Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 9827294 | 73891 | None | 9 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 499 | 5 | 2 | 7 | 3.7 | O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 | 10.1016/j.ejmech.2016.02.058 | ||
| CHEMBL2018953 | 73891 | None | 9 | Human | Functional | pEC50 | = | 8 | 8.0 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 499 | 5 | 2 | 7 | 3.7 | O=C([C@H]1CCCCN1)N1CCN(c2nc(NCc3ccc(Cl)cc3Cl)c3cccnc3n2)CC1 | 10.1016/j.ejmech.2016.02.058 | ||
| 127046612 | 139837 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 474 | 6 | 2 | 6 | 4.4 | Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 | 10.1016/j.ejmech.2016.02.058 | ||
| CHEMBL3798452 | 139837 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 474 | 6 | 2 | 6 | 4.4 | Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@@H]5CCCN5)C4)CC3)n2)c(Cl)c1 | 10.1016/j.ejmech.2016.02.058 | ||
| 127046614 | 140013 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 442 | 6 | 2 | 6 | 3.4 | Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 | 10.1016/j.ejmech.2016.02.058 | ||
| CHEMBL3799578 | 140013 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 442 | 6 | 2 | 6 | 3.4 | Fc1ccc(CNc2ccnc(N3CCC4(CCN(CC5CCCN5)C4)CC3)n2)c(F)c1 | 10.1016/j.ejmech.2016.02.058 | ||
| 127047356 | 139721 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 488 | 6 | 1 | 6 | 4.5 | CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 | 10.1016/j.ejmech.2016.02.058 | ||
| CHEMBL3797662 | 139721 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 488 | 6 | 1 | 6 | 4.5 | CN(Cc1ccc(Cl)cc1Cl)c1ccnc(N2CCC3(CCN(CC4CCCN4)C3)CC2)n1 | 10.1016/j.ejmech.2016.02.058 | ||
| 44288958 | 168830 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4 |
ChEMBL | 624 | 11 | 2 | 5 | 5.6 | Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL43698 | 168830 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4 |
ChEMBL | 624 | 11 | 2 | 5 | 5.6 | Cc1c(Cl)cccc1CNC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O | 10.1016/j.bmcl.2004.01.072 | ||
| 127047440 | 139694 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 542 | 7 | 2 | 8 | 4.4 | COc1cc2nc(N3CCC(N(C)C(=O)[C@H]4CCCN4)CC3)nc(Nc3ccc(Cl)cc3F)c2cc1OC | 10.1016/j.ejmech.2016.02.058 | ||
| CHEMBL3797462 | 139694 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 542 | 7 | 2 | 8 | 4.4 | COc1cc2nc(N3CCC(N(C)C(=O)[C@H]4CCCN4)CC3)nc(Nc3ccc(Cl)cc3F)c2cc1OC | 10.1016/j.ejmech.2016.02.058 | ||
| 127047612 | 139979 | None | 0 | Human | Functional | pEC50 | = | 8.2 | 8.2 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 474 | 6 | 2 | 6 | 4.4 | Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 | 10.1016/j.ejmech.2016.02.058 | ||
| CHEMBL3799393 | 139979 | None | 0 | Human | Functional | pEC50 | = | 8.2 | 8.2 | - | 1 | Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometryInduction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry |
ChEMBL | 474 | 6 | 2 | 6 | 4.4 | Clc1ccc(CNc2ccnc(N3CCC4(CCN(C[C@H]5CCCN5)C4)CC3)n2)c(Cl)c1 | 10.1016/j.ejmech.2016.02.058 | ||
| 44288959 | 165402 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4 |
ChEMBL | 640 | 11 | 2 | 5 | 6.3 | C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL42334 | 165402 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4Inhibition of MDC-stimulated chemotaxis in transfected murine cell line expressing human chemokine receptor 4 |
ChEMBL | 640 | 11 | 2 | 5 | 6.3 | C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 10238794 | 162930 | None | 0 | Human | Functional | pIC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 473 | 7 | 2 | 6 | 4.3 | O=S(=O)(Nc1ncc(Cl)nc1OCc1ccccc1CO)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4172769 | 162930 | None | 0 | Human | Functional | pIC50 | = | 9.5 | 9.5 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 473 | 7 | 2 | 6 | 4.3 | O=S(=O)(Nc1ncc(Cl)nc1OCc1ccccc1CO)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 10195057 | 162592 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 444 | 6 | 1 | 6 | 4.2 | O=S(=O)(Nc1ncc(Cl)nc1OCc1cccnc1)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4167445 | 162592 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 444 | 6 | 1 | 6 | 4.2 | O=S(=O)(Nc1ncc(Cl)nc1OCc1cccnc1)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 23585443 | 542 | None | 16 | Mouse | Functional | pIC50 | = | 9 | 9.0 | 3 | 3 | Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4 |
