dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: C14: Caspase (type: enzyme)
Target: Caspase 4

Ligand: casp 4 inhib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): Potent and selective nonpeptide inhibitors of caspases 3 and 7.
Published in: J Med Chem

Ligand: M826 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: VRT-043198 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): (S)-1-((S)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an orally available selective interleukin (IL)-converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18.
Published in: J Pharmacol Exp Ther
Target family: C14: Caspase (type: enzyme)
Target: Caspase 5

Ligand: M826 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pIC50
Reference (Journal): Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: uracil 20 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.53000020980835 pIC50
Reference (Journal): Rational Drug Design of Topically Administered Caspase 1 Inhibitors for the Treatment of Inflammatory Acne.
Published in: J Med Chem

Ligand: Z-WEHD-FMK (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Anticancer mechanisms of 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl) cytosine (ECyd, TAS-106).
Published in: Nucleic Acids Res Suppl
Target family: C14: Caspase (type: enzyme)
Target: Caspase 6

Ligand: Ac-VEID-CHO (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.
Published in: J Med Chem

Ligand: Z-VEID-FMK (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Caspase-6 gene disruption reveals a requirement for lamin A cleavage in apoptotic chromatin condensation.
Published in: EMBO J
Target family: C14: Caspase (type: enzyme)
Target: Caspase 7

Ligand: compound 4 [PMID: 12408711] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.889999866485596 pKi
Reference (Journal): Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.
Published in: J Med Chem

Ligand: isatin sulfonamide 34 [PMID: 11384246] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Potent and selective nonpeptide inhibitors of caspases 3 and 7.
Published in: J Med Chem

Ligand: M826 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Published in: Bioorg Med Chem Lett
Target family: C14: Caspase (type: enzyme)
Target: Caspase 8

Ligand: compound 4 [PMID: 12408711] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.059999942779541 pKi
Reference (Journal): Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.
Published in: J Med Chem

Ligand: emricasan (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.3 pKi
Reference (Journal): First-in-class pan caspase inhibitor developed for the treatment of liver disease.
Published in: J Med Chem

Ligand: Z-IETD-FMK (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Function of caspases in regulating apoptosis caused by erythropoietin deprivation in erythroid progenitors.
Published in: J Cell Physiol
Target family: C14: Caspase (type: enzyme)
Target: Caspase 9

Ligand: isatin sulfonamide 34 [PMID: 11384246] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pKi
Reference (Journal): Potent and selective nonpeptide inhibitors of caspases 3 and 7.
Published in: J Med Chem

Ligand: Z-LEHD-FMK (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  -
Reference (Journal): Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury.
Published in: Br J Pharmacol
Target family: C19: Ubiquitin-specific protease (type: enzyme)
Target: ubiquitin specific peptidase 1

Ligand: compound 61 [PMID: 36221183] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.860000133514404 pIC50
Reference (Journal): Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer.
Published in: J Med Chem

Ligand: KSQ-4279 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (usp1) inhibitors

Ligand: ML323 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.119999885559082 pIC50
Reference (Journal): Synthesis and Structure-Activity Relationship Studies of N-Benzyl-2-phenylpyrimidin-4-amine Derivatives as Potent USP1/UAF1 Deubiquitinase Inhibitors with Anticancer Activity against Nonsmall Cell Lung Cancer.
Published in: J Med Chem

Ligand: SJB2-043 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.260000228881836 pIC50
Reference (Journal): Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells.
Published in: Mol Cancer Ther

Ligand: TNG348 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Purine derivatives as anticancer agents
Target family: C19: Ubiquitin-specific protease (type: enzyme)
Target: ubiquitin specific peptidase 14

Ligand: IU1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.329999923706055 pIC50
Reference (Journal): Enhancement of proteasome activity by a small-molecule inhibitor of USP14.
Published in: Nature

Ligand: VLX1570 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): The proteasome deubiquitinase inhibitor VLX1570 shows selectivity for ubiquitin-specific protease-14 and induces apoptosis of multiple myeloma cells.
Published in: Sci Rep
Target family: C19: Ubiquitin-specific protease (type: enzyme)
Target: ubiquitin specific peptidase 2

Ligand: ML364 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.960000038146973 pIC50
Reference (Journal): USP2 inhibition prevents infection with ACE2-dependent coronaviruses in vitro and is protective against SARS-CoV-2 in mice.
Published in: Sci Transl Med

