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
| |
| 71525974 | 133389 | None | 0 | Human | Functional | pIC50 | = | 8.9 | 8.9 | 51 | 4 | 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 | 439 | 7 | 3 | 8 | 2.5 | Cc1ccc([C@H](Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | ||
| CHEMBL3704570 | 133389 | None | 0 | Human | Functional | pIC50 | = | 8.9 | 8.9 | 51 | 4 | 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 | 439 | 7 | 3 | 8 | 2.5 | Cc1ccc([C@H](Nc2c(Nc3cccc(C(=O)N(C)C)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | ||
| 71555361 | 133392 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | 15 | 5 | FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50). |
ChEMBL | 564 | 8 | 3 | 10 | 2.4 | Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | ||
| CHEMBL3704573 | 133392 | None | 0 | Human | Functional | pIC50 | = | 8.7 | 8.7 | 15 | 5 | FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50).FLIPR Assay: The experiments were carried out on the FLIPR TETRA.RTM. platform from Molecular Devices. After the basal level had been read, the compounds were added to the cells expressing the chemokine receptor of interest and the agonist activity was read at 10 seconds. After a further incubation for 10 minutes, the cells were activated, with a concentration equivalent to the AC80, using a reference agonist in order to detect whether this compound exhibits antagonist activity.Each cell line expressing a chemokine receptor was established on the basis of the Chem-1 cell stably expressing the recombinant form of the chemokine receptor and also an associated G protein, with the aim of coupling the receptor to the calcium signalling pathway. 21 receptors belonging to the chemokine receptor family (CCRs and CXCRs) were analyzed. All the CXCR2 antagonists were tested in a dose-dependent manner and the concentration corresponding to 50% inhibition of the response was determined (IC.sub.50). |
ChEMBL | 564 | 8 | 3 | 10 | 2.4 | Cc1ccc([C@H](Nc2c(Nc3ccc(Cl)c(S(=O)(=O)N4CCN(C)CC4)c3O)c(=O)c2=O)C2(C)COC2)o1 | nan | ||
| 1472329 | 34856 | None | 22 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -1 | 3 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 278 | 3 | 0 | 5 | 2.1 | Cc1ccc(S(=O)(=O)c2ccc([N+](=O)[O-])cn2)cc1 | nan | ||
| CHEMBL1431608 | 34856 | None | 22 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -1 | 3 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 278 | 3 | 0 | 5 | 2.1 | Cc1ccc(S(=O)(=O)c2ccc([N+](=O)[O-])cn2)cc1 | nan | ||
| 901998 | 35396 | None | 6 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -1 | 3 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 332 | 3 | 0 | 5 | 2.8 | O=[N+]([O-])c1ccc(S(=O)(=O)c2cccc(C(F)(F)F)c2)nc1 | nan | ||
| CHEMBL1437683 | 35396 | None | 6 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -1 | 3 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 332 | 3 | 0 | 5 | 2.8 | O=[N+]([O-])c1ccc(S(=O)(=O)c2cccc(C(F)(F)F)c2)nc1 | nan | ||
| 805087 | 48676 | None | 4 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -2 | 4 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 299 | 3 | 1 | 4 | 3.6 | O=C(Nc1nnc(-c2ccccc2)o1)c1ccc(Cl)cc1 | nan | ||
| CHEMBL1557648 | 48676 | None | 4 | Human | Functional | pIC50 | = | 5.0 | 5.0 | -2 | 4 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 299 | 3 | 1 | 4 | 3.6 | O=C(Nc1nnc(-c2ccccc2)o1)c1ccc(Cl)cc1 | nan | ||
| 9500339 | 38417 | None | 1 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 384 | 4 | 4 | 10 | -1.2 | Cc1n[nH]c(=S)n(NC(=O)CC(=O)Nn2c(=S)[nH]nc(C)c2=O)c1=O | nan | ||
| CHEMBL1463647 | 38417 | None | 1 | Human | Functional | pIC50 | = | 5.0 | 5.0 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 384 | 4 | 4 | 10 | -1.2 | Cc1n[nH]c(=S)n(NC(=O)CC(=O)Nn2c(=S)[nH]nc(C)c2=O)c1=O | nan | ||
| 9958995 | 59659 | None | 33 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 541 | 1 | 0 | 6 | 6.7 | CC1(C)CC[C@]2(C(=O)n3ccnc3)CC[C@]3(C)[C@H](C(=O)C=C4[C@@]3(C)CC[C@H]3C(C)(C)C(=O)C(C#N)=C[C@]43C)[C@@H]2C1 | nan | ||
