Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
9827294 73502 1 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 73502 1 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 139207 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 139207 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 139383 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 139383 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 139091 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 139091 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 168151 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 168151 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 139064 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 139064 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 139349 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 139349 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 164744 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 164744 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 162273 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 162273 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 161935 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 161935 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 537 7 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 537 7 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 537 7 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 161612 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 161612 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 540 35 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 540 35 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 540 35 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 162126 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 162126 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 134692 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 134692 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 187241 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 187241 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 187331 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 187331 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 192035 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 192035 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 86714 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 86714 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 86716 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 86716 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 86717 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 86717 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 86731 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 86731 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 161865 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 161865 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 112464 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 112464 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 161552 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 161552 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 162144 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 162144 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 157707 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 157707 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 158609 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 158609 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 162027 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 162027 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 169890 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 169890 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 83910 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 83910 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 185296 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 185296 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 185296 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 185296 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 112465 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 112465 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 73518 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 73518 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 86361 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 86361 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 86733 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 86733 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 161599 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 161599 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 161844 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 161844 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 162475 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 162475 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 177624 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 177624 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 86732 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 86732 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 161414 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 161414 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 162529 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 162529 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 158203 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 158203 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 162212 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 162212 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 155839 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 155839 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 172612 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 172612 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 73515 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 73515 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 175639 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 175639 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 188447 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 188447 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 186163 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 186163 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 185296 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 185296 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 185845 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 185845 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 185296 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 185296 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 185845 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 185845 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 176623 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 176623 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 1841 23 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 1841 23 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 1841 23 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 168151 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 168151 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 1120 24 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 1120 24 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 1120 24 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 187179 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 187179 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 177237 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 177237 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 86723 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 86723 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 86724 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 86724 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 86725 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 86725 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 86727 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 86727 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 86736 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 86736 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 86748 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 86748 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 540 35 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 540 35 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 540 35 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 161624 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 161624 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 162148 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 162148 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 186136 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 186136 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 132278 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 132278 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 73506 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 73506 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 537 7 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 537 7 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 537 7 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 86730 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 86730 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 156066 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 156066 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 161933 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 161933 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 162506 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 162506 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 112468 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 112468 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 157850 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 157850 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 175172 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 175172 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 174892 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 174892 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 177341 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 177341 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 1120 24 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 1120 24 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 1120 24 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 1120 24 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 1120 24 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 1120 24 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 172401 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 172401 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 187670 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 187670 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 185845 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 185845 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 185845 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 185845 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 187269 0 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 187269 0 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 185845 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 185845 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 192035 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 192035 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 86715 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 86715 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 86718 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 86718 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 161771 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 161771 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 161989 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 161989 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 72765 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 72765 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 112460 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 112460 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 112470 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 112470 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 157668 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 157668 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 161617 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 161617 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 161821 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 161821 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 112462 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 112462 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 112467 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 112467 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 158523 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 158523 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 112461 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 112461 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 537 7 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 537 7 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 537 7 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 161485 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 161485 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 185845 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 185845 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 185845 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 185845 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 175641 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 175641 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 192946 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 192946 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 176922 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 176922 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 176741 4 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 176741 4 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 177460 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 177460 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 73508 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 73508 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 186137 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 186137 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 188517 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 188517 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 170526 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 170526 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 170366 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 170366 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 177079 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 177079 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 170675 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 170675 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 187269 0 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 187269 0 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 192835 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 192835 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 171833 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 171833 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 176569 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 176569 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 185296 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 185296 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 185296 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 185296 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 176498 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 176498 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 186039 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 186039 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 112471 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 112471 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 86726 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 86726 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 162018 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 162018 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 174394 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 174394 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 86729 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 86729 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 86749 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 86749 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 157003 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 157003 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 158486 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 158486 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 158664 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 158664 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 169743 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 169743 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 186127 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 186127 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 174071 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 174071 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 73517 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 73517 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 169096 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 169096 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 176524 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 176524 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 186164 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 186164 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 92198 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 92198 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 177465 