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
| |
| 14434082 | 83816 | None | 16 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccnc2c1ccc1c(C=O)ccnc12 | 10.1021/jm301121j | ||
| CHEMBL2205801 | 83816 | None | 16 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccnc2c1ccc1c(C=O)ccnc12 | 10.1021/jm301121j | ||
| 14434082 | 83816 | None | 16 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccnc2c1ccc1c(C=O)ccnc12 | 10.1021/jm301121j | ||
| CHEMBL2205801 | 83816 | None | 16 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccnc2c1ccc1c(C=O)ccnc12 | 10.1021/jm301121j | ||
| 72791 | 210699 | None | 48 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| CHEMBL98682 | 210699 | None | 48 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 72791 | 210699 | None | 48 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| CHEMBL98682 | 210699 | None | 48 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 77865 | 107342 | None | 51 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 214 | 0 | 0 | 2 | 3.4 | Clc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| CHEMBL317115 | 107342 | None | 51 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 214 | 0 | 0 | 2 | 3.4 | Clc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 14338 | 4369 | None | 74 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccnc(-c2cc(C)ccn2)c1 | 10.1021/jm301121j | ||
| CHEMBL101165 | 4369 | None | 74 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccnc(-c2cc(C)ccn2)c1 | 10.1021/jm301121j | ||
| 77865 | 107342 | None | 51 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 214 | 0 | 0 | 2 | 3.4 | Clc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| CHEMBL317115 | 107342 | None | 51 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 1 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 214 | 0 | 0 | 2 | 3.4 | Clc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 14338 | 4369 | None | 74 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccnc(-c2cc(C)ccn2)c1 | 10.1021/jm301121j | ||
| CHEMBL101165 | 4369 | None | 74 | Human | Functional | pEC50 | = | 5.5 | 5.5 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccnc(-c2cc(C)ccn2)c1 | 10.1021/jm301121j | ||
| 667748 | 83819 | None | 57 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 267 | 2 | 0 | 3 | 3.9 | Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 | 10.1021/jm301121j | ||
| CHEMBL2205805 | 83819 | None | 57 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 267 | 2 | 0 | 3 | 3.9 | Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 | 10.1021/jm301121j | ||
| 12425 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| 1318 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| CHEMBL415879 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| DB02365 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| 667748 | 83819 | None | 57 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 267 | 2 | 0 | 3 | 3.9 | Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 | 10.1021/jm301121j | ||
| CHEMBL2205805 | 83819 | None | 57 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 3 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 267 | 2 | 0 | 3 | 3.9 | Clc1cc(-c2ccccn2)nc(-c2ccccn2)c1 | 10.1021/jm301121j | ||
| 12425 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| 1318 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| CHEMBL415879 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| DB02365 | 6 | None | 76 | Human | Functional | pEC50 | = | 5.4 | 5.4 | 1 | 4 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 180 | 0 | 0 | 2 | 2.8 | C1=CC2=C(C3=C(C=CC=N3)C=C2)N=C1 | 10.1021/jm301121j | ||
| 1474 | 154488 | None | 79 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 156 | 1 | 0 | 2 | 2.1 | c1ccc(-c2ccccn2)nc1 | 10.1021/jm301121j | ||
| CHEMBL39879 | 154488 | None | 79 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 156 | 1 | 0 | 2 | 2.1 | c1ccc(-c2ccccn2)nc1 | 10.1021/jm301121j | ||
| 1474 | 154488 | None | 79 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 156 | 1 | 0 | 2 | 2.1 | c1ccc(-c2ccccn2)nc1 | 10.1021/jm301121j | ||
| CHEMBL39879 | 154488 | None | 79 | Human | Functional | pEC50 | = | 4.4 | 4.4 | -1 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 156 | 1 | 0 | 2 | 2.1 | c1ccc(-c2ccccn2)nc1 | 10.1021/jm301121j | ||
| 74265 | 210806 | None | 69 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 2 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 0 | 0 | 2 | 4.0 | Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C | 10.1021/jm301121j | ||
| CHEMBL99384 | 210806 | None | 69 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 2 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 0 | 0 | 2 | 4.0 | Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C | 10.1021/jm301121j | ||