| CHEMBL1720855 | 59659 | None | 33 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 541 | 1 | 0 | 6 | 6.7 | CC1(C)CC[C@]2(C(=O)n3ccnc3)CC[C@]3(C)[C@H](C(=O)C=C4[C@@]3(C)CC[C@H]3C(C)(C)C(=O)C(C#N)=C[C@]43C)[C@@H]2C1 | nan | ||
| 136496399 | 30344 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 354 | 9 | 3 | 5 | 1.5 | CCCCCCC(=O)NN/C=C1\C(=O)NC(=S)N(C(C)CC)C1=O | nan | ||
| CHEMBL1391621 | 30344 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 354 | 9 | 3 | 5 | 1.5 | CCCCCCC(=O)NN/C=C1\C(=O)NC(=S)N(C(C)CC)C1=O | nan | ||
| 145985454 | 165571 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 503 | 6 | 2 | 5 | 5.1 | NC(=O)c1cccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)c1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4239904 | 165571 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 503 | 6 | 2 | 5 | 5.1 | NC(=O)c1cccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)c1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145985433 | 165486 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 346 | 5 | 1 | 4 | 3.0 | COc1ccc(S(=O)(=O)N2CCC(Nc3ccccc3)CC2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4237952 | 165486 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 346 | 5 | 1 | 4 | 3.0 | COc1ccc(S(=O)(=O)N2CCC(Nc3ccccc3)CC2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145982664 | 165995 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 443 | 5 | 1 | 6 | 3.8 | N#Cc1ccc(-c2ccc(S(=O)(=O)N3CCC(Nc4ccc(C#N)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4249961 | 165995 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 443 | 5 | 1 | 6 | 3.8 | N#Cc1ccc(-c2ccc(S(=O)(=O)N3CCC(Nc4ccc(C#N)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145983631 | 165997 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -1 | 2 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 503 | 6 | 2 | 5 | 5.1 | NC(=O)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4250007 | 165997 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -1 | 2 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 503 | 6 | 2 | 5 | 5.1 | NC(=O)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 243574 | 59831 | None | 39 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 201 | 1 | 0 | 2 | 1.7 | Cc1cc(C)cc(N2C(=O)C=CC2=O)c1 | nan | ||
| CHEMBL1727268 | 59831 | None | 39 | Human | Functional | pIC50 | = | 4.9 | 4.9 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 201 | 1 | 0 | 2 | 1.7 | Cc1cc(C)cc(N2C(=O)C=CC2=O)c1 | nan | ||
| 2884240 | 31862 | None | 4 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -1 | 3 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 436 | 3 | 1 | 5 | 3.3 | COC(=O)C1=NN(C(=O)c2cccc(Br)c2)C(O)(c2ccc(Cl)cc2)C1 | nan | ||
| CHEMBL1406895 | 31862 | None | 4 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -1 | 3 | PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340]PUBCHEM_BIOASSAY: SAR analysis of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159, AID540340] |
ChEMBL | 436 | 3 | 1 | 5 | 3.3 | COC(=O)C1=NN(C(=O)c2cccc(Br)c2)C(O)(c2ccc(Cl)cc2)C1 | nan | ||
| 887191 | 36674 | None | 6 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -2 | 2 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 342 | 3 | 0 | 5 | 4.3 | Cc1ccc(C(=O)Oc2ccc(Cl)c3cccnc23)cc1[N+](=O)[O-] | nan | ||
| CHEMBL1448982 | 36674 | None | 6 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -2 | 2 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 342 | 3 | 0 | 5 | 4.3 | Cc1ccc(C(=O)Oc2ccc(Cl)c3cccnc23)cc1[N+](=O)[O-] | nan | ||
