PG 97-269

Ligand Id: 2268
Ligand name PG 97-269


Selectivity at human GPCRs
Key to terms and symbols Click column headers to sort
Target Type Action Affinity Units Concentration range (M) Reference
VPAC1 receptor Antagonist Antagonist 7.1 – 8.7 pIC50 - 1-2,4
pIC50 8.7 (IC50 2x10-9 M) [4]
Description: cyclic AMP formation in CHO cells stably expressing recombinant receptor
pIC50 8.7 (IC50 2x10-9 M) [2]
Description: inhibition of [125I]-VIP binding to membranes from LoVo cells endogenously expressing the receptor
pIC50 8.7 (IC50 2x10-9 M) [4]
Description: inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor
pIC50 8.0 (IC50 9.9x10-9 M) [1]
Description: inhibition of calcium influx stimulated by 30nM VIP in CHO cells stably expressing recombinant receptor
pIC50 7.1 (IC50 8x10-8 M) [1]
Description: inhibition of cyclic AMP formation stimulated by 0.3nM VIP in CHO cells stably expressing recombinant receptor
VPAC2 receptor Antagonist Antagonist 5.5 – 5.7 pIC50 - 2,4
pIC50 5.7 (IC50 2x10-6 M) [4]
Description: inhibition of [125I]Ro25 1553 binding to membranes from CHO cells stably expressing the recombinant receptor
pIC50 5.5 (IC50 3x10-6 M) [2]
Description: inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor
PAC1 receptor Antagonist Antagonist - - - 3
[3]
Selectivity at rat GPCRs
Key to terms and symbols Click column headers to sort
Target Type Action Affinity Units Concentration range (M) Reference
VPAC1 receptor Antagonist Antagonist 8.0 pIC50 - 2
pIC50 8.0 (IC50 1x10-8 M) [2]
Description: inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor
VPAC2 receptor Antagonist Antagonist 5.7 pIC50 - 2
pIC50 5.7 (IC50 2x10-6 M) [2]
Description: inhibition of [125I]-VIP binding to membranes from CHO cells stably expressing the recombinant receptor
PAC1 receptor Antagonist Antagonist 4.5 pIC50 - 2
pIC50 4.5 (IC50 3x10-5 M) [2]
Description: inhibition of [125I]-[Ac-His1]PACAP-27 binding to membranes from CHO cells stably expressing the recombinant receptor