCC(N4C(=O)N(C5CCOCC5)C[C@H]4c4ccccc4)CC3)cn2)cc1 10.1021/jm401101p
11525206 142006 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of chemotaxis of murine CCR4 transfected L1.2 cellsInhibition of chemotaxis of murine CCR4 transfected L1.2 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL372399 142006 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of chemotaxis of murine CCR4 transfected L1.2 cellsInhibition of chemotaxis of murine CCR4 transfected L1.2 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
155557193 181304 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
CHEMBL4555534 181304 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
70689680 80642 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018955 80642 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
25141190 7929 28 None 1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
9478 7929 28 None 1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
CHEMBL508207 7929 28 None 1 2 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.11.020
10416 8660 30 None 309 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
46861584 8660 30 None 309 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
CHEMBL2018969 8660 30 None 309 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
59456111 93937 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
CHEMBL2326618 93937 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
59456026 93951 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326631 93951 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59455990 93952 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326632 93952 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
10288569 168819 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 461 4 1 6 3.5 COc1nc(Br)cnc1NS(=O)(=O)c1sc(Cl)cc1Br 10.1021/acsmedchemlett.7b00315
CHEMBL4160139 168819 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 461 4 1 6 3.5 COc1nc(Br)cnc1NS(=O)(=O)c1sc(Cl)cc1Br 10.1021/acsmedchemlett.7b00315
10287192 168835 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 5 2 6 2.4 COc1nc(CO)c(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160463 168835 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 377 5 2 6 2.4 COc1nc(CO)c(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
10193586 169601 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(C)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172568 169601 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1nc(C)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44581103 194552 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495737 194552 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
118706828 119758 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 442 5 3 6 2.6 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CNC1 10.1016/j.bmc.2014.05.021
CHEMBL3310837 119758 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 442 5 3 6 2.6 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C1CNC1 10.1016/j.bmc.2014.05.021
56848673 93962 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)c(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326923 93962 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)c(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
56848670 93964 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326925 93964 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 576 9 3 7 4.6 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
118706825 119755 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 6 2 5 3.9 CCCn1c(=O)[nH]c2cc(NS(=O)(=O)c3cccc(Cl)c3Cl)c(OC)cc21 10.1016/j.bmc.2014.05.021
CHEMBL3310834 119755 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 429 6 2 5 3.9 CCCn1c(=O)[nH]c2cc(NS(=O)(=O)c3cccc(Cl)c3Cl)c(OC)cc21 10.1016/j.bmc.2014.05.021
137656805 166505 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 7 1 8 2.5 COc1nn(CCN(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4104585 166505 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 7 1 8 2.5 COc1nn(CCN(C)C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
10417 7855 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
134324842 7855 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
CHEMBL4459231 7855 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
155541406 179774 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4518040 179774 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
58054487 80651 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018963 80651 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
134211126 184348 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4640439 184348 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
155531126 178386 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4465359 178386 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44581043 194613 0 None -1 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496152 194613 0 None -1 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44562191 193535 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488857 193535 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 485 9 2 8 4.3 COc1cc2nc(N3CCC(N(C)CCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44581042 194612 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496151 194612 0 None -6 2 Mouse 6.4 pIC50 = 6.4 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581102 194551 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495736 194551 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
71555361 140102 0 None -234 5 Human 6.4 pIC50 = 6.4 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 564 8 3 10 2.4 Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
CHEMBL3704573 140102 0 None -234 5 Human 6.4 pIC50 = 6.4 Functional
FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).
ChEMBL 564 8 3 10 2.4 Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 nan
134210778 184481 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4642090 184481 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
118706821 119752 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 444 6 3 6 1.9 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CC(N)=O 10.1016/j.bmc.2014.05.021
CHEMBL3310830 119752 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 444 6 3 6 1.9 COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2CC(N)=O 10.1016/j.bmc.2014.05.021
134336138 184274 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639418 184274 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134324973 177166 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4447900 177166 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
70693879 80196 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2016602 80196 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
44581042 194612 0 None 6 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496151 194612 0 None 6 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44561561 185780 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL470962 185780 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
10215932 79902 1 None 22 2 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL2011441 79902 1 None 22 2 Mouse 8.3 pIC50 = 8.3 Functional
Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
9827294 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
CHEMBL2018953 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
9827294 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
CHEMBL2018953 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
9827294 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2017.07.052
9827294 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
CHEMBL2018953 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2017.07.052
CHEMBL2018953 80640 3 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
118706831 119762 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310841 119762 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
56848674 93963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 542 9 3 7 3.9 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326924 93963 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 542 9 3 7 3.9 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59168115 169075 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1ncc(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4164247 169075 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 347 4 1 5 2.9 COc1ncc(C)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44430315 18638 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL1182360 18638 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233047 18638 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
11223594 77859 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195298 77859 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)Inhibitory concentration in CCR4-transfected murine pre-B L1.2 cells (chemotaxis assay)
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
10308720 7333 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 7333 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 7333 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
10308720 7333 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 7333 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 7333 42 None -4 3 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxisAntagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
137638825 163649 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 1.4 COc1nn(CC(N)=O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4071815 163649 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 6 2 8 1.4 COc1nn(CC(N)=O)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
59168213 168930 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 5 1 7 2.0 COc1nc(S(C)(=O)=O)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4161922 168930 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 5 1 7 2.0 COc1nc(S(C)(=O)=O)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
145955410 169176 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 381 4 1 5 3.3 CCc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL4165828 169176 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 381 4 1 5 3.3 CCc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
10309892 169245 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1021/acsmedchemlett.7b00315
CHEMBL4167021 169245 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1cc(Cl)cc(Cl)c1 10.1021/acsmedchemlett.7b00315
156018931 184648 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 540 6 0 6 6.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4644412 184648 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 540 6 0 6 6.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44581043 194613 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496152 194613 0 None 1 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 1 8 5.1 COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44561363 196463 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 466 6 1 6 6.3 COc1cc2nc(C3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL515355 196463 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 466 6 1 6 6.3 COc1cc2nc(C3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44581044 200227 0 None 3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
CHEMBL526474 200227 0 None 3 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
11496063 83894 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
CHEMBL207642 83894 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
155540774 179293 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
CHEMBL4483537 179293 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
155543069 179967 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 459 5 2 5 4.7 C[C@@H](Nc1cncc(C2=CCN(C(=O)[C@H]3CCCCN3)CC2)n1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.9b00506
CHEMBL4522437 179967 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 459 5 2 5 4.7 C[C@@H](Nc1cncc(C2=CCN(C(=O)[C@H]3CCCCN3)CC2)n1)c1ccc(Cl)cc1Cl 10.1021/acs.jmedchem.9b00506
59456003 80639 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018952 80639 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
44562235 193239 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 495 6 1 7 5.9 COc1cc2nc(N3CCCN(C4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487665 193239 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 495 6 1 7 5.9 COc1cc2nc(N3CCCN(C4CCCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44561332 183001 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL459463 183001 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells by [35S]GTPgammaS binding assay
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCN(C4CCCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
58835024 99418 0 None -398 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 570 8 1 6 5.5 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
CHEMBL2435852 99418 0 None -398 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysisAntagonist activity at CCR4 (unknown origin) expressed in HEK293F cell membranes assessed as inhibition of TARC-induced calcium flux preincubated for 15 mins by spectrophotometric analysis
ChEMBL 570 8 1 6 5.5 Cc1nc(Oc2ccc(C(=O)O)cc2)ccc1CN1CCC(N2C(=O)N(C3CCOCC3)C[C@H]2c2ccccc2)CC1 10.1021/jm401101p
134324891 181346 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4556507 181346 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
25212379 194641 1 None -2 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496356 194641 1 None -2 2 Mouse 7.2 pIC50 = 7.2 Functional
Antagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at mouse CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 511 7 2 8 4.7 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
134210775 184555 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 7 0 8 4.8 CCOC(=O)CN1CCCC(C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4643066 184555 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 7 0 8 4.8 CCOC(=O)CN1CCCC(C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
134211057 184404 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641127 184404 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
59455976 93930 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
CHEMBL2326611 93930 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
59456050 93945 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
CHEMBL2326625 93945 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
118706816 119747 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2014.05.021
CHEMBL3310825 119747 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2014.05.021
118706816 119747 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2017.07.052
CHEMBL3310825 119747 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1cccc2c1c(NS(=O)(=O)c1cccc(Cl)c1Cl)nn2C 10.1016/j.bmc.2017.07.052
44562192 192556 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486656 192556 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 499 10 2 8 4.7 COc1cc2nc(N3CCC(N(C)CCCCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
44581103 194552 0 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495737 194552 0 None 6 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 539 9 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581068 194703 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496787 194703 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 513 7 2 9 3.7 COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
137636569 162653 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 4 1 7 2.5 COc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4060413 162653 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 4 1 7 2.5 COc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
10215932 79902 1 None -22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
CHEMBL2011441 79902 1 None -22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 383 4 1 6 2.8 COc1nc(Br)cnc1NS(=O)(=O)c1ccc(Cl)s1 10.1021/acsmedchemlett.7b00315
145958908 168869 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 401 4 1 5 3.6 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(C(F)(F)F)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4160965 168869 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 401 4 1 5 3.6 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(C(F)(F)F)c1Cl 10.1021/acsmedchemlett.7b00315
145951136 169531 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 358 4 1 6 2.5 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C#N 10.1021/acsmedchemlett.7b00315
CHEMBL4171579 169531 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 358 4 1 6 2.5 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1C#N 10.1021/acsmedchemlett.7b00315