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 177465 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 86818 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 86818 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 73503 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 73503 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 73503 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 73503 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 73503 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 73503 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 73503 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 73503 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 537 7 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 537 7 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 537 7 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 161523 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 161523 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 162294 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 162294 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 162429 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 162429 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 192035 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 192035 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 176721 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 176721 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 185983 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 185983 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 189276 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 189276 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 540 35 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 540 35 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 540 35 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 73514 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 73514 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 73514 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 73514 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 86709 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 86709 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 86719 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 86719 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 86721 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 86721 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 112459 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 112459 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 537 7 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 537 7 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 537 7 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 86712 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 86712 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 155980 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 155980 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 157758 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 157758 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 155794 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 155794 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 156840 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 156840 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 161685 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 161685 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 162319 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 162319 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 162403 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 162403 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 171609 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 171609 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 174450 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 174450 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 173128 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 173128 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 73500 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 73500 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 185983 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 185983 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 73510 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 73510 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 171766 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 171766 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 177323 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 177323 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 169534 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 169534 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 185185 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 185185 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 177104 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 177104 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 174800 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 174800 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 177031 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 177031 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 92130 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 92130 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 134692 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 134692 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 173943 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 173943 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 73504 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 73504 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 1120 24 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 1120 24 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 1120 24 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 1841 23 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 1841 23 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 1841 23 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 86720 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 86720 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 86734 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 86734 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 86735 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 86735 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 161479 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 161479 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 161495 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 161495 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 162260 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 162260 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 187180 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 187180 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 112469 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 112469 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 86745 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 86745 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 86747 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 86747 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 112466 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 112466 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 159167 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 159167 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 1049 5 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 1049 5 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 1049 5 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 172416 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 172416 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 73513 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 73513 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 176985 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 176985 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 171031 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 171031 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 187241 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 187241 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 186164 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 186164 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 187240 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 187240 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 187179 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 187179 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 132790 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 132790 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 177118 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 177118 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 112463 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 112463 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 176911 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 176911 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 169808 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 169808 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 73059 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 73059 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 187240 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 187240 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 178413 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 178413 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 72765 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 72765 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 73502 1 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 73502 1 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 73502 1 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 73502 1 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 73502 1 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 73502 1 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 73502 1 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 73502 1 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 112473 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 112473 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 86746 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 86746 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 161734 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 161734 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 11746 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 11746 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 11746 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 70725 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 70725 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 540 35 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 540 35 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 540 35 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 540 35 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 540 35 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 540 35 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 156316 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 156316 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 161590 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 161590 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 161835 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 161835 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 161904 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 161904 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 177285 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 177285 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 187241 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 187241 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 189082 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 189082 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 192835 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 192835 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 76751 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 76751 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 171937 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 171937 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 172607 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 172607 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 73501 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 73501 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 185868 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 185868 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 175638 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 175638 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 92197 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 92197 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 173985 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 173985 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 187269 0 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 187269 0 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 177192 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 177192 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 177041 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 177041 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 86713 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 86713 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 86728 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 86728 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 112458 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 112458 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 112458 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 112458 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 185185 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 185185 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 187180 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 187180 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 187331 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 187331 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 155321 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 155321 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 72765 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 72765 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 161529 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 161529 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 162190 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 162190 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 155884 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 155884 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 158174 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 158174 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 158347 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 158347 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 162366 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 162366 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 162381 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 162381 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 192835 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 192835 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 140819 16 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 140819 16 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 170114 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 170114 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 176870 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 176870 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 174396 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 174396 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 186039 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 186039 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 86818 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 86818 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 134692 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 134692 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 139091 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 139091 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 139326 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 139326 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 139383 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 139383 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 161816 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 161816 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 162341 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 162341 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 185983 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 185983 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 176554 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 176554 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 112472 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 112472 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 73512 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 73512 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 86710 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 86710 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 86737 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 86737 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 156124 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 156124 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 156276 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 156276 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 162481 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 162481 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 155376 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 155376 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 155924 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 155924 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 