Target family: Bradykinin receptors (type: gpcr)
Target: B<sub>2</sub> receptor

Ligand: anatibant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Pharmacological profile of LF 16-0687, a new potent non-peptide bradykinin B2 receptor antagonist.
Published in: Immunopharmacology

Ligand: anatibant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Pharmacological profile of LF 16-0687, a new potent non-peptide bradykinin B2 receptor antagonist.
Published in: Immunopharmacology

Ligand: B-9430 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): A new generation of bradykinin antagonists.
Published in: Immunopharmacology

Ligand: B-9430 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pA2
Reference (Journal): Bradykinin receptors and their antagonists.
Published in: Eur J Pharmacol

Ligand: B-9430 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Partial agonists and full antagonists at the human and murine bradykinin B1 receptors.
Published in: Can J Physiol Pharmacol

Ligand: B-9430 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Partial agonists and full antagonists at the human and murine bradykinin B1 receptors.
Published in: Can J Physiol Pharmacol

Ligand: bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: bradyzide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
Published in: Br J Pharmacol

Ligand: bradyzide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
Published in: Br J Pharmacol

Ligand: compound 3 [PMID: 32636746] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): <i>In Vitro</i> Pharmacological Profile of a New Small Molecule Bradykinin B<sub>2</sub> Receptor Antagonist.
Published in: Front Pharmacol

Ligand: [des-Arg10]kallidin (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 4.6 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: [des-Arg9]bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.2 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: [des-Arg9]bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.1 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: deucrictibant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.329999923706055 pKi
Reference (Journal): <i>In Vitro</i> Pharmacological Profile of a New Small Molecule Bradykinin B<sub>2</sub> Receptor Antagonist.
Published in: Front Pharmacol

Ligand: deucrictibant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.329999923706055 pKi
Reference (Journal): In vitro pharmacological profile of PHA-022121, a small molecule bradykinin B<sub>2</sub> receptor antagonist in clinical development.
Published in: Int Immunopharmacol

Ligand: FR167344 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.2 pIC50
Reference (Journal): Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657.
Published in: Mol Pharmacol

Ligand: FR173657 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657.
Published in: Mol Pharmacol

Ligand: FR173657 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pA2
Reference (Journal): FR 173657: a new, potent, nonpeptide kinin B2 receptor antagonist. An in vitro study.
Published in: Hypertension

Ligand: FR190997 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Nonpeptide mimic of bradykinin with long-acting properties at the bradykinin B2 receptor.
Published in: Mol Pharmacol

Ligand: FR191413 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.2 pIC50
Reference (Journal): Discovery of the first non-peptide full agonists for the human bradykinin B(2) receptor incorporating 4-(2-picolyloxy)quinoline and 1-(2-picolyl)benzimidazole frameworks.
Published in: J Med Chem

Ligand: [Hyp3,Tyr(Me)8]BK (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Primary target: yes
Median affinity: 10.1899995803833 pKi
Reference (Journal): Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
Published in: J Med Chem

Ligand: icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Primary target: yes
Median affinity: 8.399999618530273 pA2
Reference (Journal): Receptors for kinins in the human isolated umbilical vein.
Published in: Br J Pharmacol

Ligand: icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Novel subtype-selective nonpeptide bradykinin receptor antagonists FR167344 and FR173657.
Published in: Mol Pharmacol

Ligand: icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Median affinity: 9.6 pKi
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: EMA (2008), FDA (2011)
Median affinity:  pKi
Reference (Journal): Bradyzide, a potent non-peptide B(2) bradykinin receptor antagonist with long-lasting oral activity in animal models of inflammatory hyperalgesia.
Published in: Br J Pharmacol

Ligand: JMV1116 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
Published in: J Med Chem

Ligand: JMV1116 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
Published in: J Med Chem

Ligand: JMV1431 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 pKi
Reference (Journal): Synthesis and biological evaluation of bradykinin B(1)/B(2) and selective B(1) receptor antagonists.
Published in: J Med Chem

Ligand: kallidin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: kallidin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: labradimil (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Further pharmacological evaluation of a novel synthetic peptide bradykinin B2 receptor agonist.
Published in: Biol Chem

Ligand: labradimil (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The bradykinin analog RMP-7 increases intracellular free calcium levels in rat brain microvascular endothelial cells.
Published in: J Pharmacol Exp Ther

Ligand: labradimil (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
Published in: J Med Chem

Ligand: Met-Lys-bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: Met-Lys-bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: NG291 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Structure-activity relationships of novel peptide agonists of the human bradykinin B2 receptor.
Published in: Peptides

Ligand: NPC 17731 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): The sixth transmembrane domains of the human B1 and B2 bradykinin receptors are structurally compatible and involved in discriminating between subtype-selective agonists.
Published in: J Biol Chem

Ligand: NPC 18565 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pKi
Reference (Journal): The sixth transmembrane domains of the human B1 and B2 bradykinin receptors are structurally compatible and involved in discriminating between subtype-selective agonists.
Published in: J Biol Chem

Ligand: NPC-349 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: NPC-349 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: NPC-567 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pA2
Reference (Journal): Bradykinin receptors and their antagonists.
Published in: Eur J Pharmacol

Ligand: NPC-567 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: NPC-567 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: [Phe8,ψ(CH2-NH)Arg9]BK (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [125I]HPP-HOE140 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Autoradiographic analysis of mouse brain kinin B1 and B2 receptors after closed head trauma and ability of Anatibant mesylate to cross the blood-brain barrier.
Published in: J Neurotrauma

Ligand: [125I]HPP-HOE140 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Autoradiographic detection of kinin receptors in the human medulla of control, hypertensive, and diabetic donors.
Published in: Can J Physiol Pharmacol

Ligand: [125I]-HPP-icatibant (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.520000457763672 pKd
Reference (Journal): Pharmacologic and autoradiographic evidence for an up-regulation of kinin B(2) receptors in the spinal cord of spontaneously hypertensive rats.
Published in: Br J Pharmacol

Ligand: [125I][Tyr8]bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Quantitative autoradiographic localization of [125I-Tyr8]bradykinin receptor binding sites in the rat spinal cord: effects of neonatal capsaicin, noradrenergic deafferentation, dorsal rhizotomy and peripheral axotomy.
Published in: Neuroscience

Ligand: [3H]BK (human, mouse, rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): [3H]bradykinin receptor-binding, receptor-recycling, and receptor-internalization of the B2 bradykinin receptor in the murine osteoblast-like cell line MC3T3-E1.
Published in: J Bone Miner Res

Ligand: [3H]NPC17731 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Functional studies of bradykinin receptors in Chinese hamster ovary cells stably expressing the human B2 bradykinin receptor.
Published in: Int Immunopharmacol

Ligand: [3H]NPC17731 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Characterization of bradykinin receptors in human lung fibroblasts using the binding of 3[H][Des-Arg10,Leu9]kallidin and [3H]NPC17731.
Published in: Life Sci

Ligand: [Thi5,8,D-Phe7]bradykinin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: [Thi5,8,D-Phe7]bradykinin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: [Tyr8]bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: [Tyr8]bradykinin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Differential pharmacology of cloned human and mouse B2 bradykinin receptors.
Published in: Mol Pharmacol

Ligand: WIN 64338 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor.
Published in: J Med Chem

Ligand: WIN 64338 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): The nonpeptide WIN 64338 is a bradykinin B2 receptor antagonist.
Published in: Proc Natl Acad Sci USA