137632086 163216 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 401 4 1 7 2.8 COc1nn(C)c2nc(C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4066934 163216 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 401 4 1 7 2.8 COc1nn(C)c2nc(C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137654717 165511 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 5 1 8 2.5 COc1nn(C)c2nc(N(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4093509 165511 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 430 5 1 8 2.5 COc1nn(C)c2nc(N(C)C)nc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137652889 165684 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 1.7 CNC(=O)Cn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
CHEMBL4095437 165684 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 444 6 2 8 1.7 CNC(=O)Cn1nc(OC)c2c(NS(=O)(=O)c3cccc(Cl)c3Cl)ncnc21 10.1016/j.bmc.2017.07.052
145951247 169707 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1c(Cl)cccc1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4174254 169707 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 411 4 1 5 3.4 COc1nc(Br)cnc1NS(=O)(=O)c1c(Cl)cccc1Cl 10.1021/acsmedchemlett.7b00315
10193603 169722 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1cccs1 10.1021/acsmedchemlett.7b00315
CHEMBL4174488 169722 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 349 4 1 6 2.1 COc1nc(Br)cnc1NS(=O)(=O)c1cccs1 10.1021/acsmedchemlett.7b00315
44581044 200227 0 None 3 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
CHEMBL526474 200227 0 None 3 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 525 8 1 8 5.4 COCC1CCCN(C2CCN(c3nc(Nc4ccc(Cl)cc4)c4cc(OC)c(OC)cc4n3)CC2)C1 10.1016/j.bmc.2008.11.020
692856 148141 19 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL383736 148141 19 None - 1 Human 5.2 pIC50 = 5.2 Functional
Inhibition of TARC-mediated CEM cell migrationInhibition of TARC-mediated CEM cell migration
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
134325269 177470 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 516 5 1 7 4.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(=O)O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4451802 177470 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 516 5 1 7 4.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C(=O)O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134210768 184233 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4638846 184233 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
134325215 181757 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4566304 181757 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 472 4 0 6 5.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44562155 193410 0 None 19 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488018 193410 0 None 19 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at human CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
44430312 94035 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL233046 94035 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4Inhibition of MDC-induced chemotaxis in L1.2 cells expressing CCR4
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
11525206 142006 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL372399 142006 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
127047356 146412 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 146412 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
127045756 146647 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799266 146647 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127046614 146704 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799578 146704 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assayAntagonist activity at human CCR4 expressed in CHO cells by [35S]GTPgammaS assay
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
10287052 169157 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1ncc(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4165356 169157 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 367 4 1 5 3.2 COc1ncc(Cl)nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
11234202 169682 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 373 4 1 6 3.3 COc1nc(Cl)cnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4173861 169682 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 373 4 1 6 3.3 COc1nc(Cl)cnc1NS(=O)(=O)c1scc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
44562189 193354 0 None -7 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487835 193354 0 None -7 2 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 451 6 1 7 4.6 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
156010600 183917 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633920 183917 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
118706830 119761 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310840 119761 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054532 80650 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018962 80650 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
58054387 93927 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
CHEMBL2326609 93927 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
59456098 93954 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1ccc(F)c2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326634 93954 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 522 8 2 7 4.4 COc1ccc(F)c2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
137639968 163456 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 416 5 2 8 2.5 CNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4069639 163456 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 416 5 2 8 2.5 CNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
137639432 163609 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 4 1 8 1.9 COc1nn(C)c2ncnc(NS(=O)(=O)c3ccc(Cl)s3)c12 10.1016/j.bmc.2017.07.052
CHEMBL4071299 163609 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 359 4 1 8 1.9 COc1nn(C)c2ncnc(NS(=O)(=O)c3ccc(Cl)s3)c12 10.1016/j.bmc.2017.07.052
10308962 169822 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1F 10.1021/acsmedchemlett.7b00315
CHEMBL4176082 169822 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 351 4 1 5 2.7 COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1F 10.1021/acsmedchemlett.7b00315
137634526 162708 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 8 2.5 COc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4060967 162708 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 8 2.5 COc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
137632304 163256 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1nn(C)c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4067451 163256 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 385 4 1 5 3.7 COc1nn(C)c2cccc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137647898 164520 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.5 COCCOc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4082318 164520 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 431 7 1 8 2.5 COCCOc1nn(C)c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
137644970 165274 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 5 2 6 2.9 CCOc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
CHEMBL4091069 165274 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 387 5 2 6 2.9 CCOc1n[nH]c2ncnc(NS(=O)(=O)c3cccc(Cl)c3Cl)c12 10.1016/j.bmc.2017.07.052
59168178 169763 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 343 4 1 5 2.0 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.7b00315
CHEMBL4175259 169763 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 343 4 1 5 2.0 COc1nc(Br)cnc1NS(=O)(=O)c1ccccc1 10.1021/acsmedchemlett.7b00315
137637450 162598 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 460 8 2 9 2.5 COCCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
CHEMBL4059913 162598 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay
ChEMBL 460 8 2 9 2.5 COCCNc1nc(NS(=O)(=O)c2cccc(Cl)c2Cl)c2c(OC)nn(C)c2n1 10.1016/j.bmc.2017.07.052
145955548 169391 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 423 5 1 5 4.7 CC(C)(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169258 169391 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay
ChEMBL 423 5 1 5 4.7 CC(C)(C)COc1nc(Cl)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1021/acsmedchemlett.7b00315
134225259 184523 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4642563 184523 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44430315 18638 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL1182360 18638 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233047 18638 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilizationAntagonist activity at human CCR4 expressed in CEMS529 cells assessed as effect on calcium mobilization
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
155548141 180566 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@@H](N4CCCCC4)[C@@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4537681 180566 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@@H](N4CCCCC4)[C@@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
44562155 193410 0 None -19 2 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488018 193410 0 None -19 2 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assayAntagonist activity at mouse CCR4 receptor assessed as inhibition of CCL22-induced chemotaxis by bioluminescent assay
ChEMBL 469 6 1 7 4.7 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(F)c(F)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
134324996 178522 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 540 4 0 6 6.5 CC1CN(c2cnc3c(C(F)(F)F)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
CHEMBL4467274 178522 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by fluorescence assay
ChEMBL 540 4 0 6 6.5 CC1CN(c2cnc3c(C(F)(F)F)nn(C(C)c4ccc(Cl)cc4Cl)c3n2)CCC1N1CCCCC1 10.1021/acs.jmedchem.9b00506
134210954 184589 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643609 184589 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44581042 194612 0 None 6 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL496151 194612 0 None 6 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis
ChEMBL 497 6 2 8 4.5 COc1cc2nc(N3CCC(N4CCCC(O)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
44581102 194551 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
CHEMBL495736 194551 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding
ChEMBL 525 8 2 8 4.6 COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NCc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.11.020
156012782 184143 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637695 184143 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
134210898 184562 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643158 184562 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assayAntagonist activity at human CCR4 expressed in rat chem-5 cells assessed as inhibition of CCL22-induced calcium flux measured at 2.5 secs time interval for 45 secs by calcium 6 dye-based FLIPR assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
59455974 80649 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018961 80649 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation countingAntagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
44562236 193506 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 512 10 1 8 4.9 CCN(CC)CCN1CCCN(c2nc(Nc3ccc(Cl)cc3)c3cc(OC)c(OC)cc3n2)CC1 10.1016/j.bmc.2008.07.062
CHEMBL488690 193506 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 512 10 1 8 4.9 CCN(CC)CCN1CCCN(c2nc(Nc3ccc(Cl)cc3)c3cc(OC)c(OC)cc3n2)CC1 10.1016/j.bmc.2008.07.062
44562190 193355 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 471 8 2 8 3.9 COc1cc2nc(N3CCC(N(C)CCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487836 193355 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assayAntagonist activity at human CCR4 receptor by [35S]GTPgammaS binding assay
ChEMBL 471 8 2 8 3.9 COc1cc2nc(N3CCC(N(C)CCO)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
59455974 80649 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018961 80649 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
59456102 80652 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018964 80652 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
59456003 80639 0 None - 1 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018952 80639 0 None - 1 Human 5.8 pKd = 5.8 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
59456051 80655 0 None - 1 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018967 80655 0 None - 1 Human 5.7 pKd = 5.7 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
9959269 80641 0 None - 1 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
CHEMBL2018954 80641 0 None - 1 Human 6.6 pKd = 6.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
58054516 80646 0 None - 1 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
CHEMBL2018959 80646 0 None - 1 Human 5.6 pKd = 5.6 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
9827294 80640 3 None - 1 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
CHEMBL2018953 80640 3 None - 1 Human 7.3 pKd = 7.3 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
10416 8660 30 None 309 2 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
46861584 8660 30 None 309 2 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
CHEMBL2018969 8660 30 None 309 2 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
59456067 80656 0 None - 1 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018968 80656 0 None - 1 Human 6.2 pKd = 6.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
70685473 80638 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018951 80638 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
70689680 80642 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018955 80642 0 None - 1 Human 5.2 pKd = 5.2 Functional
Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin contentAntagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
49798461 17465 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1170725 17465 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 443 5 1 5 5.3 Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798437 17331 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1169660 17331 0 None - 0 Human 5.8 pKi = 5.8 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 515 8 3 6 4.4 O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
49798349 17563 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171786 17563 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 471 6 2 4 5.9 O=C(O)c1ccccc1Oc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
16124598 17501 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
CHEMBL1171008 17501 0 None - 1 Human 6.1 pKi = 6.1 Functional
Antagonist activity at CCR4Antagonist activity at CCR4
ChEMBL 472 6 2 5 5.3 O=C(O)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2010.04.142
12893 10912 0 None - 1 Human 7.0 pIC50 < 7 Functional
Binned value from patentBinned value from patent
Guide to Pharmacology 565 7 2 6 6.3 CC1=C(C(=NC(=N1)N2CC(C2)[C@H]3CCCN(C3)C4CC(C4)(C)C(=O)O)N[C@H](C)C5=C(C=C(C=C5)Cl)Cl)Cl None
139344142 10912 0 None - 1 Human 7.0 pIC50 < 7 Functional
Binned value from patentBinned value from patent
Guide to Pharmacology 565 7 2 6 6.3 CC1=C(C(=NC(=N1)N2CC(C2)[C@H]3CCCN(C3)C4CC(C4)(C)C(=O)O)N[C@H](C)C5=C(C=C(C=C5)Cl)Cl)Cl None
5280343 195054 124 None -16 12 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL1520590 195054 124 None -16 12 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
CHEMBL50 195054 124 None -16 12 Human 8.3 pIC50 = 8.3 Functional
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
Drug Central 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 None
2812 11551 101 None 3 44 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None 3 44 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
4410 9911 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 9911 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 9911 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 9911 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 9911 106 None -18 6 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
3793 209988 77 None -1 4 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
45039617 209988 77 None -1 4 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
CHEMBL64391 209988 77 None -1 4 Human 8.2 pIC50 = 8.2 Functional
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
Drug Central 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O None
12153 8446 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patentAntagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patent
Guide to Pharmacology 542 6 1 7 4.9 C[C@H](c1c(cc(cc1)Cl)Cl)n1c2nc(cnc2c(n1)C(F)(F)F)N1CC(C1)[C@H]1CCCN(C1)CCO None
134210715 8446 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patentAntagonism of CCL22-induce calcium mobilisation in Chem5-hCCR4 cells- <i>N.B.</i> binned value from patent
Guide to Pharmacology 542 6 1 7 4.9 C[C@H](c1c(cc(cc1)Cl)Cl)n1c2nc(cnc2c(n1)C(F)(F)F)N1CC(C1)[C@H]1CCCN(C1)CCO None
10417 7855 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.
Guide to Pharmacology 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 31259550
134324842 7855 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.