157187 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 157187 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 157937 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 157937 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 162422 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 162422 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 155266 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 155266 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 162050 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 162050 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 177160 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 177160 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 11746 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 11746 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 11746 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 173205 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 173205 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 186039 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 186039 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 171167 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 171167 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 177226 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 177226 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 187240 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 187240 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 187179 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 187179 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 176780 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 176780 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 177199 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 177199 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 73511 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 73511 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 186135 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 186135 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 185984 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 185984 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 73511 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 73511 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 73514 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 73514 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 73501 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 73501 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 73517 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 73517 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 73503 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 73503 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 73508 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 73508 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 73502 1 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 73502 1 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 1841 23 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 1841 23 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 1841 23 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 73518 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 73518 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 73500 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 73500 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 73504 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 73504 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 10578 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 10578 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 10444 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 10444 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 10676 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 10676 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 10614 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 10614 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
5280343 187681 119 None -16 7 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 187681 119 None -16 7 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 187681 119 None -16 7 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 4696 96 None 3 39 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 4696 96 None 3 39 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 3076 99 None -18 5 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
65015 3076 99 None -18 5 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
844 3076 99 None -18 5 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
CHEMBL18442 3076 99 None -18 5 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
DB06809 3076 99 None -18 5 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 502 4 6 8 0.4 C1CNCCN(CCCNCCNC1)Cc1ccc(cc1)CN1CCNCCCNCCNCCC1 None
3793 201510 70 None -1 3 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 201510 70 None -1 3 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 201510 70 None -1 3 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 1627 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 1627 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 1049 5 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 1049 5 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 1049 5 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 540 35 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 540 35 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 540 35 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 1120 24 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 1120 24 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 1120 24 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 540 35 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 540 35 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 540 35 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 540 35 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 540 35 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 540 35 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 537 7 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 537 7 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 537 7 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 537 7 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 537 7 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 537 7 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
797 817 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724
23585443 537 7 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 537 7 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 537 7 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
798 831 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9430724




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
44410965 76691 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 76691 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 73571 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 73571 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 100687 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 100687 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 164498 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 164498 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 165408 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 165408 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 169198 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 169198 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 204099 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 204099 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 187681 119 None - 32 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 187681 119 None - 32 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 187681 119 None - 32 Human 5.0 pIC50 = 5 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
71720517 86565 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 86565 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 163233 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 163233 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 70876 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 70876 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 187681 119 None - 32 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 187681 119 None - 32 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 187681 119 None - 32 Human 4.0 pIC50 = 4 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
44288899 100782 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 100782 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 161510 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 161510 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 167617 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 167617 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 169706 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 169706 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 187681 119 None - 32 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL1520590 187681 119 None - 32 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
CHEMBL50 187681 119 None - 32 Human 5.0 pIC50 = 5.0 Binding
Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
ChEMBL 302 1 5 7 2.0 O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 10.1021/jm301749y
134211221 177104 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 177104 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 199015 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 199015 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 164744 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 164744 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 151578 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 151578 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 864 30 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
801 864 30 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 864 30 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 864 30 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 99995 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 99995 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 154990 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 154990 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 155079 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 155079 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 156749 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 156749 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 165755 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 165755 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 169760 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 169760 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 170403 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 170403 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 199224 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 199224 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 201510 70 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 201510 70 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 201510 70 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 176721 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 176721 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 173943 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 173943 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 192946 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 192946 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 140653 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 140653 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 78567 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 78567 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 101030 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 101030 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 162939 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 162939 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 168763 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 168763 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 76432 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 76432 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 201510 70 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 201510 70 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 201510 70 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 163096 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 163096 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 170354 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 170354 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 199042 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 199042 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 200016 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 200016 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 177079 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 177079 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 177465 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 177465 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 171937 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 171937 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 137884 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 137884 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 151836 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 151836 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 168151 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 168151 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 164994 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 164994 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 185296 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 185296 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 177031 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 177031 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 138354 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 138354 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 164066 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 164066 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 168713 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 168713 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 70193 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 70193 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 174450 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 174450 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 199026 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 199026 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 199043 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 199043 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 199537 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 199537 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 199016 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 199016 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 4696 96 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 4696 96 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 86565 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 86565 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 199400 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 199400 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 1049 5 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 1049 5 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 1049 5 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 76743 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 76743 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 140819 16 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 140819 16 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 78565 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 78565 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 169534 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 169534 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 76751 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 76751 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 168160 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 168160 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 168225 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 168225 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 78574 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 78574 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 178413 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 178413 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 99720 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 99720 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 86782 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 86782 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 170675 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 170675 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 199025 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 199025 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 86818 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 86818 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 101075 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 101075 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 201510 70 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 201510 70 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 201510 70 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 168301 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 168301 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 168766 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 168766 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 70348 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 70348 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 125881 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 125881 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 163283 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 163283 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 78571 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 78571 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 198707 18 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 198707 18 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 76936 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 76936 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 76981 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 76981 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 86676 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 86676 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 168703 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 168703 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