ChEMBL | 351 | 4 | 1 | 5 | 2.7 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 9679 | 542 | None | 16 | Mouse | Functional | pIC50 | = | 9 | 9.0 | 3 | 3 | Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4 |
ChEMBL | 351 | 4 | 1 | 5 | 2.7 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4172635 | 542 | None | 16 | Mouse | Functional | pIC50 | = | 9 | 9.0 | 3 | 3 | Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4 |
ChEMBL | 351 | 4 | 1 | 5 | 2.7 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(c1Cl)Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 145959198 | 162267 | None | 0 | Human | Functional | pIC50 | = | 9 | 9.0 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 369 | 4 | 1 | 5 | 2.9 | COc1nc(F)c(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4162364 | 162267 | None | 0 | Human | Functional | pIC50 | = | 9 | 9.0 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 369 | 4 | 1 | 5 | 2.9 | COc1nc(F)c(F)nc1NS(=O)(=O)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 10308720 | 545 | None | 41 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 2 | 3 | Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4 |
ChEMBL | 333 | 4 | 1 | 5 | 2.6 | COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 9678 | 545 | None | 41 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 2 | 3 | Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4 |
ChEMBL | 333 | 4 | 1 | 5 | 2.6 | COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4169247 | 545 | None | 41 | Mouse | Functional | pIC50 | = | 8 | 8.0 | 2 | 3 | Antagonist activity at mouse CCR4Antagonist activity at mouse CCR4 |
ChEMBL | 333 | 4 | 1 | 5 | 2.6 | COc1nccnc1NS(=O)(=O)c1cccc(c1Cl)Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 10309893 | 162783 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 411 | 4 | 1 | 5 | 3.4 | COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4170431 | 162783 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 411 | 4 | 1 | 5 | 3.4 | COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | 10.1021/acsmedchemlett.7b00315 | ||
| 11525206 | 135297 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPRCalcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR |
ChEMBL | 448 | 5 | 2 | 6 | 3.2 | O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 | 10.1016/j.bmcl.2005.09.022 | ||
| CHEMBL372399 | 135297 | None | 0 | Human | Functional | pIC50 | = | 8 | 8.0 | - | 1 | Calcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPRCalcium mobilization mediated by CCR4 receptor in CEMS529 cells by FLIPR |
ChEMBL | 448 | 5 | 2 | 6 | 3.2 | O=C([C@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 | 10.1016/j.bmcl.2005.09.022 | ||
| 44581043 | 187940 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | 1 | 2 | Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding |
ChEMBL | 511 | 7 | 1 | 8 | 5.1 | COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC | 10.1016/j.bmc.2008.11.020 | ||
| CHEMBL496152 | 187940 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | 1 | 2 | Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding |
ChEMBL | 511 | 7 | 1 | 8 | 5.1 | COc1cc2nc(N3CCC(N4CCCC(OC)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC | 10.1016/j.bmc.2008.11.020 | ||
| 44581068 | 188030 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding |
ChEMBL | 513 | 7 | 2 | 9 | 3.7 | COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC | 10.1016/j.bmc.2008.11.020 | ||
| CHEMBL496787 | 188030 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS bindingAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced [35S]GTPgammaS binding |
ChEMBL | 513 | 7 | 2 | 9 | 3.7 | COc1cc2nc(N3CCC(N4CCOC(CO)C4)CC3)nc(Nc3ccc(Cl)cc3)c2cc1OC | 10.1016/j.bmc.2008.11.020 | ||
| 25212472 | 192755 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | -2 | 2 | Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis |
ChEMBL | 497 | 7 | 2 | 8 | 4.5 | COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC | 10.1016/j.bmc.2008.11.020 | ||
| CHEMBL521737 | 192755 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | -2 | 2 | Antagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxisAntagonist activity at human CCR4 receptor expressed in mouse B300-19 cells assessed as CCL22-induced chemotaxis |