Guide to Pharmacology 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 31259550
CHEMBL4459231 7855 9 None 3 2 Human 7.4 pIC50 = 7.4 Functional
Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.Antagonism of CCL22-induced calcium flux in Chem-5 hCCR4 cells using a high-throughput FLIPR assay.
Guide to Pharmacology 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 31259550
10308720 7333 42 None -2 3 Dog 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 7333 42 None -2 3 Dog 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 7333 42 None -2 3 Dog 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
25141190 7929 28 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
9478 7929 28 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
CHEMBL508207 7929 28 None -1 2 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 19081254
10308720 7333 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 7333 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 7333 42 None -4 3 Human 7.8 pIC50 = 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
10308720 7333 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9678 7333 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4169247 7333 42 None 2 3 Mouse 8.0 pIC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
23585443 7330 12 None -3 3 Dog 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 7330 12 None -3 3 Dog 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 7330 12 None -3 3 Dog 8.5 pIC50 = 8.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
23585443 7330 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 7330 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 7330 12 None -16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
797 7619 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724
23585443 7330 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
9679 7330 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
CHEMBL4172635 7330 12 None 3 3 Mouse 9.0 pIC50 = 9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 28947948
798 7634 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
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selectivity		 # Tested
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 DOI
44410965 83834 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 5 2 4 4.1 CCNCc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207290 83834 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 5 2 4 4.1 CCNCc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44406335 80709 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL202085 80709 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44288732 107946 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(F)cc2F)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL295560 107946 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(F)cc2F)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288854 171840 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42266 171840 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
44288730 172751 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(F)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42523 172751 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(F)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289282 176555 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 617 11 3 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc2[nH]ccc2c1 10.1016/j.bmcl.2004.01.072
CHEMBL44390 176555 0 None - 0 Human 6.0 pIC50 = 6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 617 11 3 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc2[nH]ccc2c1 10.1016/j.bmcl.2004.01.072
5481702 212602 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
CHEMBL83338 212602 1 None - 0 Human 5.0 pIC50 = 5 Binding
Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptor
ChEMBL 556 8 0 4 5.3 CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00639-9
5280343 195054 124 None - 31 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None - 31 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None - 31 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
71720517 93782 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
44288960 170575 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42060 170575 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1Cl 10.1016/j.bmcl.2004.01.072
44400830 78010 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 10 1 4 5.1 CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195665 78010 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 10 1 4 5.1 CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
5280343 195054 124 None - 31 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None - 31 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None - 31 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
44288899 108042 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 13 2 6 3.6 O=C(C[C@H]1S[C@H](CCc2ccccc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL296245 108042 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 13 2 6 3.6 O=C(C[C@H]1S[C@H](CCc2ccccc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288863 168850 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 6 3.5 O=C(C[C@H]1S[C@H](C2CCCCC2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL416069 168850 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 6 3.5 O=C(C[C@H]1S[C@H](C2CCCCC2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289207 174970 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 633 9 1 5 6.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(Cc2cccc(CN3CCOCC3)c2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43330 174970 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 633 9 1 5 6.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(Cc2cccc(CN3CCOCC3)c2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288557 177063 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccoc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44463 177063 0 None - 0 Human 4.0 pIC50 = 4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccoc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
5280343 195054 124 None - 31 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 195054 124 None - 31 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 195054 124 None - 31 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
134211221 184467 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4641873 184467 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 502 7 1 7 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
45104526 207488 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 479 3 3 7 3.8 Cc1c(N2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL599995 207488 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 479 3 3 7 3.8 Cc1c(N2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
44288959 172086 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42334 172086 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 640 11 2 5 6.3 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44430304 158901 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2c(ncn2CC)n1 10.1016/j.bmcl.2006.10.091
CHEMBL396786 158901 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2c(ncn2CC)n1 10.1016/j.bmcl.2006.10.091
11285792 7666 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
801 7666 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
CHEMBL2110727 7666 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
DB11758 7666 34 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells
ChEMBL 696 17 1 7 8.7 CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC 10.1021/jm0509703
44288962 107250 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 10 2 5 4.5 CN(C)CC(=O)NCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL290845 107250 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 10 2 5 4.5 CN(C)CC(=O)NCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44288985 162321 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 668 14 2 9 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1OC 10.1016/j.bmcl.2004.01.072
CHEMBL40427 162321 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 668 14 2 9 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1OC 10.1016/j.bmcl.2004.01.072
44288961 162410 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1ccccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL40468 162410 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1ccccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
44289214 164082 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40771 164082 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288776 173098 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 10 2 8 3.3 O=C(CN1C(=O)[C@@H](CC(=O)Nc2nccs2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL42722 173098 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 10 2 8 3.3 O=C(CN1C(=O)[C@@H](CC(=O)Nc2nccs2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44288731 177118 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 11 2 6 3.9 Cc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(C)c1 10.1016/j.bmcl.2004.01.072
CHEMBL44472 177118 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 588 11 2 6 3.9 Cc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(C)c1 10.1016/j.bmcl.2004.01.072
44288963 177759 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 11 2 7 3.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccs1 10.1016/j.bmcl.2004.01.072
CHEMBL44561 177759 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 11 2 7 3.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccs1 10.1016/j.bmcl.2004.01.072
45104751 207697 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 1 1 5 1.9 Cc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL601651 207697 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 1 1 5 1.9 Cc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
3793 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
134210626 184084 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4636749 184084 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 593 9 1 8 4.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(=O)(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
155557193 181304 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
CHEMBL4555534 181304 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 538 5 1 7 6.0 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(C)(C)O 10.1021/acs.jmedchem.9b00506
44561588 201332 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL529664 201332 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44406247 147975 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 463 5 0 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(OCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
CHEMBL382826 147975 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 463 5 0 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(OCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
71454500 85767 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113068 85767 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2Cl)c1 10.1016/j.bmcl.2005.02.084
44289275 108290 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL298035 108290 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
44289277 170282 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)ccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42021 170282 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)ccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289072 176119 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.3 O=C(C[C@H]1S[C@H](c2cccc(C(F)(F)F)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44187 176119 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.3 O=C(C[C@H]1S[C@H](c2cccc(C(F)(F)F)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44411038 83575 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 471 8 1 4 7.6 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)no2)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL206921 83575 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 471 8 1 4 7.6 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)no2)c1C 10.1016/j.bmcl.2006.01.126
3793 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 4.9 pIC50 = 4.9 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44289062 170438 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42044 170438 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(-c2ccccc2)c1 10.1016/j.bmcl.2004.01.072
44289064 177710 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 660 12 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2004.01.072
CHEMBL44553 177710 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 660 12 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCCc1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2004.01.072
45104634 207515 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 2 6 1.7 CCN1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
CHEMBL600196 207515 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 2 6 1.7 CCN1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
45104523 208490 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 437 3 3 6 4.0 Cc1c(N2CCN(C(=O)Nc3ccc(C(C)C)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL606421 208490 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 437 3 3 6 4.0 Cc1c(N2CCN(C(=O)Nc3ccc(C(C)C)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
134225247 184442 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641595 184442 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 4.6 COC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
134210845 184828 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647188 184828 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 565 8 1 8 3.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
155540774 179293 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
CHEMBL4483537 179293 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 523 5 1 7 4.7 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C(N)=O 10.1021/acs.jmedchem.9b00506
44411321 145203 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 509 8 1 4 8.6 FC(F)(F)c1ccccc1CN(Cc1csc(Nc2cccc3ccccc23)n1)CC1CCCCC1 10.1016/j.bmcl.2006.01.126
CHEMBL377421 145203 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 509 8 1 4 8.6 FC(F)(F)c1ccccc1CN(Cc1csc(Nc2cccc3ccccc23)n1)CC1CCCCC1 10.1016/j.bmcl.2006.01.126
44430311 159159 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 460 11 2 6 5.9 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2cccnc2n1 10.1016/j.bmcl.2006.10.091
CHEMBL397028 159159 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 460 11 2 6 5.9 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2cccnc2n1 10.1016/j.bmcl.2006.10.091
44288958 175506 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL43698 175506 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 624 11 2 5 5.6 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O 10.1016/j.bmcl.2004.01.072
44288981 172336 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 7 2 5 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42419 172336 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 7 2 5 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
25141301 192667 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL486840 192667 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 467 6 1 7 5.1 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC 10.1016/j.bmc.2008.07.062
156015374 184394 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4640909 184394 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 6 0 7 5.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(F)(F)F)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44411492 145674 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3cnccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL378272 145674 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3cnccc23)n1 10.1016/j.bmcl.2006.01.126
44288943 171408 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42162 171408 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)cc(Cl)c1 10.1016/j.bmcl.2004.01.072
44288913 176069 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(F)c1 10.1016/j.bmcl.2004.01.072
CHEMBL44143 176069 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 596 11 2 6 3.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(F)c1 10.1016/j.bmcl.2004.01.072
44401027 77327 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL194775 77327 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
134325041 181811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4567398 181811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 502 5 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
45104946 207499 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 371 5 0 6 2.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCC3)ccc12 10.1021/jm901652p
