Target family: Class A Orphans (type: gpcr)
Target: <i>GPR139</i>

Ligand: zelatriazin (TAK-041) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia.
Published in: J Med Chem

Ligand: zelatriazin (TAK-041) (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.659999847412109 pEC50
Reference (Journal): Discovery of TAK-041: a Potent and Selective GPR139 Agonist Explored for the Treatment of Negative Symptoms Associated with Schizophrenia.
Published in: J Med Chem

Ligand: NCRW0105-E06 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.289999961853027 pIC50
Reference (Journal): Pharmacological characterization of novel small molecule agonists and antagonists for the orphan receptor GPR139.
Published in: Eur J Pharmacol

Ligand: NCRW0005-F05 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.679999828338623 pIC50
Reference (Journal): High-throughput screening of antagonists for the orphan G-protein coupled receptor GPR139.
Published in: Acta Pharmacol Sin

Ligand: L-tryptophan (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 3.6600000858306885 pEC50
Reference (Journal): Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139.
Published in: J Chem Inf Model

Ligand: L-tryptophan (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 3.130000114440918 pKi
Reference (Journal): GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Published in: Mol Pharmacol

Ligand: L-tryptophan (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 4.590000152587891 pIC50
Reference (Journal): GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Published in: Mol Pharmacol

Ligand: L-phenylalanine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 4.510000228881836 pIC50
Reference (Journal): GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Published in: Mol Pharmacol

Ligand: L-phenylalanine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 3.059999942779541 pKi
Reference (Journal): GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Published in: Mol Pharmacol

Ligand: L-phenylalanine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 3.490000009536743 pEC50
Reference (Journal): Computer-aided discovery of aromatic l-α-amino acids as agonists of the orphan G protein-coupled receptor GPR139.
Published in: J Chem Inf Model

Ligand: LP-471756 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.190000057220459 pIC50
Reference (Journal): Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139.
Published in: J Biomol Screen

Ligand: LP-360924 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification of surrogate agonists and antagonists for orphan G-protein-coupled receptor GPR139.
Published in: J Biomol Screen

Ligand: JNJ-63533054 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.619999885559082 pKi
Reference (Journal): GPR139, an Orphan Receptor Highly Enriched in the Habenula and Septum, Is Activated by the Essential Amino Acids L-Tryptophan and L-Phenylalanine.
Published in: Mol Pharmacol

Ligand: compound 1a [PMID: 24900311] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.409999847412109 pEC50
Reference (Journal): Discovery and SAR of a Series of Agonists at Orphan G Protein-Coupled Receptor 139.
Published in: ACS Med Chem Lett