ChEMBL | 497 | 7 | 2 | 8 | 4.5 | COc1cc2nc(N3CCC(N4CCCC(CO)C4)CC3)nc(NC3CCCCCC3)c2cc1OC | 10.1016/j.bmc.2008.11.020 | ||
| 59456023 | 87190 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 516 | 8 | 2 | 7 | 4.4 | CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)=O)cccc32)c1 | 10.1021/jm301572h | ||
| CHEMBL2326612 | 87190 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 516 | 8 | 2 | 7 | 4.4 | CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)=O)cccc32)c1 | 10.1021/jm301572h | ||
| 59456042 | 87192 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 532 | 8 | 3 | 7 | 4.5 | CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)(C)O)cccc32)c1 | 10.1021/jm301572h | ||
| CHEMBL2326614 | 87192 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 532 | 8 | 3 | 7 | 4.5 | CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(C)(C)O)cccc32)c1 | 10.1021/jm301572h | ||
| 59456012 | 87193 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 524 | 8 | 2 | 6 | 5.2 | CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 | 10.1021/jm301572h | ||
| CHEMBL2326615 | 87193 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 524 | 8 | 2 | 6 | 5.2 | CC(=O)NCc1cccc(Cn2nc(NS(=O)(=O)c3ccc(Cl)s3)c3c(C(F)F)cccc32)c1 | 10.1021/jm301572h | ||
| 71584536 | 87207 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 505 | 8 | 2 | 8 | 3.6 | COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccnc(CNC(C)=O)c1 | 10.1021/jm301572h | ||
| CHEMBL2326628 | 87207 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assayAntagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay |
ChEMBL | 505 | 8 | 2 | 8 | 3.6 | COc1cccc2c1c(NS(=O)(=O)c1ccc(Cl)s1)nn2Cc1ccnc(CNC(C)=O)c1 | 10.1021/jm301572h | ||
| 59168189 | 162522 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 377 | 4 | 1 | 5 | 2.7 | COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1 | 10.1021/acsmedchemlett.7b00315 | ||
| CHEMBL4166246 | 162522 | None | 0 | Human | Functional | pIC50 | = | 7 | 7.0 | - | 1 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assayAntagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay |
ChEMBL | 377 | 4 | 1 | 5 | 2.7 | COc1nc(Br)cnc1NS(=O)(=O)c1cccc(Cl)c1 | 10.1021/acsmedchemlett.7b00315 | ||
| 118706823 | 113039 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay |
ChEMBL | 429 | 5 | 2 | 5 | 4.0 | COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(C)C | 10.1016/j.bmc.2014.05.021 | ||
| CHEMBL3310832 | 113039 | None | 0 | Human | Functional | pIC50 | = | 6 | 6.0 | - | 1 | Antagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assayAntagonist activity at human CCR4 expressed in CHO cell membranes by [35S]-GTPgammaS radioligand competition assay |
ChEMBL | 429 | 5 | 2 | 5 | 4.0 | COc1cc2c(cc1NS(=O)(=O)c1cccc(Cl)c1Cl)[nH]c(=O)n2C(C)C | 10.1016/j.bmc.2014.05.021 | ||
Showing 1 to 50 of 729 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 44410965 | 77087 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line |
ChEMBL | 283 | 5 | 2 | 4 | 4.1 | CCNCc1csc(Nc2cccc3ccccc23)n1 | 10.1016/j.bmcl.2006.01.126 | ||
| CHEMBL207290 | 77087 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]TARC from CCR4 expressed in human CEM cell lineDisplacement of [125I]TARC from CCR4 expressed in human CEM cell line |
ChEMBL | 283 | 5 | 2 | 4 | 4.1 | CCNCc1csc(Nc2cccc3ccccc23)n1 | 10.1016/j.bmcl.2006.01.126 | ||
| 44406335 | 73960 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells |
ChEMBL | 448 | 5 | 2 | 6 | 3.2 | O=C([C@@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 | 10.1016/j.bmcl.2005.09.022 | ||
| CHEMBL202085 | 73960 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cellsDisplacement of [125I]TARC from human CCR4 receptor transfected in HEK293 cells |
ChEMBL | 448 | 5 | 2 | 6 | 3.2 | O=C([C@@H]1CCCCN1)N1CCN(c2nccc(NCc3ccc(Cl)cc3Cl)n2)CC1 | 10.1016/j.bmcl.2005.09.022 | ||
| 44288732 | 101223 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 596 | 11 | 2 | 6 | 3.6 | O=C(C[C@H]1S[C@H](c2ccc(F)cc2F)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL295560 | 101223 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 596 | 11 | 2 | 6 | 3.6 | O=C(C[C@H]1S[C@H](c2ccc(F)cc2F)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 44288854 | 165156 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 646 | 11 | 2 | 6 | 4.5 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL42266 | 165156 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 646 | 11 | 2 | 6 | 4.5 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc(C(F)(F)F)c1 | 10.1016/j.bmcl.2004.01.072 | ||