CHEMBL600018 207499 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 371 5 0 6 2.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCC3)ccc12 10.1021/jm901652p
45104635 207516 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 420 2 2 6 3.9 Cc1c(N2CCN(c3cccc(C(F)(F)F)c3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL600197 207516 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 420 2 2 6 3.9 Cc1c(N2CCN(c3cccc(C(F)(F)F)c3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
45104422 208011 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 406 3 2 6 2.9 Cc1c(N2CCN(C(=O)/C=C/c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL603701 208011 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 406 3 2 6 2.9 Cc1c(N2CCN(C(=O)/C=C/c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
45104527 207489 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 409 3 3 6 2.5 Cc1c(N2CCN(C(=O)NCc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL599996 207489 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 409 3 3 6 2.5 Cc1c(N2CCN(C(=O)NCc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
2812 11551 101 None - 34 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
CHEMBL104 11551 101 None - 34 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 10.1021/jm301749y
71720517 93782 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
45104848 207874 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 3 0 5 2.3 CCOc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL602887 207874 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 3 0 5 2.3 CCOc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
10417 7855 9 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
134324842 7855 9 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
CHEMBL4459231 7855 9 None - 0 Mouse 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
9814022 83886 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 268 3 1 3 5.2 CC(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207589 83886 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 268 3 1 3 5.2 CC(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
692856 148141 19 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL383736 148141 19 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
71461653 85765 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccccc2Cl)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113066 85765 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccccc2Cl)c1 10.1016/j.bmcl.2005.02.084
134335393 176891 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4443688 176891 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 499 5 1 6 5.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(C3=CC[C@H](N4CCC[C@H]4CO)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
11496063 83894 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
CHEMBL207642 83894 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
44288978 175515 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 585 10 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43706 175515 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 585 10 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288827 175580 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43758 175580 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
71458049 85774 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 359 11 1 4 4.7 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(F)cc2)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113075 85774 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 359 11 1 4 4.7 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(F)cc2)c1 10.1016/j.bmcl.2005.02.084
44561561 185780 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL470962 185780 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 439 6 1 7 4.5 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44288791 106972 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 12 2 6 3.3 CC(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL288256 106972 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 12 2 6 3.3 CC(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
44430309 93999 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ccccc12 10.1016/j.bmcl.2006.10.091
CHEMBL232841 93999 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ccccc12 10.1016/j.bmcl.2006.10.091
134325106 178030 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4460062 178030 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 500 4 0 6 6.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
45104945 207498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 385 5 0 6 2.7 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCCC3)ccc12 10.1021/jm901652p
CHEMBL600017 207498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 385 5 0 6 2.7 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCCCC3)ccc12 10.1021/jm901652p
44430312 94035 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL233046 94035 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 499 5 2 7 3.7 O=C([C@@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
44288880 108335 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 5 5.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL298454 108335 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 5 5.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
3793 209988 77 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22Inverse agonist activity at CCR4 in human HTLA cells assessed as depression of basal activity incubated for 20 mins by beta arrestin-recruitment mediated luciferase reporter gene assay in absence of CCL22
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44411325 175657 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1 10.1016/j.bmcl.2006.01.126
CHEMBL438248 175657 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1 10.1016/j.bmcl.2006.01.126
44288879 176122 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL44188 176122 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44400833 77482 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 392 11 1 5 5.1 CCN(CC)CCCC(C)Nc1nc(COc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195061 77482 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 392 11 1 5 5.1 CCN(CC)CCCC(C)Nc1nc(COc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
44401066 133193 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CN(C)CCCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL365155 133193 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CN(C)CCCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44289208 170625 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 7 1 5 4.6 CN1CCN(C(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
CHEMBL42065 170625 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 7 1 5 4.6 CN1CCN(C(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
71452724 85771 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113072 85771 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 375 11 1 4 5.2 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)cc2)c1 10.1016/j.bmcl.2005.02.084
45104633 207180 22 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 290 1 2 6 1.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL598070 207180 22 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 290 1 2 6 1.3 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
9943773 84079 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 286 2 1 3 5.1 CC(C)(C)c1csc(Nc2cccc3c2CCCC3)n1 10.1016/j.bmcl.2006.01.126
CHEMBL208249 84079 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 286 2 1 3 5.1 CC(C)(C)c1csc(Nc2cccc3c2CCCC3)n1 10.1016/j.bmcl.2006.01.126
44411033 84124 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 299 3 1 4 5.2 CCn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
CHEMBL208458 84124 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 299 3 1 4 5.2 CCn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
44430302 93893 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2nc[nH]c12 10.1016/j.bmcl.2006.10.091
CHEMBL232639 93893 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2nc[nH]c12 10.1016/j.bmcl.2006.10.091
44289116 176059 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 11 2 6 3.7 CC(C)(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL44134 176059 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 572 11 2 6 3.7 CC(C)(C)CCNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
176 7186 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -6 31 Human 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
134324891 181346 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4556507 181346 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 458 4 0 6 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
9922232 172538 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 296 3 1 3 5.6 CC(C)(C)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL424689 172538 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 296 3 1 3 5.6 CC(C)(C)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44289186 171861 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42270 171861 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 3.8 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1 10.1016/j.bmcl.2004.01.072
44289105 105208 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 656 13 2 6 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL275593 105208 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 656 13 2 6 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288818 162191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40366 162191 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44400899 77358 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 390 11 1 4 5.3 CCN(CC)CCCC(C)Nc1nc(CCc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL194930 77358 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 390 11 1 4 5.3 CCN(CC)CCCC(C)Nc1nc(CCc2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
44288912 172864 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 678 13 2 7 4.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCNS(=O)(=O)CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42586 172864 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 678 13 2 7 4.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCNS(=O)(=O)CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134211126 184348 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4640439 184348 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 515 7 1 7 4.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(N)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
10308720 7333 42 None - 0 Dog 7.6 pIC50 = 7.6 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9678 7333 42 None - 0 Dog 7.6 pIC50 = 7.6 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4169247 7333 42 None - 0 Dog 7.6 pIC50 = 7.6 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 333 4 1 5 2.6 COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
44289241 107190 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL290201 107190 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288996 176139 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL44198 176139 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
44289039 107019 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.01.072
CHEMBL288655 107019 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(-c2ccccc2)cc1 10.1016/j.bmcl.2004.01.072
44289340 108024 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 664 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2004.01.072
CHEMBL296152 108024 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 664 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1F 10.1016/j.bmcl.2004.01.072
44288911 174703 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 595 11 2 7 3.1 Cc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)n1C 10.1016/j.bmcl.2004.01.072
CHEMBL43143 174703 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 595 11 2 7 3.1 Cc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)n1C 10.1016/j.bmcl.2004.01.072
44400829 78092 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 412 9 1 4 6.4 CCN(CC)CCCC(C)Nc1nc(-c2ccc3ccccc3c2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195751 78092 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 412 9 1 4 6.4 CCN(CC)CCCC(C)Nc1nc(-c2ccc3ccccc3c2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
44400922 75425 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 11 1 5 4.6 CCN(CC)CCCC(C)Nc1ccnc(COc2cccc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
CHEMBL191915 75425 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 376 11 1 5 4.6 CCN(CC)CCCC(C)Nc1ccnc(COc2cccc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
44400881 78180 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(COc2cc(Cl)cc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195893 78180 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(COc2cc(Cl)cc(Cl)c2)n1 10.1016/j.bmcl.2005.02.084
45104427 207628 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 473 4 3 8 2.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)cc1 10.1021/jm901652p
CHEMBL601217 207628 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 473 4 3 8 2.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)cc1 10.1021/jm901652p
134325076 178964 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4473604 178964 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 579 7 1 8 4.4 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCS(N)(=O)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134211098 184823 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4647117 184823 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 564 8 0 8 4.6 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
9856506 83533 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 260 2 1 3 4.8 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL206789 83533 4 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 260 2 1 3 4.8 Cc1cccc(Nc2nc(C(C)(C)C)cs2)c1C 10.1016/j.bmcl.2006.01.126
44430305 93896 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ncn(CC)c12 10.1016/j.bmcl.2006.10.091
CHEMBL232641 93896 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 477 12 2 7 5.7 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)nc2ncn(CC)c12 10.1016/j.bmcl.2006.10.091
11223594 77859 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195298 77859 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 2 5 5.3 CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44430315 18638 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL1182360 18638 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233047 18638 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 409 11 2 5 5.3 CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
44430308 158904 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 433 10 1 5 5.7 CCN(CC)CCCC(C)Nc1ccc2cnn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
CHEMBL396787 158904 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 433 10 1 5 5.7 CCN(CC)CCCC(C)Nc1ccc2cnn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
44401007 77615 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195103 77615 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 410 11 1 5 5.3 CCN(CC)CCCC(C)Nc1ccnc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44289401 170224 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 604 10 2 6 4.0 O=C(CN1C(=O)[C@@H](CC(=O)N[C@@H]2CCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL41983 170224 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 604 10 2 6 4.0 O=C(CN1C(=O)[C@@H](CC(=O)N[C@@H]2CCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44289082 173351 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccco2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42799 173351 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 550 11 2 7 2.9 O=C(C[C@H]1S[C@H](c2ccco2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
23585443 7330 12 None - 0 Dog 8.5 pIC50 = 8.5 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9679 7330 12 None - 0 Dog 8.5 pIC50 = 8.5 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
CHEMBL4172635 7330 12 None - 0 Dog 8.5 pIC50 = 8.5 Binding
Antagonist activity at dog CCR4Antagonist activity at dog CCR4
ChEMBL 351 4 1 5 2.7 COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl 10.1021/acsmedchemlett.7b00315
9900444 83936 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3ncccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207857 83936 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 283 2 1 4 4.7 CC(C)(C)c1csc(Nc2cccc3ncccc23)n1 10.1016/j.bmcl.2006.01.126
44406309 140314 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3ccnc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
CHEMBL370861 140314 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3ccnc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
