Table 1 Binding affinity and co-operativity of ligands as activators of human GPR84.

From: On-target and off-target effects of novel orthosteric and allosteric activators of GPR84

Agonista Modulatorb logα logβ pKAc pKBd
2-HTP PSB-16671 2.41 ± 0.17 −0.15 ± 0.06 7.0 ± 0.2 6.02 ± 0.13
PSB-16671 2-HTP 2.02 ± 0.11 0.37 ± 0.12 6.1 ± 0.1 7.42 ± 0.07
  1. aAgonist is the compound used to generate concentration-response curve.
  2. bModulator is the compound used in defined concentrations.
  3. cpKA are values estimated for the agonist.
  4. dpKB are values estimated for the modulator.
  5. Data are means ± SEM, n = 4.
  6. Flp-In T-REx 293 cells harbouring a human GPR84-Gαi2 fusion protein were treated with doxycycline (100 ng.ml−1, 24 h) to induced expression of the fusion protein. [35S]GTPγS binding studies were then performed as described in Fig. 1 and binding affinity and cooperativity factors extracted from such data.