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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
| amiodarone | 398 | None | 47 | Human | Binding | pKi | = | 4.94 | 8.31 | -6 | 40 | DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) | Drug Central | 645.0 | 11 | 0 | 4 | 6.94 | CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1 | - | |
| amiodarone | 398 | None | 47 | Human | Binding | IC50 | = | 21773.00 | 4.66 | -6 | 40 | DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) | ChEMBL | 645.0 | 11 | 0 | 4 | 6.94 | CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1 | - | |
| amiodarone | 398 | None | 47 | Human | Binding | Ki | = | 11405.00 | 4.94 | -6 | 40 | DRUGMATRIX: Chemokine CCR4 radioligand binding (ligand: [125I] TARC) | ChEMBL | 645.0 | 11 | 0 | 4 | 6.94 | CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1 | - | |
| AZD1678 | 542 | None | 16 | Dog | Binding | IC50 | = | 3.16 | 8.50 | - | 3 | Antagonist activity at dog CCR4 | ChEMBL | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD2098 | 545 | None | 41 | Dog | Binding | IC50 | = | 25.12 | 7.60 | - | 3 | Antagonist activity at dog CCR4 | ChEMBL | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| cenicriviroc | 879 | None | 32 | Human | Binding | IC50 | = | 1100.00 | 5.96 | - | 6 | Displacement of [125I]TARC from CCR4 expressed in CHO cells | ChEMBL | 696.4 | 17 | 1 | 7 | 8.74 | CCCCOCCOc1ccc(-c2ccc3c(c2)C=C(C(=O)Nc2ccc([S@@](=O)Cc4cncn4CCC)cc2)CCCN3CC(C)C)cc1 | https://dx.doi.org/10.1021/jm0509703 | |
| CHEMBL1182360 | 11870 | None | 0 | Human | Binding | IC50 | = | 280.00 | 6.55 | - | 1 | Displacement of [125I]MDC from human CCR4 expressed in HEK293 cells | ChEMBL | 409.2 | 11 | 2 | 5 | 5.32 | CCN(CC)C(C)CCCNc1nccc(NCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2006.10.091 | |
| CHEMBL191915 | 68672 | None | 0 | Human | Binding | IC50 | = | 25000.00 | 4.60 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 376.2 | 11 | 1 | 5 | 4.63 | CCN(CC)CCCC(C)Nc1ccnc(COc2cccc(Cl)c2)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL194775 | 70576 | None | 0 | Human | Binding | IC50 | = | 1500.00 | 5.82 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 410.2 | 11 | 1 | 5 | 5.29 | CCN(CC)CCCC(C)Nc1nccc(OCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL194775 | 70576 | None | 0 | Human | Binding | IC50 | = | 1500.00 | 5.82 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 410.2 | 11 | 1 | 5 | 5.29 | CCN(CC)CCCC(C)Nc1nccc(OCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL194930 | 70607 | None | 0 | Human | Binding | IC50 | = | 2400.00 | 5.62 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 390.3 | 11 | 1 | 4 | 5.34 | CCN(CC)CCCC(C)Nc1nc(CCc2ccccc2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195061 | 70731 | None | 0 | Human | Binding | IC50 | = | 2000.00 | 5.70 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 392.3 | 11 | 1 | 5 | 5.13 | CCN(CC)CCCC(C)Nc1nc(COc2ccccc2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195103 | 70864 | None | 0 | Human | Binding | IC50 | = | 2800.00 | 5.55 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 410.2 | 11 | 1 | 5 | 5.29 | CCN(CC)CCCC(C)Nc1ccnc(OCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195203 | 71094 | None | 0 | Human | Binding | IC50 | = | 6100.00 | 5.21 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4; range = 3.6-6.1 uM | ChEMBL | 388.3 | 10 | 1 | 4 | 5.72 | CCN(CC)CCCC(C)Nc1nc(/C=C/c2ccccc2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195298 | 71108 | None | 0 | Human | Binding | IC50 | = | 270.00 | 6.57 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 409.2 | 11 | 2 | 5 | 5.32 | CCN(CC)CCCC(C)Nc1nccc(NCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195484 | 71150 | None | 0 | Human | Binding | IC50 | = | 8000.00 | 5.10 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 382.1 | 10 | 1 | 5 | 4.51 | CCN(CC)CCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195665 | 71259 | None | 0 | Human | Binding | IC50 | = | 10000.00 | 5.00 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 376.3 | 10 | 1 | 4 | 5.14 | CCN(CC)CCCC(C)Nc1nc(Cc2ccccc2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195751 | 71341 | None | 0 | Human | Binding | IC50 | = | 2500.00 | 5.60 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 412.3 | 9 | 1 | 4 | 6.37 | CCN(CC)CCCC(C)Nc1nc(-c2ccc3ccccc3c2)nc2ccccc12 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195764 | 71346 | None | 0 | Human | Binding | IC50 | = | 3000.00 | 5.52 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 396.1 | 11 | 1 | 5 | 4.90 | CCN(CC)CCCCNc1nccc(OCc2ccc(Cl)cc2Cl)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