692856 148141 19 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL383736 148141 19 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 240 2 1 3 4.3 Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44288879 176122 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL44188 176122 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44400947 78097 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 396 11 1 5 4.9 CCN(CC)CCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195764 78097 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 396 11 1 5 4.9 CCN(CC)CCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
11496063 83894 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
CHEMBL207642 83894 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]MDC from CCR4 expressed in human CEM cell lineDisplacement of [125I]MDC from CCR4 expressed in human CEM cell line
ChEMBL 447 8 1 4 8.0 c1ccc2c(Nc3nc(CN(CC4CCCCC4)CC4CCCCC4)cs3)cccc2c1 10.1016/j.bmcl.2006.01.126
44288903 173160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 5 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42757 173160 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 5 5.4 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
45104849 209302 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 4 0 5 4.2 CCC1CCC(Oc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)CC1 10.1021/jm901652p
CHEMBL611508 209302 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 4 0 5 4.2 CCC1CCC(Oc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)CC1 10.1021/jm901652p
45104748 207816 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 3.5 Cc1cccc(N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)c1C 10.1021/jm901652p
CHEMBL602474 207816 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 3.5 Cc1cccc(N2CCN(c3c(C)c4c(O)cc(O)cc4oc3=O)CC2)c1C 10.1021/jm901652p
44289098 108163 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 13 2 8 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1 10.1016/j.bmcl.2004.01.072
CHEMBL297173 108163 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 13 2 8 3.5 COc1ccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c(OC)c1 10.1016/j.bmcl.2004.01.072
134335394 179121 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
CHEMBL4475665 179121 0 None - 0 Mouse 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in anti-CD3/CD28 stimulated mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
134225255 184104 10 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 184104 10 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44289027 108009 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 652 8 1 5 6.3 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL296067 108009 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 652 8 1 5 6.3 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288779 108190 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 9 1 5 5.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL297335 108190 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 571 9 1 5 5.5 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289036 169885 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2cccs2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL417712 169885 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2cccs2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289106 172305 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 620 13 2 8 3.3 COc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(OC)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42411 172305 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 620 13 2 8 3.3 COc1ccc([C@H]2S[C@H](CC(=O)NCc3cccc4ccccc34)C(=O)N2CC(=O)NCCCN2CCOCC2)c(OC)c1 10.1016/j.bmcl.2004.01.072
21866580 83921 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 481 8 1 3 8.0 Cc1cccc(Nc2cccc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)n2)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL207780 83921 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 481 8 1 3 8.0 Cc1cccc(Nc2cccc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)n2)c1C 10.1016/j.bmcl.2006.01.126
44289276 174705 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 634 11 2 7 4.7 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1csc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43144 174705 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 634 11 2 7 4.7 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1csc2ccccc12 10.1016/j.bmcl.2004.01.072
44288726 176218 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 561 11 2 7 2.7 O=C(C[C@H]1S[C@H](c2ccncc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44262 176218 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 561 11 2 7 2.7 O=C(C[C@H]1S[C@H](c2ccncc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
71720517 93782 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
44289235 108157 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 8 2 5 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL297145 108157 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 584 8 2 5 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCC(=O)N2CCNCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289204 176628 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 614 10 2 6 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44401 176628 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 614 10 2 6 4.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134325003 182161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4575089 182161 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 543 7 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC(N)=O)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
134225259 184523 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4642563 184523 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 517 7 2 8 3.0 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(N)=O)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44288904 171447 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 586 11 2 5 4.9 CN(C)CCCNC(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42168 171447 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 586 11 2 5 4.9 CN(C)CCCNC(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44289227 176214 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 600 11 1 5 5.2 CN(C)CCCN(C)C(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL44259 176214 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 600 11 1 5 5.2 CN(C)CCCN(C)C(=O)CN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44430317 94117 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 439 12 3 7 4.8 CCN(CC)CCCC(C)Nc1nc(NC)nc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL233261 94117 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 439 12 3 7 4.8 CCN(CC)CCCC(C)Nc1nc(NC)nc(NCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
44288898 175467 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 515 8 1 4 5.4 CN(C)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL43661 175467 0 None - 0 Human 4.4 pIC50 = 4.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 515 8 1 4 5.4 CN(C)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
155531126 178386 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4465359 178386 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCCCC4)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
21866577 82740 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 285 2 1 4 4.7 Cn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
CHEMBL205279 82740 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 285 2 1 4 4.7 Cn1ccc2c(Nc3nc(C(C)(C)C)cs3)cccc21 10.1016/j.bmcl.2006.01.126
134210898 184562 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643158 184562 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 516 7 1 7 4.7 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44411191 147017 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 484 8 1 4 7.4 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)nn2C)c1C 10.1016/j.bmcl.2006.01.126
CHEMBL380537 147017 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 484 8 1 4 7.4 Cc1cccc(Nc2cc(CN(Cc3ccccc3C(F)(F)F)CC3CCCCC3)nn2C)c1C 10.1016/j.bmcl.2006.01.126
156012782 184143 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637695 184143 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 545 7 1 8 3.6 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C(=O)N(C)C)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44289203 177313 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 12 2 6 5.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL44498 177313 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 12 2 6 5.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134324973 177166 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4447900 177166 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 486 4 0 6 5.8 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4C)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
45104844 207699 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 1 6 1.6 COc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL601653 207699 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 304 2 1 6 1.6 COc1cc(O)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
134225255 184104 10 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assayAntagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 184104 10 None - 0 Mouse 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assayAntagonist activity at CCR4 in mouse Treg cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% mouse serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
71720517 93782 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
134211057 184404 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
CHEMBL4641127 184404 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 529 7 1 7 4.3 CC(=O)NCCN1CCC[C@H](C2CN(c3cnc4c(C)nn([C@H](C)c5ccc(Cl)cc5Cl)c4n3)C2)C1 10.1021/acs.jmedchem.0c00988
44289341 170252 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 6 4.4 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
CHEMBL42001 170252 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 626 11 2 6 4.4 Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O 10.1016/j.bmcl.2004.01.072
44288923 170447 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)ccc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42046 170447 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cc(Cl)ccc1Cl 10.1016/j.bmcl.2004.01.072
44288683 175849 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 578 11 2 6 3.5 O=C(C[C@H]1S[C@H](c2ccc(F)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43969 175849 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 578 11 2 6 3.5 O=C(C[C@H]1S[C@H](c2ccc(F)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
71449124 85768 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.02.084
CHEMBL2113069 85768 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 409 11 1 4 5.9 CCN(CC)CCCC(C)Nc1ccnc(COc2ccc(Cl)c(Cl)c2)c1 10.1016/j.bmcl.2005.02.084
134336138 184274 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639418 184274 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 527 7 1 8 4.2 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
45104752 208362 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 1 0 6 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc3c(cc12)OCO3 10.1021/jm901652p
CHEMBL605581 208362 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 302 1 0 6 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc3c(cc12)OCO3 10.1021/jm901652p
45104423 207698 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 330 2 2 6 1.3 C=CC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
CHEMBL601652 207698 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 330 2 2 6 1.3 C=CC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
45104321 207500 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 276 1 3 6 0.9 Cc1c(N2CCNCC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL600019 207500 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 276 1 3 6 0.9 Cc1c(N2CCNCC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
45104425 207658 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 2.5 Cc1c(N2CCN(C(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL601424 207658 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 380 2 2 6 2.5 Cc1c(N2CCN(C(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
134335394 179121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
CHEMBL4475665 179121 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 494 4 0 6 6.3 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1C 10.1021/acs.jmedchem.9b00506
44411266 83532 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 274 3 1 3 5.3 CC(C)c1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
CHEMBL206788 83532 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 274 3 1 3 5.3 CC(C)c1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
44289342 172891 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 606 11 2 6 4.1 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1C 10.1016/j.bmcl.2004.01.072
CHEMBL42600 172891 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 606 11 2 6 4.1 Cc1cccc(CNC(=O)C[C@H]2S[C@H](c3ccc(Cl)cc3Cl)N(CC(=O)NCCCN3CCOCC3)C2=O)c1C 10.1016/j.bmcl.2004.01.072
156010350 183861 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633133 183861 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 531 7 2 8 3.2 CNC(=O)c1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
10133595 83843 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 367 8 1 4 6.2 CC(C)CN(Cc1csc(Nc2cccc3ccccc23)n1)CC(C)C 10.1016/j.bmcl.2006.01.126
CHEMBL207320 83843 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 367 8 1 4 6.2 CC(C)CN(Cc1csc(Nc2cccc3ccccc23)n1)CC(C)C 10.1016/j.bmcl.2006.01.126
9899450 83314 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 232 2 1 3 4.2 CC(C)(C)c1csc(Nc2ccccc2)n1 10.1016/j.bmcl.2006.01.126
CHEMBL206103 83314 1 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 232 2 1 3 4.2 CC(C)(C)c1csc(Nc2ccccc2)n1 10.1016/j.bmcl.2006.01.126
45104846 207541 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 301 2 0 5 1.9 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(N(C)C)ccc12 10.1021/jm901652p
CHEMBL600409 207541 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 301 2 0 5 1.9 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(N(C)C)ccc12 10.1021/jm901652p
45104845 205953 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 318 3 0 6 1.9 COc1cc(OC)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL589521 205953 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 318 3 0 6 1.9 COc1cc(OC)c2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
21866574 83865 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 271 2 2 3 4.7 CC(C)(C)c1csc(Nc2cccc3[nH]ccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL207479 83865 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 271 2 2 3 4.7 CC(C)(C)c1csc(Nc2cccc3[nH]ccc23)n1 10.1016/j.bmcl.2006.01.126
44430303 93895 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2[nH]cnc2n1 10.1016/j.bmcl.2006.10.091
CHEMBL232640 93895 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 449 11 3 6 5.2 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2[nH]cnc2n1 10.1016/j.bmcl.2006.10.091
134225255 184104 10 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 184104 10 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
11525206 142006 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL372399 142006 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2006.10.091
11525206 142006 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL372399 142006 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44430310 94034 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2ccccc2n1 10.1016/j.bmcl.2006.10.091
CHEMBL233045 94034 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 459 11 2 5 6.5 CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2ccccc2n1 10.1016/j.bmcl.2006.10.091
3793 209988 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
3793 209988 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 6.3 pIC50 = 6.3 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44562156 193508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL488704 193508 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 511 6 1 7 5.2 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(Nc3cccc(Br)c3)c2cc1OC 10.1016/j.bmc.2008.07.062
45104847 207215 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 2 0 5 1.9 COc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
CHEMBL598339 207215 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 288 2 0 5 1.9 COc1ccc2c(C)c(N3CCN(C)CC3)c(=O)oc2c1 10.1021/jm901652p
156010372 183887 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4633494 183887 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 508 6 0 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCC#N)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
