Target family: Parathyroid hormone receptors (type: gpcr)
Target: PTH1 receptor

Ligand: abaloparatide (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2017)
Primary target: yes
Median affinity:  -
Reference (Journal): Parathyroid hormone and parathyroid hormone-related protein analogs as therapies for osteoporosis.
Published in: Curr Osteoporos Rep

Ligand: [Ala1,12,Aib3,Gln10,hArg11,Trp14,Arg19]PTH-(1-21)-NH2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pIC50
Reference (Journal): Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation.
Published in: Proc Natl Acad Sci USA

Ligand: [Ala1,12,Aib3,Gln10,hArg11,Trp14,Arg19]PTH-(1-28)-NH2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation.
Published in: Proc Natl Acad Sci USA

Ligand: [Ala1,12,Aib3,Gln10,hArg11,Trp14,Arg19]PTH-(1-34)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation.
Published in: Proc Natl Acad Sci USA

Ligand: [Ala1,12,Aib3,Gln10,hArg11,Trp14]PTH-(1-14)-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.5 pIC50
Reference (Journal): Prolonged signaling at the parathyroid hormone receptor by peptide ligands targeted to a specific receptor conformation.
Published in: Proc Natl Acad Sci USA

Ligand: [Arg19]PTH-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: DS69910557 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pIC50
Reference (Journal): Lead optimization of pyrido[2,3-d][1]benzazepin-6-one derivatives leading to the discovery of a potent, selective, and orally available human parathyroid hormone receptor 1 (hPTHR1) antagonist (DS69910557).
Published in: Bioorg Med Chem

Ligand: [D-Trp12,Tyr34]PTH-(7-34) (bovine) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Tuberoinfundibular peptide (7-39) [TIP(7-39)], a novel, selective, high-affinity antagonist for the parathyroid hormone-1 receptor with no detectable agonist activity.
Published in: J Pharmacol Exp Ther

Ligand: [His5,Arg19]PTH-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: [His5]PTH-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.1 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: [His5]PTH-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: [Ile5,Glu19]PTHrP-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: [Ile5,Glu19,Val21]PTHrP-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: [Ile5]PTHrP-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: [Ile5]PTHrP-(1-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: [Ile5,Trp23]PTHrP-(1-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: [Ile5,Trp23]PTHrP-(1-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Studies of the N-terminal region of a parathyroid hormone-related peptide (1-36) analog: receptor subtype-selective agonists, antagonists, and photochemical cross-linking agents.
Published in: Endocrinology

Ligand: [Ile5,Trp23]PTHrP-(2-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Studies of the N-terminal region of a parathyroid hormone-related peptide (1-36) analog: receptor subtype-selective agonists, antagonists, and photochemical cross-linking agents.
Published in: Endocrinology

Ligand: [Ile5,Trp23]PTHrP-(3-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Studies of the N-terminal region of a parathyroid hormone-related peptide (1-36) analog: receptor subtype-selective agonists, antagonists, and photochemical cross-linking agents.
Published in: Endocrinology

Ligand: [Ile5,Trp23]PTHrP-(4-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Studies of the N-terminal region of a parathyroid hormone-related peptide (1-36) analog: receptor subtype-selective agonists, antagonists, and photochemical cross-linking agents.
Published in: Endocrinology

Ligand: [Ile5,Trp23]PTHrP-(5-36) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Studies of the N-terminal region of a parathyroid hormone-related peptide (1-36) analog: receptor subtype-selective agonists, antagonists, and photochemical cross-linking agents.
Published in: Endocrinology

Ligand: [Ile5,Trp23,Tyr36]PTHrP-(1-36)-NH2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.5 pIC50
Reference (Journal): Residues in the membrane-spanning and extracellular loop regions of the parathyroid hormone (PTH)-2 receptor determine signaling selectivity for PTH and PTH-related peptide.
Published in: J Biol Chem

Ligand: [Ile5,Val21]PTHrP-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: [Nle8,18,Tyr34]PTH-(1-34)-NH2 (bovine) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Transmembrane residues of the parathyroid hormone (PTH)/PTH-related peptide receptor that specifically affect binding and signaling by agonist ligands.
Published in: J Biol Chem

Ligand: [Nle8,18,Tyr34]PTH-(3-34)-NH2 (bovine) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Transmembrane residues of the parathyroid hormone (PTH)/PTH-related peptide receptor that specifically affect binding and signaling by agonist ligands.
Published in: J Biol Chem

