Radioligand - Construct | Endogenous Ligands (CCL2 or CCL3) | Orthosteric INCB3344 | Allosteric CCR2-RA-[R] | Allosteric JNJ-27141491 | Allosteric SD-24 | ||||
---|---|---|---|---|---|---|---|---|---|
[125I]CCL2 - CCR2 | 9.7 ± 0.2a | (0.21) | 7.8 ± 0.2 | (16) | 6.1 ± 0.1 | (746) | 6.6 ± 0.1 | (241) | < 5 |
[125I]CCL3 - CCR5 | 8.7 ± 0.4b | (1.9) | 5.3 ± 0.2 | (4508) | < 5 | 5.4 ± 0.1 | (4254) | no displacement | |
[125I]CCL2 - CCR5-CCR2(all) | 8.9 ± 0.3a | (1.3) | 6.3 ± 0.1** | (516) | < 5 | 5.0 ± 0.1* | (10650) | no displacement | |
[125I]CCL3 - CCR5-CCR2(C-term) | 8.9 ± 0.2b | (1.4) | no displacement | 5.1 ± 0.1 | (7638) | < 5 | no displacement | ||
[125I]CCL2 - CCR2-CCR5(C-term) | 8.9 ± 0.2a | (1.4) | 7.3 ± 0.1 | (48) | 5.7 ± 0.2 | (1908) | 6.4 ± 0.1 | (364) | < 5 |