45104943 207903 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 5 0 6 3.5 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCc3cccs3)ccc12 10.1021/jm901652p
CHEMBL603104 207903 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 384 5 0 6 3.5 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCc3cccs3)ccc12 10.1021/jm901652p
45104524 207587 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 417 7 3 6 3.3 CCCCCCCNC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
CHEMBL600805 207587 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 417 7 3 6 3.3 CCCCCCCNC(=O)N1CCN(c2c(C)c3c(O)cc(O)cc3oc2=O)CC1 10.1021/jm901652p
4015979 84122 3 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 302 3 1 3 5.7 c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
CHEMBL208452 84122 3 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 302 3 1 3 5.7 c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
134210768 184233 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4638846 184233 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 530 8 1 7 5.1 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCC(=O)O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44406246 79801 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 479 9 2 6 4.3 CC(C)[C@@H](CNc1nccc(OCc2ccc(Cl)cc2Cl)n1)NC(=O)C1CCCN(C)C1 10.1016/j.bmcl.2005.09.022
CHEMBL200966 79801 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 479 9 2 6 4.3 CC(C)[C@@H](CNc1nccc(OCc2ccc(Cl)cc2Cl)n1)NC(=O)C1CCCN(C)C1 10.1016/j.bmcl.2005.09.022
44288897 108263 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 529 9 1 4 5.7 CN(C)CCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL297854 108263 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 529 9 1 4 5.7 CN(C)CCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44288663 107036 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 641 11 2 6 4.5 CN1CCN(CCCNC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
CHEMBL288800 107036 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 641 11 2 6 4.5 CN1CCN(CCCNC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
156010600 183917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4633920 183917 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 550 7 0 8 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(C)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
134325016 181432 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
CHEMBL4558456 181432 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 513 5 1 8 4.3 C[C@@H]1CN(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)CC[C@@H]1N1CCC[C@H]1CO 10.1021/acs.jmedchem.9b00506
45104747 207794 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 370 2 2 6 3.0 Cc1c(N2CCN(c3ccc(F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL602269 207794 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 370 2 2 6 3.0 Cc1c(N2CCN(c3ccc(F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
134211225 184704 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4645325 184704 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 557 8 1 7 5.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCNC(=O)C(C)C)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
44406338 79697 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 434 5 2 6 2.8 O=C([C@H]1CCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL200465 79697 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 434 5 2 6 2.8 O=C([C@H]1CCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44288972 173211 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 8 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42774 173211 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 638 8 1 5 5.9 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)N2CCC(N3CCCC3)CC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
45104525 208121 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 487 4 3 7 4.7 Cc1c(N2CCN(C(=O)Nc3ccccc3Oc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL604330 208121 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 487 4 3 7 4.7 Cc1c(N2CCN(C(=O)Nc3ccccc3Oc3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
44289283 108031 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(CN1C(=O)[C@@H](CC(=O)NC(c2ccccc2)c2ccccc2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL296192 108031 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(CN1C(=O)[C@@H](CC(=O)NC(c2ccccc2)c2ccccc2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44289063 168750 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL415902 168750 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 654 12 2 6 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1-c1ccccc1 10.1016/j.bmcl.2004.01.072
44289097 185404 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 680 11 2 6 5.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
CHEMBL46748 185404 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 680 11 2 6 5.2 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc(Cl)c(C(F)(F)F)c1 10.1016/j.bmcl.2004.01.072
45104426 208633 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 416 3 2 7 2.0 Cc1c(N2CCN(S(=O)(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL607137 208633 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 416 3 2 7 2.0 Cc1c(N2CCN(S(=O)(=O)c3ccccc3)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
44401118 77845 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uMInhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uM
ChEMBL 388 10 1 4 5.7 CCN(CC)CCCC(C)Nc1nc(/C=C/c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
CHEMBL195203 77845 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uMInhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uM
ChEMBL 388 10 1 4 5.7 CCN(CC)CCCC(C)Nc1nc(/C=C/c2ccccc2)nc2ccccc12 10.1016/j.bmcl.2005.02.084
134324770 177722 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
CHEMBL4455432 177722 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 509 5 1 7 5.2 C[C@@H]1CC(c2cnc3c(C#N)nn([C@H](C)c4ccc(Cl)cc4Cl)c3n2)=CC[C@@H]1N1CCC[C@H]1CN 10.1021/acs.jmedchem.9b00506
134225255 184104 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4637143 184104 10 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL17-mediated chemotaxis preincubated for 30 mins followed by CCL17 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 499 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CCO)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
44561217 195895 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL510375 195895 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCN(C(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44289057 172121 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2ccsc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42360 172121 0 None - 0 Human 4.2 pIC50 = 4.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 566 11 2 7 3.4 O=C(C[C@H]1S[C@H](c2ccsc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289281 107880 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 618 10 2 6 4.4 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL295057 107880 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 618 10 2 6 4.4 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCc3ccccc32)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
45104944 207497 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 387 5 0 7 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCOCC3)ccc12 10.1021/jm901652p
CHEMBL600016 207497 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 387 5 0 7 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(OCCN3CCOCC3)ccc12 10.1021/jm901652p
44288799 108309 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL298230 108309 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
10417 7855 9 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
134324842 7855 9 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
CHEMBL4459231 7855 9 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 510 5 1 7 5.3 OC[C@@H]1CCCN1[C@H]1CC=C(C[C@H]1C)c1cnc2c(n1)n(nc2C#N)[C@@H](c1ccc(cc1Cl)Cl)C 10.1021/acs.jmedchem.9b00506
16724339 193216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
CHEMBL487635 193216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assayDisplacement of [121I]CCL22 from human CCR4 receptor by scintillation proximity assay
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.07.062
16724339 193216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL487635 193216 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 453 6 1 7 4.8 COc1cc2nc(N3CCC(N4CCCC4)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
44406282 79479 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
CHEMBL199733 79479 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 462 5 1 6 3.4 CN1CCCC(C(=O)N2CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.bmcl.2005.09.022
44289055 107136 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 568 11 2 7 3.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccco1 10.1016/j.bmcl.2004.01.072
CHEMBL289661 107136 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 568 11 2 7 3.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccco1 10.1016/j.bmcl.2004.01.072
44288575 161961 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 10 2 6 3.6 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCCC2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
CHEMBL40238 161961 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 570 10 2 6 3.6 O=C(CN1C(=O)[C@@H](CC(=O)NC2CCCCC2)S[C@@H]1c1ccc(Cl)cc1Cl)NCCCN1CCOCC1 10.1016/j.bmcl.2004.01.072
44288698 175872 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43988 175872 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2cccc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
134210954 184589 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4643609 184589 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 551 7 1 8 3.5 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCS(N)(=O)=O)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
3793 209988 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
25141190 7929 28 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
9478 7929 28 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
CHEMBL508207 7929 28 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 467 6 1 7 5.2 COc1cc2c(NC3CCCCCC3)nc(nc2cc1OC)N1CCC(CC1)N1CCCCC1 10.1016/j.bmc.2008.05.036
44561137 193498 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
CHEMBL488640 193498 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPADisplacement of [125I]CCl22 from human CCR4 receptor expressed in mouse B300-19 cells by SPA
ChEMBL 427 6 1 7 4.3 COc1cc2nc(N3CCC(N(C)C)CC3)nc(NC3CCCCCC3)c2cc1OC 10.1016/j.bmc.2008.05.036
45104850 207875 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 394 5 0 6 3.4 COc1ccc(COc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)cc1 10.1021/jm901652p
CHEMBL602888 207875 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 394 5 0 6 3.4 COc1ccc(COc2ccc3c(C)c(N4CCN(C)CC4)c(=O)oc3c2)cc1 10.1021/jm901652p
134211185 183932 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
CHEMBL4634054 183932 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 488 6 1 7 4.2 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCO)C4)C3)cnc12 10.1021/acs.jmedchem.0c00988
156018849 184686 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4645037 184686 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 513 6 1 8 3.8 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(CC(=O)O)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
45104750 207696 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 274 1 1 5 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)ccc12 10.1021/jm901652p
CHEMBL601650 207696 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 274 1 1 5 1.6 Cc1c(N2CCN(C)CC2)c(=O)oc2cc(O)ccc12 10.1021/jm901652p
44289343 172640 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42491 172640 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 646 11 2 6 4.8 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1Cl 10.1016/j.bmcl.2004.01.072
3793 209988 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
45039617 209988 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
CHEMBL64391 209988 77 None - 1 Human 5.1 pIC50 = 5.1 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 704 11 0 12 5.6 CCC(C)n1ncn(-c2ccc(N3CCN(c4ccc(OCC5COC(Cn6cncn6)(c6ccc(Cl)cc6Cl)O5)cc4)CC3)cc2)c1=O 10.1021/jm301749y
44430313 156580 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 485 5 2 7 3.3 O=C([C@@H]1CCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
CHEMBL394859 156580 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 485 5 2 7 3.3 O=C([C@@H]1CCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2006.10.091
44411037 83558 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 266 2 1 3 4.9 CC(C)(C)c1coc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL206878 83558 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 266 2 1 3 4.9 CC(C)(C)c1coc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
9814340 146287 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 282 2 1 3 5.3 CC(C)(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL379460 146287 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 282 2 1 3 5.3 CC(C)(C)c1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44410966 175821 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 311 6 1 4 4.9 CCN(CC)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
CHEMBL439518 175821 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 311 6 1 4 4.9 CCN(CC)Cc1csc(Nc2cccc3ccccc23)n1 10.1016/j.bmcl.2006.01.126
44406355 79539 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.0 O=C(C1CCCNC1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
CHEMBL199913 79539 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells
ChEMBL 448 5 2 6 3.0 O=C(C1CCCNC1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.bmcl.2005.09.022
44288828 107234 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2c(Cl)cccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL290678 107234 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2c(Cl)cccc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289242 162214 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40377 162214 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 642 11 2 6 5.2 C[C@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44289205 169949 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 598 8 2 5 5.0 CN1CCC(NC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
CHEMBL418072 169949 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 598 8 2 5 5.0 CN1CCC(NC(=O)CN2C(=O)[C@@H](CC(=O)NCc3cccc4ccccc34)S[C@@H]2c2ccc(Cl)cc2Cl)CC1 10.1016/j.bmcl.2004.01.072
44288996 176139 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
CHEMBL44198 176139 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 592 11 2 6 4.0 C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)c1ccccc1 10.1016/j.bmcl.2004.01.072
44401087 77901 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CCN(CC)CCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL195484 77901 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 382 10 1 5 4.5 CCN(CC)CCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44430306 93997 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2ncn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
CHEMBL232839 93997 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2ncn(Cc3ccc(Cl)cc3Cl)c2n1 10.1016/j.bmcl.2006.10.091
44430307 93998 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2c(ncn2Cc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
CHEMBL232840 93998 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells
ChEMBL 434 10 1 6 5.1 CCN(CC)CCCC(C)Nc1ncc2c(ncn2Cc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2006.10.091
44288818 162191 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL40366 162191 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(CC1SC(c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288682 172863 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL42585 172863 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 594 11 2 6 4.0 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
3117 214620 103 None -4 16 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -4 16 Human 5.1 pIC50 = 5.1 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
45104424 208086 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 352 2 2 6 1.4 Cc1c(N2CCN(C(=O)CCl)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
CHEMBL604130 208086 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells
ChEMBL 352 2 2 6 1.4 Cc1c(N2CCN(C(=O)CCl)CC2)c(=O)oc2cc(O)cc(O)c12 10.1021/jm901652p
155541406 179774 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
CHEMBL4518040 179774 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis in presence of 100% human serum pre-incubated for 30 mins followed by CCL22 addition and measured after 60 mins by chemoTX probe based CellTiter-Glo assay