Ligand: ML364 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.28000020980835 pKd
Reference (Journal): USP2 inhibition prevents infection with ACE2-dependent coronaviruses in vitro and is protective against SARS-CoV-2 in mice.
Published in: Sci Transl Med

Ligand: MS102 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): USP2 inhibition prevents infection with ACE2-dependent coronaviruses in vitro and is protective against SARS-CoV-2 in mice.
Published in: Sci Transl Med
Target family: C19: Ubiquitin-specific protease (type: enzyme)
Target: ubiquitin specific peptidase 21

Ligand: BAY-805 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21.
Published in: J Med Chem
Target family: C19: Ubiquitin-specific protease (type: enzyme)
Target: ubiquitin specific peptidase 5

Ligand: vialinin A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): Vialinin A is a ubiquitin-specific peptidase inhibitor.
Published in: Bioorg Med Chem Lett
Target family: C19: Ubiquitin-specific protease (type: enzyme)
Target: ubiquitin specific peptidase 8

Ligand: compound 61 [PMID: 36221183] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.550000190734863 pIC50
Reference (Journal): Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer.
Published in: J Med Chem
Target family: C1: Papain (type: enzyme)
Target: cathepsin B

Ligand: K777 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pKi
Reference (Journal): A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells.
Published in: ACS Chem Biol

Ligand: LHVS (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.869999885559082 pIC50
Reference (Journal): Inhibition of the activation of multiple serine proteases with a cathepsin C inhibitor requires sustained exposure to prevent pro-enzyme processing.
Published in: J Biol Chem

Ligand: poststatin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Poststatin, a new inhibitor of prolyl endopeptidase. V. Endopeptidase inhibitory activity of poststatin analogues.
Published in: J Antibiot

Ligand: VBY-825 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.479999542236328 pKi
Reference (Journal): Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model.
Published in: Biochimie

Ligand: Z-Arg-Leu-Val-Agly-Ile-Val-OMe (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 10.1 pKi
Reference (Journal): Azapeptides structurally based upon inhibitory sites of cystatins as potent and selective inhibitors of cysteine proteases.
Published in: J Med Chem
Target family: C1: Papain (type: enzyme)
Target: cathepsin C

Ligand: brensocatib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.600000381469727 pKd
Reference (Journal): Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Published in: J Med Chem

Ligand: brensocatib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Published in: J Med Chem

Ligand: brensocatib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Published in: J Med Chem

Ligand: brensocatib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986).
Published in: J Med Chem

Ligand: compound 3d [PMID: 3941405] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.570000171661377 pKi
Reference (Journal): Carboxyl-modified amino acids and peptides as protease inhibitors.
Published in: J Med Chem

Ligand: IcatCXPZ-01 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Structure-based design and in vivo anti-arthritic activity evaluation of a potent dipeptidyl cyclopropyl nitrile inhibitor of cathepsin C.
Published in: Biochem Pharmacol
Target family: C1: Papain (type: enzyme)
Target: cathepsin F

Ligand: compound (R)-26 [PMID: 22686657] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pKi
Reference (Journal): Selective nitrile inhibitors to modulate the proteolytic synergism of cathepsins S and F.
Published in: J Med Chem

Ligand: VBY-825 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.329999923706055 pKi
Reference (Journal): Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model.
Published in: Biochimie
Target family: C1: Papain (type: enzyme)
Target: cathepsin H

Ligand: compound 1b [PMID: 16290936] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pKi
Reference (Journal): Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Published in: Bioorg Med Chem Lett

Ligand: compound 1e [PMID: 27285276] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.360000133514404 pIC50
Reference (Journal): 2,5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L.
Published in: Bioorg Chem
Target family: C1: Papain (type: enzyme)
Target: cathepsin V

Ligand: citibrasine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKi
Reference (Journal): Acridone alkaloids as potent inhibitors of cathepsin V.
Published in: Bioorg Med Chem

Ligand: Citrusinine II (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.380000114440918 pKi
Reference (Journal): Acridone alkaloids as potent inhibitors of cathepsin V.
Published in: Bioorg Med Chem

Ligand: petesicatib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): Cathepsin S inhibition combines control of systemic and peripheral pathomechanisms of autoimmune tissue injury.
Published in: Sci Rep