| 20445 | 83820 | None | 65 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 2 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1cccc(-c2cccc(C)n2)n1 | 10.1021/jm301121j | ||
| CHEMBL2205806 | 83820 | None | 65 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 2 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1cccc(-c2cccc(C)n2)n1 | 10.1021/jm301121j | ||
| 70848 | 209130 | None | 67 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 233 | 2 | 0 | 3 | 3.2 | c1ccc(-c2cccc(-c3ccccn3)n2)nc1 | 10.1021/jm301121j | ||
| CHEMBL89445 | 209130 | None | 67 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 233 | 2 | 0 | 3 | 3.2 | c1ccc(-c2cccc(-c3ccccn3)n2)nc1 | 10.1021/jm301121j | ||
| 72792 | 202179 | None | 52 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccnc2c1ccc1c(C)ccnc12 | 10.1021/jm301121j | ||
| CHEMBL593442 | 202179 | None | 52 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccnc2c1ccc1c(C)ccnc12 | 10.1021/jm301121j | ||
| 74265 | 210806 | None | 69 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 2 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 0 | 0 | 2 | 4.0 | Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C | 10.1021/jm301121j | ||
| CHEMBL99384 | 210806 | None | 69 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 2 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 0 | 0 | 2 | 4.0 | Cc1cnc2c(ccc3c(C)c(C)cnc32)c1C | 10.1021/jm301121j | ||
| 20445 | 83820 | None | 65 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 2 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1cccc(-c2cccc(C)n2)n1 | 10.1021/jm301121j | ||
| CHEMBL2205806 | 83820 | None | 65 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 2 | 2 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1cccc(-c2cccc(C)n2)n1 | 10.1021/jm301121j | ||
| 2733927 | 83822 | None | 59 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 1 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 216 | 3 | 0 | 4 | 2.2 | COc1ccnc(-c2cc(OC)ccn2)c1 | 10.1021/jm301121j | ||
| CHEMBL2205808 | 83822 | None | 59 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 1 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 216 | 3 | 0 | 4 | 2.2 | COc1ccnc(-c2cc(OC)ccn2)c1 | 10.1021/jm301121j | ||
| 70848 | 209130 | None | 67 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 233 | 2 | 0 | 3 | 3.2 | c1ccc(-c2cccc(-c3ccccn3)n2)nc1 | 10.1021/jm301121j | ||
| CHEMBL89445 | 209130 | None | 67 | Human | Functional | pEC50 | = | 5.3 | 5.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 233 | 2 | 0 | 3 | 3.2 | c1ccc(-c2cccc(-c3ccccn3)n2)nc1 | 10.1021/jm301121j | ||
| 72792 | 202179 | None | 52 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccnc2c1ccc1c(C)ccnc12 | 10.1021/jm301121j | ||
| CHEMBL593442 | 202179 | None | 52 | Human | Functional | pEC50 | = | 6.3 | 6.3 | 5 | 3 | Allosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR8 transfected in COS7 cells assessed as [3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccnc2c1ccc1c(C)ccnc12 | 10.1021/jm301121j | ||
Showing 1 to 50 of 317 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
| |
| 163322187 | 196450 | None | 10 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1ccccc1C(=O)Nc1c(C)cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)cc1Cl | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5424187 | 196450 | None | 10 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1ccccc1C(=O)Nc1c(C)cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)cc1Cl | 10.1021/acs.jmedchem.3c00030 | ||
| 172445647 | 195486 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 465 | 6 | 2 | 4 | 4.4 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5404620 | 195486 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 465 | 6 | 2 | 4 | 4.4 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| 167339834 | 195156 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1cccc(Cl)c1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5397693 | 195156 | None | 0 | Human | Binding | pIC50 | = | 8.9 | 8.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1cccc(Cl)c1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167339722 | 195818 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccc(Cl)cc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5411391 | 195818 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccc(Cl)cc1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167339983 | 195897 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1cc(Cl)ccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5412884 | 195897 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1cc(Cl)ccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| 91032188 | 193653 | None | 19 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 471 | 8 | 1 | 5 | 4.5 | COc1ccccc1Oc1cccc(CN2CCC3(CC2)C(=O)NCN3CCc2ccccc2)c1 | 10.1021/acs.jmedchem.6b01309 | ||
