Target family: Proteinase-activated receptors (type: gpcr)
Target: PAR2

Ligand: P2pal18S (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pIC50

Ligand: Isox-Cha-Chg-ARK(Sulfo-Cy5)-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pEC50
Reference (Journal): High Affinity Fluorescent Probe for Proteinase-Activated Receptor 2 (PAR2).
Published in: ACS Med Chem Lett

Ligand: Isox-Cha-Chg-Ala-Arg-Dpr(4FB)-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pEC50
Reference (Journal): Protease-activated receptor 2 (PAR2)-targeting peptide derivatives for positron emission tomography (PET) imaging.
Published in: Eur J Med Chem

Ligand: I-287 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.139999866485596 pIC50
Reference (Journal): The PAR2 inhibitor I-287 selectively targets G&#x3b1;<sub>q</sub> and G&#x3b1;<sub>12/13</sub> signaling and has anti-inflammatory effects.
Published in: Commun Biol

Ligand: I-287 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.409999847412109 pIC50
Reference (Journal): The PAR2 inhibitor I-287 selectively targets G&#x3b1;<sub>q</sub> and G&#x3b1;<sub>12/13</sub> signaling and has anti-inflammatory effects.
Published in: Commun Biol

Ligand: I-191 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): A Potent Antagonist of Protease-Activated Receptor 2 That Inhibits Multiple Signaling Functions in Human Cancer Cells.
Published in: J Pharmacol Exp Ther

Ligand: GB88 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110).
Published in: Br J Pharmacol

Ligand: GB110 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.55 pEC50
Reference (Journal): Novel agonists and antagonists for human protease activated receptor 2.
Published in: J Med Chem

Ligand: C391 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.840000152587891 pIC50
Reference (Journal): The novel PAR2 ligand C391 blocks multiple PAR2 signalling pathways in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: C391 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.889999866485596 pIC50
Reference (Journal): The novel PAR2 ligand C391 blocks multiple PAR2 signalling pathways in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: AZ8838 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pIC50
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ8838 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 6.460000038146973 pKd
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ8838 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.639999866485596 pIC50
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ7188 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.21999979019165 pIC50
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ3451 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 7.869999885559082 pKd
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ3451 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pIC50
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ3451 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: yes
Median affinity: 8.270000457763672 pIC50
Reference (Journal): Structural insight into allosteric modulation of protease-activated receptor 2.
Published in: Nature

Ligand: AZ2429 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition.
Published in: Commun Biol

Ligand: AY77 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pEC50
Reference (Journal): Potent Small Agonists of Protease Activated Receptor 2.
Published in: ACS Med Chem Lett

Ligand: AC-98170 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pEC50
Reference (Journal): Discovery of potent and selective small-molecule PAR-2 agonists.
Published in: J Med Chem

Ligand: AC-55541 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pEC50
Reference (Journal): Discovery of potent and selective small-molecule PAR-2 agonists.
Published in: J Med Chem

Ligand: trans-cinnamoyl-LIGRLO [N-[3H]propionyl]-NH2 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.
Published in: J Pharmacol Exp Ther