Ligand: PCO371 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.389999866485596 pEC50
Reference (Journal): Lead Optimization and Avoidance of Reactive Metabolite Leading to PCO371, a Potent, Selective, and Orally Available Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist.
Published in: J Med Chem

Ligand: [Phe23]PTH-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: PTH-(1-34) (rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Studies of the N-terminal region of a parathyroid hormone-related peptide (1-36) analog: receptor subtype-selective agonists, antagonists, and photochemical cross-linking agents.
Published in: Endocrinology

Ligand: PTHrP-(1-20)/TIP-(23-39) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Tuberoinfundibular peptide 39 binds to the parathyroid hormone (PTH)/PTH-related peptide receptor, but functions as an antagonist.
Published in: Endocrinology

Ligand: PTHrP-(1-21)/PTH-(22-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: PTHrP-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: PTHrP-(1-36) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: PTHrP-(7-34) (human, rat, mouse) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Tuberoinfundibular peptide (7-39) [TIP(7-39)], a novel, selective, high-affinity antagonist for the parathyroid hormone-1 receptor with no detectable agonist activity.
Published in: J Pharmacol Exp Ther

Ligand: [125I][Nle8,21,Tyr34]PTH-(1-34)-NH2 (rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKd
Reference (Journal): Residues in the membrane-spanning and extracellular loop regions of the parathyroid hormone (PTH)-2 receptor determine signaling selectivity for PTH and PTH-related peptide.
Published in: J Biol Chem

Ligand: teriparatide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1987), EMA (2003)
Median affinity:  pIC50
Reference (Journal): Parathyroid hormone (PTH)-PTH-related peptide hybrid peptides reveal functional interactions between the 1-14 and 15-34 domains of the ligand.
Published in: J Biol Chem

Ligand: teriparatide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1987), EMA (2003)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: TIP39 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular determinants of tuberoinfundibular peptide of 39 residues (TIP39) selectivity for the parathyroid hormone-2 (PTH2) receptor. N-terminal truncation of TIP39 reverses PTH2 receptor/PTH1 receptor binding selectivity.
Published in: J Biol Chem

Ligand: TIP39 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Tuberoinfundibular peptide 39 binds to the parathyroid hormone (PTH)/PTH-related peptide receptor, but functions as an antagonist.
Published in: Endocrinology

Ligand: TIP39-(3-39) (human/bovine) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Tuberoinfundibular peptide 39 binds to the parathyroid hormone (PTH)/PTH-related peptide receptor, but functions as an antagonist.
Published in: Endocrinology

Ligand: TIP39-(7-39) (human/bovine) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): Tuberoinfundibular peptide (7-39) [TIP(7-39)], a novel, selective, high-affinity antagonist for the parathyroid hormone-1 receptor with no detectable agonist activity.
Published in: J Pharmacol Exp Ther

Ligand: TIP39-(9-39) (human/bovine) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.4 pIC50
Reference (Journal): Tuberoinfundibular peptide 39 binds to the parathyroid hormone (PTH)/PTH-related peptide receptor, but functions as an antagonist.
Published in: Endocrinology

Ligand: [Trp23]PTHrP-(1-36) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): Converting parathyroid hormone-related peptide (PTHrP) into a potent PTH-2 receptor agonist.
Published in: J Biol Chem

Ligand: [Trp23,Tyr36]PTHrP-(1-36)-NH2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Residues in the membrane-spanning and extracellular loop regions of the parathyroid hormone (PTH)-2 receptor determine signaling selectivity for PTH and PTH-related peptide.
Published in: J Biol Chem

Ligand: [Tyr34]PTH-(1-34) (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Tuberoinfundibular peptide 39 binds to the parathyroid hormone (PTH)/PTH-related peptide receptor, but functions as an antagonist.
Published in: Endocrinology

Ligand: [Tyr34]PTH-(1-34)-NH2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.2 pIC50
Reference (Journal): Transmembrane residues of the parathyroid hormone (PTH)/PTH-related peptide receptor that specifically affect binding and signaling by agonist ligands.
Published in: J Biol Chem

Ligand: [Tyr34]PTH-(3-34)-NH2 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Journal): Transmembrane residues of the parathyroid hormone (PTH)/PTH-related peptide receptor that specifically affect binding and signaling by agonist ligands.
Published in: J Biol Chem

Ligand: [Tyr36]-PTHrP-(1-36) amide (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Tuberoinfundibular peptide 39 binds to the parathyroid hormone (PTH)/PTH-related peptide receptor, but functions as an antagonist.
Published in: Endocrinology