176 394 63 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 394 63 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 394 63 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 394 63 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 394 63 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 173985 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 173985 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 165195 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 165195 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 164519 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 164519 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 97967 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 97967 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 154861 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 154861 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 70224 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 70224 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 165521 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 165521 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 176985 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 176985 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 540 35 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 540 35 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 540 35 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 99935 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 99935 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 168783 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 168783 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 99766 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 99766 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 100764 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 100764 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 167350 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 167350 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 70958 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 70958 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 68293 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 68293 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 71046 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 71046 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 199155 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 199155 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 171609 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 171609 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 177460 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 177460 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 76390 0 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 76390 0 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 86679 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 86679 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 70725 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 70725 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 11746 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 11746 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 11746 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 151581 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 151581 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 70481 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 70481 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 162881 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 162881 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 166008 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 166008 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 537 7 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 537 7 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 537 7 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 76793 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 76793 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 133000 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 133000 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 140819 16 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 140819 16 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 168766 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 168766 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 70963 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 70963 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 76751 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 76751 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 165817 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 165817 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 200827 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 200827 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 199342 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 199342 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 100903 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 100903 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 171766 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 171766 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 176741 4 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 176741 4 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 100749 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 100749 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 100930 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 100930 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 162544 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 162544 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 164963 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 164963 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 76778 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 76778 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 167352 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 167352 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 168861 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 168861 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 86565 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 86565 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 100897 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 100897 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 169271 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 169271 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 174800 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 174800 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 177160 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 177160 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 164105 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 164105 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 168857 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 168857 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 86900 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 86900 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 168112 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 168112 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 171031 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 171031 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 75597 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 75597 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 177199 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 177199 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 139696 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 139696 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 176780 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 176780 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 169956 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 169956 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 169808 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 169808 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 199226 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 199226 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 176741 4 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 176741 4 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 86565 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 86565 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 177041 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 177041 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 162909 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 162909 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 163105 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 163105 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 168493 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 168493 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 78568 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 78568 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 176911 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 176911 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 199888 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 199888 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 199225 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 199225 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 199027 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 199027 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 199185 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 199185 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 171766 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 171766 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 76389 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 76389 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 165548 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 165548 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 176498 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 176498 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 76700 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 76700 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 76171 2 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 76171 2 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 199068 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 199068 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 197485 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 197485 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 76722 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 76722 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 86678 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 86678 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 176741 4 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 176741 4 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 134692 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 134692 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 134692 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 134692 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 86817 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 86817 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 201510 70 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 201510 70 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 201510 70 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 201510 70 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 201510 70 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 201510 70 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 186137 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 186137 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 198742 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 198742 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 176524 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 176524 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 199429 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 199429 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 199114 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 199114 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 76979 2 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 76979 2 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 176870 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 176870 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 72665 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 72665 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 101003 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 101003 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 99783 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 99783 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 176554 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 176554 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 174071 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 174071 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 199320 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 199320 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 177341 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 177341 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 72562 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 72562 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 165868 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 165868 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 199647 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 199647 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 100771 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 100771 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 161410 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 161410 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 178039 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 178039 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 200159 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 200159 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 70711 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 70711 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 170366 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 170366 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 176741 4 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 176741 4 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 188517 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 188517 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 164779 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 164779 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 100621 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 100621 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 199024 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 199024 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 101049 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 101049 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 1049 5 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 1049 5 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 1049 5 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 185845 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 185845 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 185845 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 185845 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 72344 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 72344 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 99883 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 99883 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 154631 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 154631 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 168516 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 168516 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 177226 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 177226 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 201510 70 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 201510 70 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 201510 70 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 1120 24 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 1120 24 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 1120 24 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 186127 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 186127 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 199401 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 199401 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 176569 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 176569 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 177323 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 177323 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 199223 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 199223 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 165297 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 165297 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 201510 70 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 201510 70 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 201510 70 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 149257 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 149257 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 