| 145984200 | 165592 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 473 | 5 | 1 | 5 | 6.1 | CC(C)(C)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C#N)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4240463 | 165592 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 473 | 5 | 1 | 5 | 6.1 | CC(C)(C)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C#N)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 26042546 | 165813 | None | 4 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -1 | 2 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in human CCL20-dependent cell migration incubated for 4 hrs by Diff-Quik staining based assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in human CCL20-dependent cell migration incubated for 4 hrs by Diff-Quik staining based assay |
ChEMBL | 356 | 4 | 1 | 5 | 2.5 | Cc1ccc(S(=O)(=O)N2CCC(Nc3ccc(C#N)cn3)CC2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4245957 | 165813 | None | 4 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -1 | 2 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in human CCL20-dependent cell migration incubated for 4 hrs by Diff-Quik staining based assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in human CCL20-dependent cell migration incubated for 4 hrs by Diff-Quik staining based assay |
ChEMBL | 356 | 4 | 1 | 5 | 2.5 | Cc1ccc(S(=O)(=O)N2CCC(Nc3ccc(C#N)cn3)CC2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 2884240 | 31862 | None | 4 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -1 | 3 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 436 | 3 | 1 | 5 | 3.3 | COC(=O)C1=NN(C(=O)c2cccc(Br)c2)C(O)(c2ccc(Cl)cc2)C1 | nan | ||
| CHEMBL1406895 | 31862 | None | 4 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -1 | 3 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 436 | 3 | 1 | 5 | 3.3 | COC(=O)C1=NN(C(=O)c2cccc(Br)c2)C(O)(c2ccc(Cl)cc2)C1 | nan | ||
| 901998 | 35396 | None | 6 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 3 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 332 | 3 | 0 | 5 | 2.8 | O=[N+]([O-])c1ccc(S(=O)(=O)c2cccc(C(F)(F)F)c2)nc1 | nan | ||
| CHEMBL1437683 | 35396 | None | 6 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 3 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 332 | 3 | 0 | 5 | 2.8 | O=[N+]([O-])c1ccc(S(=O)(=O)c2cccc(C(F)(F)F)c2)nc1 | nan | ||
| 3241407 | 33821 | None | 9 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 2 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 319 | 4 | 1 | 7 | 4.0 | COc1ccc2nc(Nc3nc(C)c(C(C)=O)s3)sc2c1 | nan | ||
| CHEMBL1422976 | 33821 | None | 9 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 2 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 319 | 4 | 1 | 7 | 4.0 | COc1ccc2nc(Nc3nc(C)c(C(C)=O)s3)sc2c1 | nan | ||
| 4887113 | 36076 | None | 8 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 3 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 334 | 1 | 2 | 5 | 1.2 | CN1C(=O)C(=C2CC(c3ccc(Cl)cc3)NN2)C(=O)N(C)C1=O | nan | ||
| CHEMBL1443778 | 36076 | None | 8 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 3 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 334 | 1 | 2 | 5 | 1.2 | CN1C(=O)C(=C2CC(c3ccc(Cl)cc3)NN2)C(=O)N(C)C1=O | nan | ||
| 145985837 | 166047 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 376 | 4 | 1 | 5 | 2.9 | N#Cc1ccc(NC2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)nc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4251392 | 166047 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | - | 1 | Inhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of human CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 376 | 4 | 1 | 5 | 2.9 | N#Cc1ccc(NC2CCN(S(=O)(=O)c3ccc(Cl)cc3)CC2)nc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 512832 | 50307 | None | 9 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 256 | 2 | 0 | 3 | 2.1 | O=C1C=CC(=O)N1c1ccc(N2CCCCC2)cc1 | nan | ||
| CHEMBL1571835 | 50307 | None | 9 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 256 | 2 | 0 | 3 | 2.1 | O=C1C=CC(=O)N1c1ccc(N2CCCCC2)cc1 | nan | ||
| 9612752 | 71750 | None | 1 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 365 | 5 | 2 | 2 | 4.4 | C/C(=N\NC(=S)NCCc1ccccc1)c1ccc(Cl)cc1Cl | nan | ||
| CHEMBL1965860 | 71750 | None | 1 | Human | Functional | pIC50 | = | 4.8 | 4.8 | - | 1 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 365 | 5 | 2 | 2 | 4.4 | C/C(=N\NC(=S)NCCc1ccccc1)c1ccc(Cl)cc1Cl | nan | ||