| CHEMBL195893 | 71429 | None | 0 | Human | Binding | IC50 | = | 25000.00 | 4.60 | - | 1 | Inhibitory concentration against human C-C chemokine receptor type 4 | ChEMBL | 410.2 | 11 | 1 | 5 | 5.29 | CCN(CC)CCCC(C)Nc1ccnc(COc2cc(Cl)cc(Cl)c2)n1 | https://dx.doi.org/10.1016/j.bmcl.2005.02.084 | |
Showing 1 to 20 of 384 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
| AZD1678 | 542 | None | 16 | Human | Functional | pIC50 | = | - | 8.60 | -16 | 3 | Unclassified | Guide to Pharmacology | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://pubmed.ncbi.nlm.nih.gov/28947948 | |
| AZD1678 | 542 | None | 16 | Human | Functional | IC50 | = | 316.23 | 6.50 | -16 | 3 | Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis | ChEMBL | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD1678 | 542 | None | 16 | Human | Functional | IC50 | = | 2.51 | 8.60 | -16 | 3 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay | ChEMBL | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD1678 | 542 | None | 16 | Human | Functional | IC50 | = | 158.49 | 6.80 | -16 | 3 | Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis | ChEMBL | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD1678 | 542 | None | 16 | Human | Functional | IC50 | = | 3.98 | 8.40 | -16 | 3 | Antagonist activity at human CCR4 expressed in HEK cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization | ChEMBL | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD1678 | 542 | None | 16 | Dog | Functional | pIC50 | = | - | 8.50 | -3 | 3 | Unclassified | Guide to Pharmacology | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://pubmed.ncbi.nlm.nih.gov/28947948 | |
| AZD1678 | 542 | None | 16 | Mouse | Functional | pIC50 | = | - | 9.00 | 3 | 3 | Unclassified | Guide to Pharmacology | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://pubmed.ncbi.nlm.nih.gov/28947948 | |
| AZD1678 | 542 | None | 16 | Mouse | Functional | IC50 | = | 1.00 | 9.00 | 3 | 3 | Antagonist activity at mouse CCR4 | ChEMBL | 351.0 | 4 | 1 | 5 | 2.73 | COc1nc(F)cnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD2098 | 545 | None | 41 | Human | Functional | pIC50 | = | - | 7.80 | -4 | 3 | Unclassified | Guide to Pharmacology | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://pubmed.ncbi.nlm.nih.gov/28947948 | |
| AZD2098 | 545 | None | 41 | Human | Functional | IC50 | = | 501.19 | 6.30 | -4 | 3 | Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL17 induced chemotaxis | ChEMBL | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD2098 | 545 | None | 41 | Human | Functional | IC50 | = | 501.19 | 6.30 | -4 | 3 | Antagonist activity at human CCR4 expressed in Th2 cells coexpressing CD45RA+ assessed as inhibition of CCL22 induced chemotaxis | ChEMBL | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD2098 | 545 | None | 41 | Human | Functional | IC50 | = | 15.85 | 7.80 | -4 | 3 | Antagonist activity at recombinant human CCR4 expressed in CHO-K1 cells assessed as inhibition of CCL22 induced Ca2+ mobilization after 2 hrs by FMAT based fluorescence assay | ChEMBL | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD2098 | 545 | None | 41 | Human | Functional | IC50 | = | 31.62 | 7.50 | -4 | 3 | Antagonist activity at human CCR4 expressed in CHO cells coexpressing CD4+ assessed as inhibition of CCL22 induced Ca2+ mobilization | ChEMBL | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| AZD2098 | 545 | None | 41 | Dog | Functional | pIC50 | = | - | 7.60 | -2 | 3 | Unclassified | Guide to Pharmacology | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://pubmed.ncbi.nlm.nih.gov/28947948 | |
| AZD2098 | 545 | None | 41 | Mouse | Functional | pIC50 | = | - | 8.00 | 2 | 3 | Unclassified | Guide to Pharmacology | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://pubmed.ncbi.nlm.nih.gov/28947948 | |
| AZD2098 | 545 | None | 41 | Mouse | Functional | IC50 | = | 10.00 | 8.00 | 2 | 3 | Antagonist activity at mouse CCR4 | ChEMBL | 333.0 | 4 | 1 | 5 | 2.59 | COc1nccnc1NS(=O)(=O)c1cccc(Cl)c1Cl | https://dx.doi.org/10.1021/acsmedchemlett.7b00315 | |
| CCL17 | 832 | None | 0 | Human | Functional | pIC50 | = | - | 8.70 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9430724 | |
| CCL22 | 846 | None | 0 | Human | Functional | pIC50 | = | - | 9.20 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9430724 | |
| CHEMBL1169660 | 10562 | None | 0 | Human | Functional | Ki | = | 1584.89 | 5.80 | - | 2 | Antagonist activity at CCR4 | ChEMBL | 515.0 | 8 | 3 | 6 | 4.36 | O=C(NCCO)c1ccccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.142 | |
| CHEMBL1170725 | 10697 | None | 0 | Human | Functional | Ki | = | 1258.93 | 5.90 | - | 2 | Antagonist activity at CCR4 | ChEMBL | 443.0 | 5 | 1 | 5 | 5.34 | Cc1ncccc1Oc1ncc(Cl)cc1NS(=O)(=O)c1ccc(Cl)c(Cl)c1 | https://dx.doi.org/10.1016/j.bmcl.2010.04.142 | |
Showing 1 to 20 of 347 entries