| 44288730 | 166067 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 612 | 11 | 2 | 6 | 4.1 | O=C(C[C@H]1S[C@H](c2ccc(F)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL42523 | 166067 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 612 | 11 | 2 | 6 | 4.1 | O=C(C[C@H]1S[C@H](c2ccc(F)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 44289282 | 169879 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 617 | 11 | 3 | 6 | 4.0 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc2[nH]ccc2c1 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL44390 | 169879 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 617 | 11 | 3 | 6 | 4.0 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccc2[nH]ccc2c1 | 10.1016/j.bmcl.2004.01.072 | ||
| 5481702 | 208281 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptor |
ChEMBL | 556 | 8 | 0 | 4 | 5.3 | CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 | 10.1016/s0960-894x(00)00639-9 | ||
| CHEMBL83338 | 208281 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Compound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptorCompound concentration that causes 50 % inhibition of binding of specific radioligand to human CCR4 receptor |
ChEMBL | 556 | 8 | 0 | 4 | 5.3 | CN(C[C@@H](CCN1CCC2(CC1)C[S+]([O-])c1ccccc12)c1cccc(Cl)c1)S(=O)(=O)c1ccccc1 | 10.1016/s0960-894x(00)00639-9 | ||
| 5280343 | 188382 | None | 69 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| CHEMBL1520590 | 188382 | None | 69 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| CHEMBL50 | 188382 | None | 69 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| 71720517 | 87041 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 822 | 2 | 2 | 4 | 6.0 | O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 | 10.1021/jm301749y | ||
| CHEMBL2324200 | 87041 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 822 | 2 | 2 | 4 | 6.0 | O=C1OC(c2cc(I)c(O)c(I)c2)(c2c(I)cc(O)cc2I)c2ccccc21 | 10.1021/jm301749y | ||
| 44288960 | 163891 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 612 | 11 | 2 | 6 | 4.1 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1Cl | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL42060 | 163891 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 612 | 11 | 2 | 6 | 4.1 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1ccccc1Cl | 10.1016/j.bmcl.2004.01.072 | ||
| 44400830 | 71259 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4 |
ChEMBL | 376 | 10 | 1 | 4 | 5.1 | CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 | 10.1016/j.bmcl.2005.02.084 | ||
| CHEMBL195665 | 71259 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibitory concentration against human C-C chemokine receptor type 4Inhibitory concentration against human C-C chemokine receptor type 4 |
ChEMBL | 376 | 10 | 1 | 4 | 5.1 | CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 | 10.1016/j.bmcl.2005.02.084 | ||
| 5280343 | 188382 | None | 69 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| CHEMBL1520590 | 188382 | None | 69 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| CHEMBL50 | 188382 | None | 69 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| 44288899 | 101319 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 588 | 13 | 2 | 6 | 3.6 | O=C(C[C@H]1S[C@H](CCc2ccccc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL296245 | 101319 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 588 | 13 | 2 | 6 | 3.6 | O=C(C[C@H]1S[C@H](CCc2ccccc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 44288863 | 162165 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 566 | 11 | 2 | 6 | 3.5 | O=C(C[C@H]1S[C@H](C2CCCCC2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL416069 | 162165 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 566 | 11 | 2 | 6 | 3.5 | O=C(C[C@H]1S[C@H](C2CCCCC2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 44289207 | 168294 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 633 | 9 | 1 | 5 | 6.8 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(Cc2cccc(CN3CCOCC3)c2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL43330 | 168294 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 633 | 9 | 1 | 5 | 6.8 | O=C(C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(Cc2cccc(CN3CCOCC3)c2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 44288557 | 170387 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 550 | 11 | 2 | 7 | 2.9 | O=C(C[C@H]1S[C@H](c2ccoc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL44463 | 170387 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 550 | 11 | 2 | 7 | 2.9 | O=C(C[C@H]1S[C@H](c2ccoc2)N(CC(=O)NCCCN2CCOCC2)C1=O)NCc1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 5280343 | 188382 | None | 69 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| CHEMBL1520590 | 188382 | None | 69 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| CHEMBL50 | 188382 | None | 69 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 32 | Inhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assayInhibition of CCL22-stimulated CCR4 in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay |
ChEMBL | 302 | 1 | 5 | 7 | 2.0 | O=c1c(O)c(-c2ccc(O)c(O)c2)oc2cc(O)cc(O)c12 | 10.1021/jm301749y | ||
| 134211221 | 177793 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay |
ChEMBL | 502 | 7 | 1 | 7 | 4.6 | Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 | 10.1021/acs.jmedchem.0c00988 | ||
| CHEMBL4641873 | 177793 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assayAntagonist activity at CCR4 in human CCRF-CEM cells assessed as inhibition of CCL22-mediated chemotaxis preincubated for 30 mins followed by CCL22 addition and measured after 60 mins in presence of 100% human serum by CellTiter-Glo assay |
ChEMBL | 502 | 7 | 1 | 7 | 4.6 | Cc1nn([C@H](C)c2ccc(Cl)cc2Cl)c2nc(N3CC([C@H]4CCCN(CCCO)C4)C3)cnc12 | 10.1021/acs.jmedchem.0c00988 | ||
| 45104526 | 203165 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells |
ChEMBL | 479 | 3 | 3 | 7 | 3.8 | Cc1c(N2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 | 10.1021/jm901652p | ||
| CHEMBL599995 | 203165 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cellsDisplacement of FITC-CKLF1-C27 from human CCR4 receptor expressed in human HEK293 cells |
ChEMBL | 479 | 3 | 3 | 7 | 3.8 | Cc1c(N2CCN(C(=O)Nc3ccc(OC(F)(F)F)cc3)CC2)c(=O)oc2cc(O)cc(O)c12 | 10.1021/jm901652p | ||
| 44288959 | 165402 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 640 | 11 | 2 | 5 | 6.3 | C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| CHEMBL42334 | 165402 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 640 | 11 | 2 | 5 | 6.3 | C[C@@H](NC(=O)C[C@H]1S[C@H](c2ccc(Cl)cc2Cl)N(CC(=O)NCCCN2CCCCC2)C1=O)c1cccc2ccccc12 | 10.1016/j.bmcl.2004.01.072 | ||
| 44430304 | 152211 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells |
ChEMBL | 477 | 12 | 2 | 7 | 5.7 | CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2c(ncn2CC)n1 | 10.1016/j.bmcl.2006.10.091 | ||
| CHEMBL396786 | 152211 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]MDC from human CCR4 expressed in HEK293 cellsDisplacement of [125I]MDC from human CCR4 expressed in HEK293 cells |
ChEMBL | 477 | 12 | 2 | 7 | 5.7 | CCN(CC)CCCC(C)Nc1nc(NCc2ccc(Cl)cc2Cl)c2c(ncn2CC)n1 | 10.1016/j.bmcl.2006.10.091 | ||
| 11285792 | 879 | None | 32 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells |
ChEMBL | 696 | 17 | 1 | 7 | 8.7 | CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC | 10.1021/jm0509703 | ||
| 801 | 879 | None | 32 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells |
ChEMBL | 696 | 17 | 1 | 7 | 8.7 | CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC | 10.1021/jm0509703 | ||
| CHEMBL2110727 | 879 | None | 32 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells |
ChEMBL | 696 | 17 | 1 | 7 | 8.7 | CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC | 10.1021/jm0509703 | ||
| DB11758 | 879 | None | 32 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]TARC from CCR4 expressed in CHO cellsDisplacement of [125I]TARC from CCR4 expressed in CHO cells |
ChEMBL | 696 | 17 | 1 | 7 | 8.7 | CCCCOCCOc1ccc(cc1)c1ccc2c(c1)C=C(CCCN2CC(C)C)C(=O)Nc1ccc(cc1)[S@@](=O)Cc1cncn1CCC | 10.1021/jm0509703 | ||
| 44288962 | 100528 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cellsInhibition of [125I]MDC binding to recombinant human C-C chemokine receptor type 4 (CCR4) expressed in murine pre-B cells |
ChEMBL | 572 | 10 | 2 | 5 | 4.5 | CN(C)CC(=O)NCCN1C(=O)[C@@H](CC(=O)NCc2cccc3ccccc23)S[C@@H]1c1ccc(Cl)cc1Cl | 10.1016/j.bmcl.2004.01.072 | ||
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