| 5791769 | 201982 | None | 6 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 2 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 424 | 5 | 1 | 6 | 3.4 | CCc1ccc(S(=O)(=O)/N=C2/C=C(Sc3nc[nH]n3)C(=O)c3ccccc32)cc1 | nan | ||
| CHEMBL592124 | 201982 | None | 6 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -1 | 2 | PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159]PUBCHEM_BIOASSAY: Dose Response confirmation of small molecule antagonists of the CCR6 receptor: a luminescent beta-arrestin assay. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID493098, AID493121, AID493159] |
ChEMBL | 424 | 5 | 1 | 6 | 3.4 | CCc1ccc(S(=O)(=O)/N=C2/C=C(Sc3nc[nH]n3)C(=O)c3ccccc32)cc1 | nan | ||
Showing 1 to 50 of 560 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
| |
| 134817249 | 165922 | None | 19 | Rhesus macaque | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 504 | 6 | 2 | 6 | 4.5 | NC(=O)c1cc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)ccn1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4248604 | 165922 | None | 19 | Rhesus macaque | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 504 | 6 | 2 | 6 | 4.5 | NC(=O)c1cc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)ccn1 | 10.1016/j.bmcl.2018.07.042 | ||
| 26042546 | 165813 | None | 4 | Rhesus macaque | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 356 | 4 | 1 | 5 | 2.5 | Cc1ccc(S(=O)(=O)N2CCC(Nc3ccc(C#N)cn3)CC2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4245957 | 165813 | None | 4 | Rhesus macaque | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 356 | 4 | 1 | 5 | 2.5 | Cc1ccc(S(=O)(=O)N2CCC(Nc3ccc(C#N)cn3)CC2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145983631 | 165997 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 503 | 6 | 2 | 5 | 5.1 | NC(=O)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4250007 | 165997 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 503 | 6 | 2 | 5 | 5.1 | NC(=O)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145983516 | 165657 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 7.7 | 7.7 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 485 | 5 | 1 | 5 | 5.8 | N#Cc1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4242040 | 165657 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 7.7 | 7.7 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 485 | 5 | 1 | 5 | 5.8 | N#Cc1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145985518 | 165776 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 6.6 | 6.6 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 418 | 5 | 1 | 5 | 3.9 | N#Cc1ccc(NC2CCN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)CC2)nc1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4245036 | 165776 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 6.6 | 6.6 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 418 | 5 | 1 | 5 | 3.9 | N#Cc1ccc(NC2CCN(S(=O)(=O)c3ccc(-c4ccccc4)cc3)CC2)nc1 | 10.1016/j.bmcl.2018.07.042 | ||
| 145985766 | 165789 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 504 | 6 | 2 | 6 | 4.5 | NC(=O)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cn1 | 10.1016/j.bmcl.2018.07.042 | ||
| CHEMBL4245355 | 165789 | None | 0 | Rhesus macaque | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Inhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assayInhibition of monkey CCR6 expressed in CHO cells assessed as decrease in CCL20-induced reduction of forskolin-stimulated cAMP accumulation preincubated for 30 mins followed agonist addition measured after 30 mins by HTRF assay |
ChEMBL | 504 | 6 | 2 | 6 | 4.5 | NC(=O)c1ccc(-c2ccc(S(=O)(=O)[C@H]3CC[C@H](Nc4ccc(C(F)(F)F)cn4)CC3)cc2)cn1 | 10.1016/j.bmcl.2018.07.042 | ||
| 809 | 842 | None | 0 | Human | Binding | pKd | None | 9 | 9.0 | - | 1 | UnclassifiedUnclassified |
Guide to Pharmacology | None | None | None | None | 9169459 | ||||
Showing 1 to 13 of 13 entries