Table 3. Ligand potency (EC50 value) and efficacy (Emax value) for the human GCGR family.
huGIPR | huGLP1R | huGLP2R | huGCGR | |||||
peptides | EC50 | Emax | EC50 | Emax | EC50 | Emax | EC50 | Emax |
[nM] | [foldinduction] | [nM] | [foldinduction] | [nM] | [foldinduction] | [nM] | [foldinduction] | |
Exe-4 | 22.86±5.61 | 5.36±0.15 | 0.09±0.03 | 40.95±1.51 | 107.15±31.35 | 6.29±0.28 | NR | NR |
chGCRP | NR | 3.03±2.41 | 48.87±9.15 | 19.84±0.57 | 591.56±126.74 | 6.32±0.24 | 42.66±14.47 | 6.32±0.24 |
xeGCRP | NR | 1.95±0.14 | >1000 | 24.11±1.68 | NR | NR | 181.55±39.49 | 2.09±0.12 |
mdGCRP | NR | 2.11±0.09 | 155.96±32.84 | 20.90±0.74 | NR | NR | 175.39±41.78 | 2.27±0.11 |
huGIP | 0.17±0.05 | 5.21±0.12 | ND | ND | ND | ND | ND | ND |
huGLP1 | ND | ND | 0.14±0.03 | 40.61±0.73 | ND | ND | ND | ND |
huGLP2 | ND | ND | ND | ND | 0.89±0.25 | 6.09±0.09 | ND | ND |
huGCG | ND | ND | ND | ND | ND | ND | 0.78±0.21 | 6.09±0.18 |
Results are presented as mean ± S.E. of at least three independent experiments. NR, no response; ND, not determined.