ChEMBL 525 6 0 7 6.0 Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC[C@H](N4CCC[C@H]4CCC#N)[C@H](C)C3)cnc12 10.1021/acs.jmedchem.9b00506
5071677 82775 19 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 358 3 1 3 7.0 CC(C)(C)c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
CHEMBL205490 82775 19 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 358 3 1 3 7.0 CC(C)(C)c1ccc(-c2csc(Nc3cccc4ccccc34)n2)cc1 10.1016/j.bmcl.2006.01.126
44411322 147693 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
CHEMBL382244 147693 1 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line
ChEMBL 246 2 1 3 4.5 Cc1ccccc1Nc1nc(C(C)(C)C)cs1 10.1016/j.bmcl.2006.01.126
44288481 107928 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 557 8 1 5 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL295405 107928 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 557 8 1 5 5.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44288998 173279 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 10 3 5 4.3 NCCNC(=O)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
CHEMBL42786 173279 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 558 10 3 5 4.3 NCCNC(=O)CCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2004.01.072
44289278 174629 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)cc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
CHEMBL43092 174629 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 628 11 2 6 4.6 O=C(C[C@H]1S[C@H](c2cc(Cl)cc(Cl)c2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 10.1016/j.bmcl.2004.01.072
44401153 142060 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 368 9 1 5 4.1 CCN(CC)CCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
CHEMBL372670 142060 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4
ChEMBL 368 9 1 5 4.1 CCN(CC)CCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 10.1016/j.bmcl.2005.02.084
44288964 171683 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1 10.1016/j.bmcl.2004.01.072
CHEMBL42226 171683 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells
ChEMBL 612 11 2 6 4.1 O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(Cl)c1 10.1016/j.bmcl.2004.01.072
134210933 184285 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
CHEMBL4639600 184285 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay
ChEMBL 535 6 1 8 4.7 C[C@H](c1ccc(Cl)cc1Cl)n1nc(C#N)c2ncc(N3CC([C@H]4CCCN(Cc5cnc[nH]5)C4)C3)nc21 10.1021/acs.jmedchem.0c00988
71720517 93782 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
CHEMBL2324200 93782 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 822 2 2 4 6.0 O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 10.1021/jm301749y
127047356 146412 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 146412 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
59456102 80652 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2018964 80652 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
59455976 93930 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
CHEMBL2326611 93930 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 504 8 3 7 3.7 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(CO)cccc32)c1 10.1021/jm301572h
71583488 93935 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
CHEMBL2326616 93935 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 546 9 2 8 3.9 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COC2)c1 10.1021/jm301572h
59455990 93952 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326632 93952 0 None - 1 Human 6.0 pKd = 6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
59456103 93942 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
CHEMBL2326622 93942 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 573 9 3 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2CCCCN2)c1 10.1021/jm301572h
56849395 93965 0 None - 1 Human 5.9 pKd = 5.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326926 93965 0 None - 1 Human 5.9 pKd = 5.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 540 9 3 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(C)c(F)c1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59456014 93941 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
CHEMBL2326621 93941 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 9 3 8 4.0 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)N)c1 10.1021/jm301572h
11525206 142006 0 None - 1 Human 6.8 pKd = 6.8 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL372399 142006 0 None - 1 Human 6.8 pKd = 6.8 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
127045756 146647 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799266 146647 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
59455988 93940 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
CHEMBL2326620 93940 0 None - 1 Human 6.7 pKd = 6.7 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 547 10 3 8 3.8 CN[C@H](C)C(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1021/jm301572h
9959269 80641 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
CHEMBL2018954 80641 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
9959269 80641 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
CHEMBL2018954 80641 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmc.2014.05.021
9959269 80641 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
CHEMBL2018954 80641 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1021/jm301572h
59456050 93945 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
CHEMBL2326625 93945 0 None - 1 Human 6.6 pKd = 6.6 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 589 9 2 9 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2COCCN2C)c1 10.1021/jm301572h
118706830 119761 0 None - 1 Human 5.6 pKd = 5.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310840 119761 0 None - 1 Human 5.6 pKd = 5.6 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1nc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
59456019 93950 0 None - 1 Human 5.5 pKd = 5.5 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
CHEMBL2326630 93950 0 None - 1 Human 5.5 pKd = 5.5 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 522 8 2 7 4.4 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1021/jm301572h
9827294 80640 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
CHEMBL2018953 80640 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmc.2014.05.021
9827294 80640 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
CHEMBL2018953 80640 3 None - 1 Human 7.3 pKd = 7.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1021/jm301572h
59455975 93932 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
CHEMBL2326613 93932 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 518 8 3 7 4.3 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)O)cccc32)c1 10.1021/jm301572h
59456010 93938 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
CHEMBL2326619 93938 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 574 9 2 8 4.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCOCC2)c1 10.1021/jm301572h
118706817 119748 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310826 119748 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 387 4 3 4 3.0 COc1cc2[nH]c(=O)[nH]c2cc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054387 93927 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
CHEMBL2326609 93927 0 None - 1 Human 5.3 pKd = 5.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 492 7 2 6 4.4 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(F)cccc32)c1 10.1021/jm301572h
58054475 93943 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326623 93943 0 None - 1 Human 6.3 pKd = 6.3 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@H]2COCCN2)c1 10.1021/jm301572h
10416 8660 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.ejmech.2016.02.058
46861584 8660 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.ejmech.2016.02.058
CHEMBL2018969 8660 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometryAntagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.ejmech.2016.02.058
10416 8660 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
46861584 8660 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
CHEMBL2018969 8660 30 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1021/jm301572h
59456026 93951 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326631 93951 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1c(F)ccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
59456058 93953 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
CHEMBL2326633 93953 0 None - 1 Human 6.2 pKd = 6.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 566 9 3 8 4.1 COc1cc(F)cc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)(C)O)c1 10.1021/jm301572h
118706831 119762 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310841 119762 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 389 4 3 6 1.8 COc1nc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
58054384 93926 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
CHEMBL2326608 93926 0 None - 1 Human 5.2 pKd = 5.2 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 508 7 2 6 4.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(Cl)cccc32)c1 10.1021/jm301572h
58054368 93944 0 None - 1 Human 7.1 pKd = 7.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
CHEMBL2326624 93944 0 None - 1 Human 7.1 pKd = 7.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 575 9 3 9 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)[C@@H]2COCCN2)c1 10.1021/jm301572h
102143549 119760 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
CHEMBL3310839 119760 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometryAntagonist activity at CCR4 in human whole blood assessed as F-actin polymerization in CD4+ CCR4+ lymphocytes by phalloidin staining based flow cytometry
ChEMBL 388 4 3 5 2.4 COc1cc2[nH]c(=O)[nH]c2nc1NS(=O)(=O)c1cccc(Cl)c1Cl 10.1016/j.bmc.2014.05.021
136116031 93577 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
CHEMBL2321924 93577 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 490 7 3 7 3.9 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(O)cccc32)c1 10.1021/jm301572h
59456111 93937 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
CHEMBL2326618 93937 0 None - 1 Human 6.1 pKd = 6.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 560 9 2 8 4.4 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C2CCCO2)c1 10.1021/jm301572h
59456012 93934 0 None - 1 Human 5.1 pKd = 5.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
CHEMBL2326615 93934 0 None - 1 Human 5.1 pKd = 5.1 Binding
Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysisAntagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis
ChEMBL 524 8 2 6 5.2 CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 10.1021/jm301572h
9827294 80640 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
CHEMBL2018953 80640 3 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 499 5 2 7 3.7 O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 10.1016/j.bmcl.2012.02.104
127047356 146412 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3797662 146412 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 1 6 4.5 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
127045756 146647 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799266 146647 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
71462571 89345 3 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to CCR4Binding affinity to CCR4
ChEMBL 506 8 3 8 3.5 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(NC(=O)CO)c1 10.1021/jm300682j
CHEMBL2178575 89345 3 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to CCR4Binding affinity to CCR4
ChEMBL 506 8 3 8 3.5 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(NC(=O)CO)c1 10.1021/jm300682j
10416 8660 30 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
46861584 8660 30 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
CHEMBL2018969 8660 30 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 10.1016/j.bmcl.2012.02.104
127047973 146543 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 496 5 1 6 4.9 O=C(c1ccccn1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798539 146543 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 496 5 1 6 4.9 O=C(c1ccccn1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127045977 146761 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3799904 146761 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59455974 80649 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018961 80649 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 462 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CN)c1 10.1016/j.bmcl.2012.02.104
16747697 100303 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246334 100303 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
71457815 90760 0 None -19 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207091 90760 0 None -19 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 3.8 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
71214976 90771 0 None -79 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207101 90771 0 None -79 3 Human 6.0 pKi = 6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.5 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1cccc(C(F)(F)F)c1 10.1016/j.bmcl.2012.09.020
44440045 100367 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 443 6 1 4 3.2 CC(C)CN1CCC(NC(=O)[C@@H]2CCCN2S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246584 100367 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 443 6 1 4 3.2 CC(C)CN1CCC(NC(=O)[C@@H]2CCCN2S(=O)(=O)c2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2007.03.030
44440043 173646 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 469 7 1 4 3.7 CC(C)c1ccc(S(=O)(=O)N2CCC[C@H]2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.030
CHEMBL428576 173646 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 469 7 1 4 3.7 CC(C)c1ccc(S(=O)(=O)N2CCC[C@H]2C(=O)NC2CCN(Cc3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.030
176 7186 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -6 31 Human 4.9 pKi = 4.9 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
59456102 80652 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018964 80652 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(C)=O)c1 10.1016/j.bmcl.2012.02.104
127046413 146894 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 6 2 6 3.4 CNCC(=O)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797946 146894 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 6 2 6 3.4 CNCC(=O)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3800702 146894 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 462 6 2 6 3.4 CNCC(=O)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59455992 80644 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018957 80644 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
71461439 90756 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
CHEMBL2207087 90756 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)cc1 10.1016/j.bmcl.2012.09.020
71452487 90757 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207088 90757 0 None -12 3 Human 5.9 pKi = 5.9 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 382 5 1 5 3.4 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cccc(Cl)c1 10.1016/j.bmcl.2012.09.020
58054487 80651 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018963 80651 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 7 1 7 4.3 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(=O)N(C)C)c1 10.1016/j.bmcl.2012.02.104
44440051 156394 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL394714 156394 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
127045976 146609 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3799025 146609 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C([C@H]1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59456051 80655 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018967 80655 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 520 9 3 8 3.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)CO)c1 10.1016/j.bmcl.2012.02.104
16747697 100303 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assayDisplacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246334 100303 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assayDisplacement of mouse MDC from recombinant CCR4 receptor expressed in CHO cells coexpressing G-alpha-16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
44440041 100311 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 441 7 1 4 2.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)Cc1ccccc1 10.1016/j.bmcl.2007.03.030
CHEMBL246384 100311 0 None - 1 Human 4.8 pKi = 4.8 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 441 7 1 4 2.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)Cc1ccccc1 10.1016/j.bmcl.2007.03.030