Ligand: VBY-825 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.600000381469727 pKi
Reference (Journal): Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model.
Published in: Biochimie
Target family: C1: Papain (type: enzyme)
Target: cathepsin Z

Ligand: odanacatib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Published in: Bioorg Med Chem Lett
Target family: C2: Calpain (type: enzyme)
Target: calpain 1

Ligand: calpeptin (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Subsite requirements for peptide aldehyde inhibitors of human calpain I
Published in: Bioorg Med Chem Lett

Ligand: compound 4b [PMID: 20690647] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.639999866485596 pKi
Reference (Journal): Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.
Published in: J Med Chem

Ligand: GC-376 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.
Published in: ACS Pharmacol Transl Sci

Ligand: mercaptoacrylate inhibitor of calpain 1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Potent inhibition of Ca<sup>2+</sup>-dependent activation of calpain-1 by novel mercaptoacrylates.
Published in: Medchemcomm

Ligand: UAWJ9-36-3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.699999809265137 pIC50
Reference (Journal): Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir.
Published in: ACS Pharmacol Transl Sci
Target family: C2: Calpain (type: enzyme)
Target: calpain 2

Ligand: compound 19 [PMID: 8831774] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.
Published in: J Med Chem

Ligand: compound 5a [PMID: 20690647] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 pKi
Reference (Journal): Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors.
Published in: J Med Chem
Target family: C48: Ulp1 endopeptidase (type: enzyme)
Target: SUMO peptidase family member, NEDD8 specific

Ligand: ST074946 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 7.8 pIC50
Reference (Webpage): Dose-response confirmation of uHTS inhibitor hits of Sentrin-Specific Protease 8 using a kinetic assay with Nedd8 Protein Substrate - BioAssay Summary.
Target family: C48: Ulp1 endopeptidase (type: enzyme)
Target: SUMO specific peptidase 1

Ligand: compound 8e [PMID: 23044371] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.730000019073486 pIC50
Reference (Journal): 2-(4-Chlorophenyl)-2-oxoethyl 4-benzamidobenzoate derivatives, a novel class of SENP1 inhibitors: Virtual screening, synthesis and biological evaluation.
Published in: Bioorg Med Chem Lett
Target family: C65: Otubains (type: enzyme)
Target: OTU deubiquitinase, ubiquitin aldehyde binding 1

Ligand: compound 61 [PMID: 36221183] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.770000457763672 pIC50
Reference (Journal): Discovery of Potent OTUB1/USP8 Dual Inhibitors Targeting Proteostasis in Non-Small-Cell Lung Cancer.
Published in: J Med Chem
Target family: Calcitonin receptors (type: gpcr)
Target: AMY<sub>3</sub> receptor

Ligand: calcitonin (salmon) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1978)
Primary target: no
Median affinity:  -
Target family: Calcitonin receptors (type: gpcr)
Target: AM<sub>2</sub> receptor

Ligand: AM-(20-50) (rat) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function.
Published in: Mol Cell Endocrinol

Ligand: AM-(20-50) (rat) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Three receptor-activity-modifying proteins define calcitonin gene-related peptide or adrenomedullin selectivity of the mouse calcitonin-like receptor in COS-7 cells.
Published in: Biochem Pharmacol

Ligand: AM-(22-52) (human) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: AM-(22-52) (human) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: AM-(22-52) (human) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The amino terminus of receptor activity modifying proteins is a critical determinant of glycosylation state and ligand binding of calcitonin receptor-like receptor.
Published in: Mol Pharmacol

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): The amino terminus of receptor activity modifying proteins is a critical determinant of glycosylation state and ligand binding of calcitonin receptor-like receptor.
Published in: Mol Pharmacol

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Receptor activity modifying proteins interaction with human and porcine calcitonin receptor-like receptor (CRLR) in HEK-293 cells.
Published in: Mol Cell Biochem

Ligand: β-CGRP (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.7 pIC50
Reference (Journal): Mouse receptor-activity-modifying proteins 1, -2 and -3: amino acid sequence, expression and function.
Published in: Mol Cell Endocrinol

Ligand: compound 8 [Avgoustou et al., 2020] (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.210000038146973 pIC50
Reference (Journal): Discovery of a First-in-Class Potent Small Molecule Antagonist against the Adrenomedullin-2 Receptor
Published in: ACS Pharmacol Transl Sci

Ligand: [125I]AM (rat) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd