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
| |
| 93149 | 107257 | None | 55 | Human | Functional | pEC50 | = | 6 | 6.0 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1ccnc2c1ccc1cccnc12 | 10.1021/jm301121j | ||
| CHEMBL316589 | 107257 | None | 55 | Human | Functional | pEC50 | = | 6 | 6.0 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1ccnc2c1ccc1cccnc12 | 10.1021/jm301121j | ||
| 336912 | 83817 | None | 20 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 240 | 2 | 2 | 4 | 1.8 | OCc1ccc2ccc3ccc(CO)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL2205802 | 83817 | None | 20 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 240 | 2 | 2 | 4 | 1.8 | OCc1ccc2ccc3ccc(CO)nc3c2n1 | 10.1021/jm301121j | ||
| 2733927 | 83822 | None | 59 | Human | Functional | pEC50 | = | 5 | 5.0 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | 5.0 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 667748 | 83819 | None | 57 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.9 | 5.9 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 20445 | 83820 | None | 65 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -2 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 4.9 | 4.9 | -2 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 667748 | 83819 | None | 57 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.9 | 5.9 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 15783796 | 83825 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cnc2c(ccc3cccnc32)c1 | 10.1021/jm301121j | ||
| CHEMBL2205810 | 83825 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cnc2c(ccc3cccnc32)c1 | 10.1021/jm301121j | ||
| 602123 | 83818 | None | 43 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL2205803 | 83818 | None | 43 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 | 10.1021/jm301121j | ||
| 20445 | 83820 | None | 65 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -2 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 4.9 | 4.9 | -2 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 15783796 | 83825 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cnc2c(ccc3cccnc32)c1 | 10.1021/jm301121j | ||
| CHEMBL2205810 | 83825 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cnc2c(ccc3cccnc32)c1 | 10.1021/jm301121j | ||
| 602123 | 83818 | None | 43 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL2205803 | 83818 | None | 43 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 236 | 2 | 0 | 4 | 2.4 | O=Cc1ccc2ccc3ccc(C=O)nc3c2n1 | 10.1021/jm301121j | ||
| 74265 | 210806 | None | 69 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.8 | 5.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 353741 | 72088 | None | 4 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 364 | 2 | 0 | 2 | 4.6 | BrCc1ccc2ccc3ccc(CBr)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL1976682 | 72088 | None | 4 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 364 | 2 | 0 | 2 | 4.6 | BrCc1ccc2ccc3ccc(CBr)nc3c2n1 | 10.1021/jm301121j | ||
| 65237 | 137711 | None | 68 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 28 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccc2ccc3ccc(C)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL375781 | 137711 | None | 68 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 28 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccc2ccc3ccc(C)nc3c2n1 | 10.1021/jm301121j | ||
| 74265 | 210806 | None | 69 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.8 | 5.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | ||
| 353741 | 72088 | None | 4 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 364 | 2 | 0 | 2 | 4.6 | BrCc1ccc2ccc3ccc(CBr)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL1976682 | 72088 | None | 4 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 364 | 2 | 0 | 2 | 4.6 | BrCc1ccc2ccc3ccc(CBr)nc3c2n1 | 10.1021/jm301121j | ||
| 15664 | 83821 | None | 63 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccc(-c2ccc(C)cn2)nc1 | 10.1021/jm301121j | ||
| CHEMBL2205807 | 83821 | None | 63 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccc(-c2ccc(C)cn2)nc1 | 10.1021/jm301121j | ||
| 65237 | 137711 | None | 68 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 28 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccc2ccc3ccc(C)nc3c2n1 | 10.1021/jm301121j | ||
| CHEMBL375781 | 137711 | None | 68 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 28 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 208 | 0 | 0 | 2 | 3.4 | Cc1ccc2ccc3ccc(C)nc3c2n1 | 10.1021/jm301121j | ||
| 15664 | 83821 | None | 63 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccc(-c2ccc(C)cn2)nc1 | 10.1021/jm301121j | ||
| CHEMBL2205807 | 83821 | None | 63 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -3 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 184 | 1 | 0 | 2 | 2.8 | Cc1ccc(-c2ccc(C)cn2)nc1 | 10.1021/jm301121j | ||
| 72791 | 210699 | None | 48 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.8 | 5.8 | 1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 214 | 0 | 0 | 2 | 3.4 | Clc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 72791 | 210699 | None | 48 | Human | Functional | pEC50 | = | 5.7 | 5.7 | 1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 194 | 0 | 0 | 2 | 3.1 | Cc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 12041800 | 205951 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopyAgonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopy |
ChEMBL | 410 | 7 | 2 | 4 | 6.4 | Clc1ccc2c(NCCCCNc3ccnc4cc(Cl)ccc34)ccnc2c1 | 10.1016/j.bmcl.2011.11.014 | ||
| CHEMBL66165 | 205951 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopyAgonist activity at human CCR1 expressed in CHO cells by cellular dielectric spectroscopy |
ChEMBL | 410 | 7 | 2 | 4 | 6.4 | Clc1ccc2c(NCCCCNc3ccnc4cc(Cl)ccc34)ccnc2c1 | 10.1016/j.bmcl.2011.11.014 | ||
| 77865 | 107342 | None | 51 | Human | Functional | pEC50 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 5.7 | 5.7 | -1 | 2 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 214 | 0 | 0 | 2 | 3.4 | Clc1cc2cccnc2c2ncccc12 | 10.1021/jm301121j | ||
| 1474 | 154488 | None | 79 | Human | Functional | pEC50 | = | 4.5 | 4.5 | 1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr 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 | = | 4.5 | 4.5 | 1 | 3 | Allosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysisAllosteric modulation at human CCR1 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as {3H]IP3 turnover by liquid scintillation counting analysis |
ChEMBL | 156 | 1 | 0 | 2 | 2.1 | c1ccc(-c2ccccn2)nc1 | 10.1021/jm301121j | ||
Showing 1 to 50 of 728 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
| |
| 72548703 | 161661 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysis |
ChEMBL | 583 | 8 | 3 | 6 | 5.8 | CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 | 10.1016/j.bmcl.2018.03.093 | ||
| CHEMBL4128926 | 161661 | None | 0 | Human | Binding | pIC50 | = | 10.1 | 10.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 receptor after 120 mins by scintillation counting analysis |
ChEMBL | 583 | 8 | 3 | 6 | 5.8 | CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 | 10.1016/j.bmcl.2018.03.093 | ||
| 25109291 | 191495 | None | 6 | Human | Binding | pIC50 | = | 10.1 | 10.1 | 56 | 12 | Displacement of radiolabeled MIP1alpha from human CCR1 receptorDisplacement of radiolabeled MIP1alpha from human CCR1 receptor |
ChEMBL | 327 | 1 | 2 | 6 | 1.7 | Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 | 10.1021/jm8007618 | ||
| CHEMBL519240 | 191495 | None | 6 | Human | Binding | pIC50 | = | 10.1 | 10.1 | 56 | 12 | Displacement of radiolabeled MIP1alpha from human CCR1 receptorDisplacement of radiolabeled MIP1alpha from human CCR1 receptor |
ChEMBL | 327 | 1 | 2 | 6 | 1.7 | Nc1nc2c(c(N3CCNCC3)n1)CCC1=C2[C@@H]2CCCC[C@@H]2O1 | 10.1021/jm8007618 | ||
| 59278286 | 171658 | None | 1 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay |
ChEMBL | 453 | 6 | 1 | 7 | 3.2 | CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 | 10.1016/j.bmcl.2018.12.024 | ||
| CHEMBL4464625 | 171658 | None | 1 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay |
ChEMBL | 453 | 6 | 1 | 7 | 3.2 | CC[C@H](NC(=O)c1cncc2c1cnn2-c1ccc(F)cc1)c1ccnc(S(C)(=O)=O)c1 | 10.1016/j.bmcl.2018.12.024 | ||
| 11744314 | 87388 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay |
ChEMBL | 446 | 6 | 3 | 6 | 3.2 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2013.04.047 | ||
| CHEMBL2332935 | 87388 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay |
ChEMBL | 446 | 6 | 3 | 6 | 3.2 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2013.04.047 | ||
| 68959963 | 87386 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 432 | 6 | 2 | 5 | 3.1 | CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332933 | 87386 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 432 | 6 | 2 | 5 | 3.1 | CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| 11744314 | 87388 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 446 | 6 | 3 | 6 | 3.2 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332935 | 87388 | None | 0 | Human | Binding | pIC50 | = | 9.4 | 9.4 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 446 | 6 | 3 | 6 | 3.2 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| 10094212 | 87389 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay |
ChEMBL | 430 | 6 | 3 | 6 | 2.7 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2013.04.047 | ||
| CHEMBL2332936 | 87389 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay |
ChEMBL | 430 | 6 | 3 | 6 | 2.7 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2013.04.047 | ||
| 10094212 | 87389 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 430 | 6 | 3 | 6 | 2.7 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332936 | 87389 | None | 0 | Human | Binding | pIC50 | = | 9.3 | 9.3 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 430 | 6 | 3 | 6 | 2.7 | CC(=O)Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| 72945512 | 104381 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis |
ChEMBL | 471 | 7 | 4 | 6 | 3.0 | O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)NC1CC1 | 10.1016/j.bmcl.2013.11.062 | ||
| CHEMBL3099947 | 104381 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis |
ChEMBL | 471 | 7 | 4 | 6 | 3.0 | O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2)NC1CC1 | 10.1016/j.bmcl.2013.11.062 | ||
| 10478859 | 87384 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 448 | 6 | 2 | 5 | 3.6 | CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332931 | 87384 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 448 | 6 | 2 | 5 | 3.6 | CC(=O)Nc1ccc(F)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| 25141109 | 130348 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay |
ChEMBL | 493 | 5 | 4 | 4 | 3.8 | C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O | nan | ||
| CHEMBL3679659 | 130348 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Displacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assayDisplacement of [125I]-MIP-1alpha from CCR1 in human THP1 cells after 12 hrs by scintillation proximity assay |
ChEMBL | 493 | 5 | 4 | 4 | 3.8 | C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O | nan | ||
| 25141109 | 130348 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA). |
ChEMBL | 493 | 5 | 4 | 4 | 3.8 | C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O | nan | ||
| CHEMBL3679659 | 130348 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA).Scintillation Proximity Assay (SPA): CCR1 ligand binding using scintillation proximity assay (SPA). |
ChEMBL | 493 | 5 | 4 | 4 | 3.8 | C[C@H](NC(=O)N[C@@H]1CCCC[C@@H]1C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1)C(C)(C)O | nan | ||
| 71570633 | 87393 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 445 | 6 | 3 | 6 | 3.2 | CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332940 | 87393 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 445 | 6 | 3 | 6 | 3.2 | CC(=O)Nc1ccc(O)cc1OC[C@@H](N)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| 21070989 | 86923 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxis |
ChEMBL | 450 | 4 | 0 | 5 | 3.9 | COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl | 10.1016/j.bmcl.2013.01.005 | ||
| CHEMBL2322875 | 86923 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxisAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of CCL5/RANTES-induced chemotaxis |
ChEMBL | 450 | 4 | 0 | 5 | 3.9 | COc1cc(N2CCN(C(=O)Cn3nc(C(F)(F)F)c(Cl)c3C)CC2)ccc1Cl | 10.1016/j.bmcl.2013.01.005 | ||
| 57889003 | 91189 | None | 5 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity to human CCR1Binding affinity to human CCR1 |
ChEMBL | 450 | 5 | 3 | 4 | 3.1 | CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 | 10.1016/j.bmcl.2013.04.079 | ||
| CHEMBL2398726 | 91189 | None | 5 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity to human CCR1Binding affinity to human CCR1 |
ChEMBL | 450 | 5 | 3 | 4 | 3.1 | CC(C)[C@@H](NC(=O)[C@@H]1CC[C@@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 | 10.1016/j.bmcl.2013.04.079 | ||
| 57888919 | 91192 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity to human CCR1Binding affinity to human CCR1 |
ChEMBL | 450 | 5 | 3 | 4 | 3.1 | CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 | 10.1016/j.bmcl.2013.04.079 | ||
| CHEMBL2398729 | 91192 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity to human CCR1Binding affinity to human CCR1 |
ChEMBL | 450 | 5 | 3 | 4 | 3.1 | CC(C)[C@@H](NC(=O)[C@@H]1CC[C@H](O)C1)C(=O)N1CC[C@](O)(c2ccc(Cl)cc2)C(C)(C)C1 | 10.1016/j.bmcl.2013.04.079 | ||
| 72945510 | 104379 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis |
ChEMBL | 487 | 7 | 4 | 6 | 3.5 | O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)NC1CC1 | 10.1016/j.bmcl.2013.11.062 | ||
| CHEMBL3099945 | 104379 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysisDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cell membranes after 1.5 hrs by microbeta counting analysis |
ChEMBL | 487 | 7 | 4 | 6 | 3.5 | O=C(Nc1ccc(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)NC1CC1 | 10.1016/j.bmcl.2013.11.062 | ||
| 6918497 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity towards C-C chemokine receptor type 1Binding affinity towards C-C chemokine receptor type 1 |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1016/s0960-894x(03)00748-0 | ||
| CHEMBL277930 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity towards C-C chemokine receptor type 1Binding affinity towards C-C chemokine receptor type 1 |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1016/s0960-894x(03)00748-0 | ||
| CHEMBL331897 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Binding affinity towards C-C chemokine receptor type 1Binding affinity towards C-C chemokine receptor type 1 |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1016/s0960-894x(03)00748-0 | ||
| 6918497 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1016/s0960-894x(01)00176-7 | ||
| CHEMBL277930 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1016/s0960-894x(01)00176-7 | ||
| CHEMBL331897 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Concentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cellsConcentration required for 50% inhibition of [125I]eotaxin binding to human CCR1 receptor expressed in CHO cells |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1016/s0960-894x(01)00176-7 | ||
| 10389562 | 87383 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 460 | 7 | 2 | 6 | 3.5 | COc1ccc(NC(C)=O)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332930 | 87383 | None | 0 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 460 | 7 | 2 | 6 | 3.5 | COc1ccc(NC(C)=O)c(OC[C@@H](O)CN2CCC3(CC2)Cc2cc(Cl)ccc2O3)c1 | 10.1016/j.bmcl.2012.12.095 | ||
| 6918497 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors. |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1021/jm0004244 | ||
| CHEMBL277930 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors. |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1021/jm0004244 | ||
| CHEMBL331897 | 113493 | None | 1 | Human | Binding | pIC50 | = | 9.1 | 9.1 | - | 0 | Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors. |
ChEMBL | 527 | 5 | 1 | 2 | 7.6 | CC[N+]1(C/C2=C/CCCCCC2)CCC(NC(=O)C2c3cc(Cl)ccc3Oc3ccc(Cl)cc32)CC1 | 10.1021/jm0004244 | ||
| 10032207 | 90819 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay |
ChEMBL | 536 | 6 | 3 | 7 | 3.1 | O=C(c1cc(Cl)c(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 | 10.1016/j.bmcl.2013.04.047 | ||
| CHEMBL2391803 | 90819 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assayAntagonist activity at CCR1 in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 2 hrs by fluorescence assay |
ChEMBL | 536 | 6 | 3 | 7 | 3.1 | O=C(c1cc(Cl)c(O)cc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2)N1CC[C@H](O)C1 | 10.1016/j.bmcl.2013.04.047 | ||
| 9954423 | 87385 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 430 | 6 | 2 | 5 | 3.5 | CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| CHEMBL2332932 | 87385 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 430 | 6 | 2 | 5 | 3.5 | CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(Cl)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
| 10409538 | 87387 | None | 0 | Human | Binding | pIC50 | = | 9.0 | 9.0 | - | 0 | Displacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrsDisplacement of [125I]MIP-1alpha from human recombinant CCR1 expressed in HEK293 cells after 1.5 hrs |
ChEMBL | 414 | 6 | 2 | 5 | 3.0 | CC(=O)Nc1ccccc1OC[C@@H](O)CN1CCC2(CC1)Cc1cc(F)ccc1O2 | 10.1016/j.bmcl.2012.12.095 | ||
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