71450658 90767 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207098 90767 0 None -15 3 Human 6.8 pKi = 6.8 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 450 5 1 5 4.7 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
59455973 80643 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccccc1Cn1nc(NS(=O)(=O)c2ccc(Cl)s2)c2c(OC)cccc21 10.1016/j.bmcl.2012.02.104
CHEMBL2018956 80643 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccccc1Cn1nc(NS(=O)(=O)c2ccc(Cl)s2)c2c(OC)cccc21 10.1016/j.bmcl.2012.02.104
58054491 80654 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CNC(C)=O)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018966 80654 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 504 8 2 7 4.2 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CNC(C)=O)cc1 10.1016/j.bmcl.2012.02.104
127046189 146399 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797567 146399 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
58054516 80646 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
CHEMBL2018959 80646 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 493 8 1 8 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1OC 10.1016/j.bmcl.2012.02.104
15604497 90768 0 None -79 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207099 90768 0 None -79 3 Human 5.7 pKi = 5.7 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 432 5 1 7 3.0 Cn1nnnc1Cc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
11525206 142006 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
CHEMBL372399 142006 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 448 5 2 6 3.2 O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 10.1016/j.ejmech.2016.02.058
127046247 146394 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 2 6 4.8 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3797537 146394 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 6 2 6 4.8 Clc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
44440135 100110 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
CHEMBL245319 100110 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
44440081 100172 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 582 8 1 5 3.9 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(N)=O)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245730 100172 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 582 8 1 5 3.9 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(N)=O)CC1 10.1016/j.bmcl.2007.03.030
127045978 146460 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797980 146460 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.4 O=C([C@H]1CCCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127045975 146508 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798263 146508 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 4.0 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127046787 146694 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 1 6 4.0 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(C(=O)C4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
CHEMBL3799514 146694 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 1 6 4.0 CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(C(=O)C4CCCN4)C3)CC2)n1 10.1016/j.ejmech.2016.02.058
127046613 146751 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 456 5 2 6 2.9 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(F)cc4F)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3799865 146751 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 456 5 2 6 2.9 O=C(C1CCCN1)N1CCC2(CCN(c3nccc(NCc4ccc(F)cc4F)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
44440031 156282 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 427 6 1 3 4.6 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
CHEMBL394642 156282 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 427 6 1 3 4.6 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1Cc1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
70689680 80642 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018955 80642 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 433 6 1 6 4.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1 10.1016/j.bmcl.2012.02.104
59456072 80645 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2018958 80645 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 1 7 4.6 COc1ccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)cc1 10.1016/j.bmcl.2012.02.104
70681287 80648 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
CHEMBL2018960 80648 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccccc1CO 10.1016/j.bmcl.2012.02.104
71461438 90751 0 None -251 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207082 90751 0 None -251 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cnnc1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71461440 90766 0 None -79 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207097 90766 0 None -79 3 Human 5.6 pKi = 5.6 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 400 5 1 5 3.6 O=S(=O)(Nc1cc(F)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
44440072 100304 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 557 7 0 4 5.0 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2F)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246335 100304 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 557 7 0 4 5.0 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2F)CC1 10.1016/j.bmcl.2007.03.030
44440047 100368 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1cccc2ccccc12)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246585 100368 0 None - 1 Human 4.6 pKi = 4.6 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 491 6 0 4 4.1 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1cccc2ccccc12)C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
44440083 157590 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 554 7 1 5 4.4 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2N)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL395680 157590 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 554 7 1 5 4.4 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2N)CC1 10.1016/j.bmcl.2007.03.030
44440059 100299 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 553 8 0 4 5.2 CCN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246328 100299 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 553 8 0 4 5.2 CCN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
9959269 80641 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
CHEMBL2018954 80641 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.ejmech.2016.02.058
127046614 146704 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799578 146704 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 442 6 2 6 3.4 Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 10.1016/j.ejmech.2016.02.058
9959269 80641 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
CHEMBL2018954 80641 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 550 11 1 8 3.9 COc1ccc(COc2nc(Br)cnc2NS(=O)(=O)c2ccc(C)cc2)cc1OCCN(C)C 10.1016/j.bmcl.2012.02.104
127046612 146528 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3798452 146528 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127046412 146892 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 391 4 2 5 4.0 Clc1ccc(CNc2ccnc(N3CCC4(CCNC4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3797678 146892 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 391 4 2 5 4.0 Clc1ccc(CNc2ccnc(N3CCC4(CCNC4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3800700 146892 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 391 4 2 5 4.0 Clc1ccc(CNc2ccnc(N3CCC4(CCNC4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
58054532 80650 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018962 80650 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 490 7 2 7 4.0 CNC(=O)c1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(OC)cccc32)c1 10.1016/j.bmcl.2012.02.104
71456007 90761 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207092 90761 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 373 5 1 6 2.7 N#Cc1cccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)c1 10.1016/j.bmcl.2012.09.020
71456008 90764 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
CHEMBL2207095 90764 0 None -50 3 Human 5.5 pKi = 5.5 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 404 5 1 6 4.0 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1csc2ccccc12 10.1016/j.bmcl.2012.09.020
70685473 80638 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018951 80638 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CO)c1 10.1016/j.bmcl.2012.02.104
59456003 80639 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018952 80639 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 476 7 2 7 3.7 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(C(N)=O)c1 10.1016/j.bmcl.2012.02.104
15985912 90750 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207081 90750 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71450657 90763 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207094 90763 0 None -15 3 Human 6.4 pKi = 6.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1cc(Cl)c(Cl)s1 10.1016/j.bmcl.2012.09.020
71452488 90762 0 None -79 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207093 90762 0 None -79 3 Human 5.4 pKi = 5.4 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 388 5 1 6 3.5 O=S(=O)(Nc1cc(Cl)ccc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
44440076 158185 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL396166 158185 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.030
44440084 100212 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 607 7 0 4 5.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245931 100212 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 607 7 0 4 5.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.030
3117 214620 103 None -4 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -4 16 Human 5.4 pKi = 5.4 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
44440075 100112 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245331 100112 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.030
44440028 100653 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
CHEMBL247976 100653 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 477 6 1 4 3.8 O=C(NC1CCN(Cc2ccccc2)CC1)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1 10.1016/j.bmcl.2007.03.030
44440079 100139 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 569 8 0 5 4.8 COc1cccc(CCN2CCC(N(C)C(=O)[C@@H]3CCCN3S(=O)(=O)c3ccc4c(Cl)cccc4c3)CC2)c1 10.1016/j.bmcl.2007.03.030
CHEMBL245531 100139 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 569 8 0 5 4.8 COc1cccc(CCN2CCC(N(C)C(=O)[C@@H]3CCCN3S(=O)(=O)c3ccc4c(Cl)cccc4c3)CC2)c1 10.1016/j.bmcl.2007.03.030
127047612 146670 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
CHEMBL3799393 146670 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 474 6 2 6 4.4 Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 10.1016/j.ejmech.2016.02.058
127047970 146600 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.2 O=C(C1CCCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798949 146600 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 502 5 2 6 4.2 O=C(C1CCCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
127046191 146893 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 3.8 O=C(C1CCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3798941 146893 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 3.8 O=C(C1CCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3800701 146893 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 488 5 2 6 3.8 O=C(C1CCNC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
70693879 80196 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
CHEMBL2016602 80196 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 463 7 2 7 4.1 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccc(CO)cc1 10.1016/j.bmcl.2012.02.104
16747697 100303 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246334 100303 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human MDC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 539 7 0 4 4.8 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
71454246 90758 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
CHEMBL2207089 90758 0 None -1 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 376 5 1 5 3.4 Cc1ccc(S(=O)(=O)Nc2cc(Cl)ccc2Cn2ccnn2)cc1C 10.1016/j.bmcl.2012.09.020
71454248 90770 0 None -39 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
CHEMBL2207100 90770 0 None -39 3 Human 6.3 pKi = 6.3 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 422 5 1 6 4.1 O=S(=O)(Nc1cc(Cl)c(Cl)cc1Cn1ccnn1)c1ccc(Cl)s1 10.1016/j.bmcl.2012.09.020
44440080 160138 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 583 8 1 5 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(=O)O)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL397848 160138 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 583 8 1 5 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccccc2C(=O)O)CC1 10.1016/j.bmcl.2007.03.030
44440054 100470 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 505 7 0 4 4.2 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL246986 100470 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 505 7 0 4 4.2 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
44440055 160132 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 519 8 0 4 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL397845 160132 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 519 8 0 4 4.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2ccccc2c1)C1CCN(CCCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
71214725 90752 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207083 90752 0 None -15 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 416 5 1 5 4.1 O=S(=O)(Nc1cc(Cl)ccc1Cn1cncn1)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
71214710 90754 0 None -39 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
CHEMBL2207085 90754 0 None -39 3 Human 6.2 pKi = 6.2 Binding
Binding affinity to CCR4 by 35S-gamma-GTP membrane assayBinding affinity to CCR4 by 35S-gamma-GTP membrane assay
ChEMBL 431 5 1 6 3.6 Cn1nnnc1Cc1ccc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 10.1016/j.bmcl.2012.09.020
127047972 146398 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 501 5 1 5 5.8 O=C(C1CCCCC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
CHEMBL3797555 146398 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting methodDisplacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
ChEMBL 501 5 1 5 5.8 O=C(C1CCCCC1)N1CCC2(CCN(c3nccc(NCc4ccc(Cl)cc4Cl)n3)CC2)C1 10.1016/j.ejmech.2016.02.058
59456067 80656 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
CHEMBL2018968 80656 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPADisplacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA
ChEMBL 534 9 3 8 3.6 COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1cccc(CNC(=O)C(C)O)c1 10.1016/j.bmcl.2012.02.104
44440077 100113 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245332 100113 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 573 7 0 4 5.5 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(Cl)cccc2c1)C1CCN(CCc2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.030
44440065 100109 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 523 7 0 4 4.3 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(F)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
CHEMBL245313 100109 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assayDisplacement of human TARC from recombinant CCR4 receptor expressed in CHO cells co-expressing Galpha16 by FLIPR assay
ChEMBL 523 7 0 4 4.3 CN(C(=O)[C@@H]1CCCN1S(=O)(=O)c1ccc2c(F)cccc2c1)C1CCN(CCc2ccccc2)CC1 10.1016/j.bmcl.2007.03.030
10416 8660 30 None - 1 Human 7.8 pIC50 = 7.8 Binding
IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.
Guide to Pharmacology 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 23409871
46861584 8660 30 None - 1 Human 7.8 pIC50 = 7.8 Binding
IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.
Guide to Pharmacology 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 23409871
CHEMBL2018969 8660 30 None - 1 Human 7.8 pIC50 = 7.8 Binding
IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.IC<sub>50</sub> determined in a GTP&gamma;S binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor.
Guide to Pharmacology 548 9 3 8 4.0 COc1cccc2c1c(nn2Cc1cccc(c1)CNC(=O)C(O)(C)C)NS(=O)(=O)c1ccc(s1)Cl 23409871
176 7186 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 7186 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 7186 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 7186 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 7186 66 None -6 31 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
3117 214620 103 None -4 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 214620 103 None -4 16 Human 8.3 pKi = 8.3 Binding
DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None