| CHEMBL5268017 | 193653 | None | 19 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 471 | 8 | 1 | 5 | 4.5 | COc1ccccc1Oc1cccc(CN2CCC3(CC2)C(=O)NCN3CCc2ccccc2)c1 | 10.1021/acs.jmedchem.6b01309 | ||
| 60016664 | 194059 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 527 | 11 | 1 | 5 | 5.8 | COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C(CCN3CCCC3)c3ccccc3)CC2)c1 | 10.1021/acs.jmedchem.6b01309 | ||
| CHEMBL5277802 | 194059 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 527 | 11 | 1 | 5 | 5.8 | COc1ccccc1Oc1cccc(CN2CCC(NC(=O)C(CCN3CCCC3)c3ccccc3)CC2)c1 | 10.1021/acs.jmedchem.6b01309 | ||
| 166926303 | 196807 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 451 | 6 | 3 | 4 | 4.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC(C)C2CCCNC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5432566 | 196807 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 451 | 6 | 3 | 4 | 4.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC(C)C2CCCNC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| 167339714 | 197032 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 487 | 8 | 2 | 6 | 3.1 | COC(=O)CN1CCC([C@@H](C)NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c(C)c2)CC1 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5437230 | 197032 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 487 | 8 | 2 | 6 | 3.1 | COC(=O)CN1CCC([C@@H](C)NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c(C)c2)CC1 | 10.1021/acs.jmedchem.3c00030 | ||
| 167339681 | 195313 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 443 | 7 | 2 | 4 | 3.8 | CCc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5400674 | 195313 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 443 | 7 | 2 | 4 | 3.8 | CCc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167339838 | 195319 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 451 | 6 | 3 | 4 | 4.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCNCC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5400852 | 195319 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 451 | 6 | 3 | 4 | 4.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCNCC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| 60016619 | 193840 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 526 | 10 | 2 | 7 | 4.3 | CCNS(=O)(=O)c1ccc(OC)cc1C1(O)CCN(Cc2cccc(Oc3ccccc3OC)c2)CC1 | 10.1021/acs.jmedchem.6b01309 | ||
| CHEMBL5272687 | 193840 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 526 | 10 | 2 | 7 | 4.3 | CCNS(=O)(=O)c1ccc(OC)cc1C1(O)CCN(Cc2cccc(Oc3ccccc3OC)c2)CC1 | 10.1021/acs.jmedchem.6b01309 | ||
| 172465785 | 196955 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)c(Cl)c1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5435573 | 196955 | None | 0 | Human | Binding | pIC50 | = | 6.8 | 6.8 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 463 | 6 | 2 | 4 | 4.2 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)c(Cl)c1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167339843 | 194979 | None | 0 | Human | Binding | pIC50 | = | 6.7 | 6.7 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 486 | 8 | 3 | 5 | 2.7 | CNC(=O)CN1CCC([C@@H](C)NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c(C)c2)CC1 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5394357 | 194979 | None | 0 | Human | Binding | pIC50 | = | 6.7 | 6.7 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 486 | 8 | 3 | 5 | 2.7 | CNC(=O)CN1CCC([C@@H](C)NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c(C)c2)CC1 | 10.1021/acs.jmedchem.3c00030 | ||
| 166926318 | 195613 | None | 9 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 429 | 6 | 2 | 4 | 3.6 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5407071 | 195613 | None | 9 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 429 | 6 | 2 | 4 | 3.6 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167339691 | 196801 | None | 0 | Human | Binding | pIC50 | = | 6.6 | 6.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 415 | 6 | 2 | 4 | 3.2 | Cc1cc(S(=O)(=O)NCC2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5432453 | 196801 | None | 0 | Human | Binding | pIC50 | = | 6.6 | 6.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 415 | 6 | 2 | 4 | 3.2 | Cc1cc(S(=O)(=O)NCC2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167339944 | 196917 | None | 0 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 457 | 8 | 2 | 4 | 4.3 | CCCN1CCC([C@@H](C)NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c(C)c2)CC1 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5434812 | 196917 | None | 0 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 457 | 8 | 2 | 4 | 4.3 | CCCN1CCC([C@@H](C)NS(=O)(=O)c2ccc(NC(=O)c3ccccc3C)c(C)c2)CC1 | 10.1021/acs.jmedchem.3c00030 | ||
| 167339894 | 195283 | None | 0 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 449 | 6 | 2 | 4 | 3.9 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)cc1Cl | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5400080 | 195283 | None | 0 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 449 | 6 | 2 | 4 | 3.9 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)cc1Cl | 10.1021/acs.jmedchem.3c00030 | ||
| 167339899 | 195872 | None | 0 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 435 | 6 | 2 | 4 | 3.9 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)C1CCCCCC1 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5412408 | 195872 | None | 0 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 435 | 6 | 2 | 4 | 3.9 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)C1CCCCCC1 | 10.1021/acs.jmedchem.3c00030 | ||
| 166926032 | 195241 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 451 | 6 | 3 | 4 | 4.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC(C)C2CCNCC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5399315 | 195241 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 451 | 6 | 3 | 4 | 4.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)NC(C)C2CCNCC2)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| 172457962 | 196476 | None | 0 | Human | Binding | pIC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 477 | 6 | 2 | 4 | 4.6 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C23CCN(CC2)CC3)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5424675 | 196476 | None | 0 | Human | Binding | pIC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 477 | 6 | 2 | 4 | 4.6 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C23CCN(CC2)CC3)c2ccccc12 | 10.1021/acs.jmedchem.3c00030 | ||
| 60016473 | 193727 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 433 | 7 | 2 | 5 | 4.7 | COc1ccccc1Oc1cccc(CN2CCC(O)(c3ccccc3C(=O)O)CC2)c1 | 10.1021/acs.jmedchem.6b01309 | ||
| CHEMBL5270110 | 193727 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Inhibition of CCR8 mutant (unknown origin)Inhibition of CCR8 mutant (unknown origin) |
ChEMBL | 433 | 7 | 2 | 5 | 4.7 | COc1ccccc1Oc1cccc(CN2CCC(O)(c3ccccc3C(=O)O)CC2)c1 | 10.1021/acs.jmedchem.6b01309 | ||
| 167339928 | 195750 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 435 | 6 | 2 | 5 | 3.6 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccsc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5410064 | 195750 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 435 | 6 | 2 | 5 | 3.6 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccsc1C | 10.1021/acs.jmedchem.3c00030 | ||
| 167529305 | 197035 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 440 | 6 | 2 | 5 | 3.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)cc1C#N | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5437244 | 197035 | None | 0 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Antagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assayAntagonist activity against CCR8 (unknown origin) expressed in CHO-K1 cells preincubated for 1 hr followed by CCL1 addition measured after 24 hrs by ONE-Glo assay |
ChEMBL | 440 | 6 | 2 | 5 | 3.1 | Cc1ccccc1C(=O)Nc1ccc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)cc1C#N | 10.1021/acs.jmedchem.3c00030 | ||
| 166926318 | 195613 | None | 9 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Inhibition of CCR8-mediated cell migration in CCL1-induced human PBMC preincubated for 1 hr followed by CCL1 addition measured after 4 hrs by cell counting methodInhibition of CCR8-mediated cell migration in CCL1-induced human PBMC preincubated for 1 hr followed by CCL1 addition measured after 4 hrs by cell counting method |
ChEMBL | 429 | 6 | 2 | 4 | 3.6 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
| CHEMBL5407071 | 195613 | None | 9 | Human | Binding | pIC50 | = | 7.5 | 7.5 | - | 0 | Inhibition of CCR8-mediated cell migration in CCL1-induced human PBMC preincubated for 1 hr followed by CCL1 addition measured after 4 hrs by cell counting methodInhibition of CCR8-mediated cell migration in CCL1-induced human PBMC preincubated for 1 hr followed by CCL1 addition measured after 4 hrs by cell counting method |
ChEMBL | 429 | 6 | 2 | 4 | 3.6 | Cc1cc(S(=O)(=O)N[C@H](C)C2CCN(C)CC2)ccc1NC(=O)c1ccccc1C | 10.1021/acs.jmedchem.3c00030 | ||
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