| | | | GPI | MVD | |
| Nos. | Compounds | | IC50 (nM)a | pA2b | IC50 (nM) | pA2 | Reference |
| 1 | H-Tyr-Pro-Trp-Phe-NH2 | (EM-1) | 4.03 | —c | 283 | — | [10] | 2 | H-Tyr-Pro-Phe-Phe-NH2 | (EM-2) | 6.88 | — | 344 | — | [10] | 19 | H-Dmt-Pro-Trp-Phe-NH2 | | 0.27 | — | >10,000 | 8.6 | [10] | 20 | H-Dmt-Pro-Phe-Phe-NH2 | | 0.07 | — | 1.87 | — | [9] | 21 | H-Dmt-Pro-Phe-NH2 | | 2.33 | — | 113 | — | [9] | 22 | H-Dmt-Pro-Phe-NH-C2H4-Ph | | 5.03 | — | >10,000 | 7.05 | [9] | 23 | H-Dmt-Pro-Phe-NH-Bzl | | 22 | — | >10,000 | 7.18 | [11] | 24 | H-Dmt-Pro-Phe-NH-Ph | | 37.7 | — | >10,000 | 6.94 | [11] | 25 | H-Dmt-Pro-Phe-NH-4-Pyr | | 11.8 | — | >10,000 | 6.52 | [11] | 26 | H-Dmt-Pro-Phe-NH-3-Pyr | | 72.8 | — | >10,000 | 6.33 | [11] | 27 | H-Dmt-Pro-Phe-NH-2-Pyr | | 15 | — | >10,000 | 6.7 | [11] | 28 | H-Dmt-Pro-Phe-NH-1-Nph | | 0.49 | — | 5.47 | — | [11] | 29 | H-Dmt-Pro-Phe-NH-3-Qln | | 9.14 | — | >10,000 | 5.93 | [11] | 30 | H-Dmt-Pro-Phe-NH-5-Qln | | 0.26 | — | 0.616 | 5.88 | [11] | 31 | H-Dmt-Pro-Phe-NH-6-Qln | | 6.21 | — | >10,000 | 5.41 | [11] | 32 | H-Dmt-Pro-Phe-NH-8-Qln | | 445 | — | 2,981 | 6.14 | [11] | 33 | H-Dmt-Pro-Phe-NH-5-Isq | | 0.94 | — | >10,000 | 6.12 | [11] | 34 | H-Mmt-Pro-Phe-Phe-NH2 | | 0.924 | — | 28.7 | ++d | [12] | 35 | H-Emt-Pro-Phe-Phe-NH2 | | 0.623 | — | 1.08 | +e | [12] | 36 | H-Imt-Pro-Phe-Phe-NH2 | | 10.6 | — | 601 | + | [12] | 37 | H-Det-Pro-Phe-Phe-NH2 | | 0.903 | — | 47.1 | + | [12] | 38 | H-Dit-Pro-Phe-Phe-NH2 | | 299 | — | >10,000 | NDf | [12] | 39 | H-Tmt-Pro-Phe-Phe-NH2 | | 2.31 | — | 46.4 | ++ | [12] | 40 | H-Dmt-Pro-Mmp-Phe-NH2 | | 0.16 | — | >10,000 | 6.59 | [13] | 41 | H-Dmt-Pro-3,5Dmp-Phe-NH2 | | 14.4 | — | >10,000 | 6.77 | [13] | 42 | H-Dmt-Pro-Dmp-Phe-NH2 | | 0.12 | — | >10,000 | 8.15 | [13] | 43 | H-Dmt-Pro-Dmt-Phe-NH2 | | 1.94 | — | >10,000 | 7.06 | [13] | 44 | H-Dmt-Pro-Tmp-Phe-NH2 | | 0.21 | — | >10,000 | 9.05 | [13] | 45 | H-Dmt-Pro-Emp-Phe-NH2 | | 0.17 | — | 0.51 | — | [13] | 46 | H-Dmt-Pro-Imp-Phe-NH2 | | 0.2 | — | 5.56 | — | [13] | 47 | [N-allyl-Dmt1]EM-1 | | >10,000 | 8.18 | >10,000 | 7.32 | [10] | 48 | [N-allyl-Dmt1]EM-2 | | >10,000 | 8.59 | >10,000 | 6.32 | [10] | 49 | 1,6-bis[N-allyl-Dmt-NH]hexane | | >10,000 | 7.23 | >10,000 | 6.83 | [10] | 50 | 3,6-bis[N-allyl-Dmt-NH-propyl]-5-methyl-2(1H)-pyrazinone | | >10,000 | 7.17 | >10,000 | 6.38 | [10] |
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