Table 3.
Solved GPCR structures complexed with synthetic allosteric modulators bound to the transmembrane domain inside 7TMD
| Structure Type | GPCR type | GPCR | Modulator | Highest Phase | Modulator type | Number | PDB code | Allosteric site | Refs |
|---|---|---|---|---|---|---|---|---|---|
| Cryo-EM | class A | FFAR3 | AR420626 | Pre-clinical | PAM | (52) | 8J20 | inside 7TMD | 469 |
| X-ray diffraction | class B | CRF1R | CP-376395 | Pre-clinical | Allosteric antagonist | (53) | 4K5Y | inside 7TMD | 470 |
| Cryo-EM | class B | PTH1R | PCO371 | Pre-clinical | Allosteric agonist | (54) | 8GW8 | inside 7TMD | 335 |
| X-ray diffraction | class C | mGluR5 | mavoglurant | Phase 3 | NAM | (55) | 4OO9 | inside 7TMD | 178 |
| X-ray diffraction | class C | mGluR5 | compound 14 | Pre-clinical | NAM | (56) | 5CGC | inside 7TMD | 321 |
| X-ray diffraction | class C | mGluR5 | HTL14242 | Phase 1 | NAM | (57) | 5CGD | inside 7TMD | 321 |
| X-ray diffraction | class C | mGluR5 | Fenobam | Phase 1 | NAM | (58) | 6FFH | inside 7TMD | 471 |
| X-ray diffraction | class C | mGluR5 | M-MPEP | Pre-clinical | NAM | (59) | 6FFI | inside 7TMD | 471 |
| Cryo-EM | class C | mGluR5 | CDPPB | Pre-clinical | PAM | (60) | 8TAO | inside 7TMD | 325 |