76415 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 76415 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 138966 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 138966 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 168465 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 168465 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 72404 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 72404 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 99979 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 99979 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 154884 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 154884 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 162608 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 162608 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 168783 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 168783 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 70767 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 70767 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 86780 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 86780 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 86781 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 86781 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 154861 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 154861 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 165520 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 165520 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 206096 100 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 206096 100 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 199612 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 199612 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 172416 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 172416 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 75632 16 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 75632 16 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 140371 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 140371 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 100669 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 100669 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 165936 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 165936 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 167276 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 167276 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 134746 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 134746 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 164341 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 164341 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 176922 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 176922 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 86565 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 86565 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 139091 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 139091 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 73514 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 73514 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 86713 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 86713 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 86718 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 86718 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 86735 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 86735 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 86725 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 86725 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 86748 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 86748 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 86724 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 86724 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 134692 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 134692 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 139326 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 139326 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 86723 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 86723 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 73503 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 73503 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 73503 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 73503 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 73503 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 73503 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 86728 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 86728 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 112472 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 112472 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 86733 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 86733 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 73502 1 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 73502 1 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 73502 1 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 73502 1 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 86715 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 86715 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 86721 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 86721 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 112459 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 112459 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 86710 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 86710 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 86726 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 86726 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 1841 23 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 1841 23 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 1841 23 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 1841 23 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 1841 23 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 1841 23 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 86734 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 86734 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 86736 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 86736 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 112473 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 112473 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 86709 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 86709 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 86727 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 86727 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 112471 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 112471 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 86361 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 86361 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 86720 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 86720 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 86717 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 86717 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 73502 1 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 73502 1 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 139091 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 139091 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 139326 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 139326 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 82144 1 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 82144 1 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 1841 23 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 1841 23 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 1841 23 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 139222 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 139222 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 139440 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 139440 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 73511 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 73511 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 93082 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 93082 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 83557 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 83557 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 83568 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 83568 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 93146 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 93146 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 166303 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 166303 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
176 394 63 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 394 63 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 394 63 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 394 63 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 394 63 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 73514 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 73514 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 139573 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 139573 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 139573 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 73506 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 73506 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 83553 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 83553 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 83554 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 83554 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 73513 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 73513 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 149071 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 149071 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 139288 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 139288 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 73517 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 73517 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 93082 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 93082 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 93090 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 93090 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 83564 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 83564 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 73505 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 73505 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 73516 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 73516 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 139078 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 139078 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 73508 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 73508 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 83565 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 83565 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 134692 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 134692 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 139073 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 139073 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 92890 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 92890 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 92952 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 92952 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 139139 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 139139 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 139187 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 139187 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 139373 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 139373 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 139430 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 139430 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 148959 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 148959 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 73504 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 73504 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 73507 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 73507 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 73510 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 73510 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 83548 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 83548 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 83563 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 83563 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 93083 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 93083 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 93147 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 93147 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 150266 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 150266 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 93078 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 93078 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 73503 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 73503 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 139383 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 139383 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 73503 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 73503 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 139207 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 139207 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 139571 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 139571 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 139571 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 73512 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 73512 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 83558 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 83558 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 83561 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 83561 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 73500 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 73500 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 73501 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 73501 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 83547 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 83547 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 83560 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 83560 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 83559 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 83559 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 150862 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 150862 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 92991 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 92991 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 206096 100 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 206096 100 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 92892 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 92892 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 93432 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 93432 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 92919 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 92919 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 139349 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 139349 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 139279 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 139279 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 139572 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 139572 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 139572 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 73059 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 73059 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 93082 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 93082 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 83555 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 83555 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 83567 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 83567 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 152813 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 152813 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 93249 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 93249 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 152807 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 152807 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 83549 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 83549 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 83551 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 83551 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 139077 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 139077 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 73518 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 73518 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 92893 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 92893 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 92889 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 92889 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 1841 23 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 1841 23 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 1841 23 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
176 394 63 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 394 63 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 394 63 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 394 63 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 394 63 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 206096 100 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 206096 100 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