dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Acetylcholine turnover (type: enzyme)
Target: butyrylcholinesterase

Ligand: bambuterol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Median affinity: 8.5 pIC50
Reference (Journal): Cholinesterases: new roles in brain function and in Alzheimer's disease.
Published in: Neurochem Res

Ligand: physostigmine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Median affinity:  pIC50
Reference (Journal): Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Published in: J Med Chem

Ligand: pyridostigmine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1955)
Primary target: no
Median affinity: 6.050000190734863 pIC50
Reference (Journal): Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
Published in: Bioorg Med Chem

Ligand: rivastigmine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2000), EMA (1998)
Primary target: yes
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Inhibition of human acetyl- and butyrylcholinesterase by novel carbamates of (-)- and (+)-tetrahydrofurobenzofuran and methanobenzodioxepine.
Published in: J Med Chem

Ligand: tacrine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity: 7.199999809265137 pKi
Reference (Journal): Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
Published in: J Med Chem
Target family: Acetylcholine turnover (type: enzyme)
Target: choline O-acetyltransferase

Ligand: naphthylvinylmethylpyridine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.46999979019165 pIC50
Reference (Journal): Approaches to protection against nerve agent poisoning. (Naphthylvinyl)pyridine derivatives as potential antidotes.
Published in: J Med Chem
Target family: Acid-sensing (proton-gated) ion channels (ASICs) (type: lgic)
Target: ASIC1

Ligand: psalmotoxin 1 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Isolation of a tarantula toxin specific for a class of proton-gated Na+ channels.
Published in: J Biol Chem
Target family: Acid-sensing (proton-gated) ion channels (ASICs) (type: lgic)
Target: ASIC2

Ligand: nafamostat (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: Japan only
Primary target: no
Median affinity: 4.199999809265137 pIC50
Reference (Journal): Nafamostat mesilate reversibly blocks acid-sensing ion channel currents.
Published in: Biochem Biophys Res Commun

Ligand: H+ (Inorganic)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  pEC50

Ligand: diminazene (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 6.099999904632568 pIC50
Reference (Journal): Inhibition of acid-sensing ion channels by diminazene and APETx2 evoke partial and highly variable antihyperalgesia in a rat model of inflammatory pain.
Published in: Br J Pharmacol

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Primary target: no
Median affinity: 3 pIC50
Reference (Journal): Subunit-dependent cadmium and nickel inhibition of acid-sensing ion channels.
Published in: Dev Neurobiol

Ligand: amiloride (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 4.599999904632568 pIC50
Reference (Journal): The mammalian degenerin MDEG, an amiloride-sensitive cation channel activated by mutations causing neurodegeneration in Caenorhabditis elegans.
Published in: J Biol Chem

Ligand: A-317567 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity: 4.5 pIC50
Reference (Journal): Electrophysiological and in vivo characterization of A-317567, a novel blocker of acid sensing ion channels.
Published in: Pain
Target family: Ack family (type: enzyme)
Target: tyrosine kinase non receptor 1

Ligand: XMD8-92 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.050000190734863 pKd
Reference (Journal): Pharmacological inhibition of BMK1 suppresses tumor growth through promyelocytic leukemia protein.
Published in: Cancer Cell

Ligand: xiliertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.590000152587891 pIC50
Reference (Journal): Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification.
Published in: Oncotarget
Target family: Ack family (type: enzyme)
Target: tyrosine kinase non receptor 2

Ligand: bosutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 8.569999694824219 pIC50
Reference (Journal): Global target profile of the kinase inhibitor bosutinib in primary chronic myeloid leukemia cells.
Published in: Leukemia

Ligand: compound 30 [PMID: 17280833] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Discovery of 4-amino-5,6-biaryl-furo[2,3-d]pyrimidines as inhibitors of Lck: development of an expedient and divergent synthetic route and preliminary SAR.
Published in: Bioorg Med Chem Lett

Ligand: NIK inhibitor 12f (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): Identification of <i>N</i>-Phenyl-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-amine Derivatives as Novel, Potent, and Selective NF-κB Inducing Kinase (NIK) Inhibitors for the Treatment of Psoriasis.
Published in: J Med Chem
Target family: Acylated lysine reader proteins (type: other_protein)
Target: MLLT1 super elongation complex subunit

Ligand: SR-0813 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pKd
Reference (Journal): Chemical Inhibition of ENL/AF9 YEATS Domains in Acute Leukemia
Published in: ACS Central Science
Target family: Acyl-CoA synthetases (type: enzyme)
Target: acyl-CoA synthetase short chain family member 2

Ligand: example 265 [WO2019097515A1] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Patent): Acss2 inhibitors and methods of use thereof

Ligand: ADG-207 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Compositions and methods for inhibiting acss2
Target family: Adenosine receptors (type: gpcr)
Target: A<sub>2A</sub> receptor

Ligand: CV-1808 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol
Target family: Adenosine receptors (type: gpcr)
Target: A<sub>2A</sub> receptor

Ligand: ZM-241385 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Published in: Br J Pharmacol

Ligand: xanthine amine congener (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: VUF5574 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Published in: J Med Chem

Ligand: visnagin (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.4 pKi
Reference (Journal): Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
Published in: J Med Chem

Ligand: vipadenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.89 pKi
Reference (Journal): Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
Published in: J Med Chem

Ligand: UK-432,097 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure of an agonist-bound human A2A adenosine receptor.
Published in: Science

Ligand: UK-432,097 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional efficacy of adenosine A₂A receptor agonists is positively correlated to their receptor residence time.
Published in: Br J Pharmacol

Ligand: tozadenant (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pKi
Reference (Journal): Adenosine A2A receptor as a drug discovery target.
Published in: J Med Chem
Target family: Adenosine turnover (type: enzyme)
Target: Ecto-5'-Nucleotidase

Ligand: mupadolimab (Antibody)
Interaction type: Antibody
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.149999618530273 pKd
Reference (Patent): Humanized anti-cd73 antibodies

Ligand: dalutrafusp alfa (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 10.15999984741211 pKd
Reference (Patent): Anti-cd73 antibodies and methods of use thereof

Ligand: compound 49 [PMID: 36529947] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.770000457763672 pIC50
Reference (Journal): Discovery of a Series of Potent, Selective, and Orally Bioavailable Nucleoside Inhibitors of CD73 That Demonstrates <i>In Vivo</i> Antitumor Activity.
Published in: J Med Chem

Ligand: compound 15 [PMID: 32045236] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.4399995803833 pKi
Reference (Journal): 2-Substituted α,β-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.
Published in: J Med Chem

Ligand: compound 15 [PMID: 32045236] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pKi
Reference (Journal): 2-Substituted α,β-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.
Published in: J Med Chem

Ligand: compound 15 [PMID: 32045236] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 pKi
Reference (Journal): 2-Substituted α,β-Methylene-ADP Derivatives: Potent Competitive Ecto-5'-nucleotidase (CD73) Inhibitors with Variable Binding Modes.
Published in: J Med Chem

Ligand: αβ-methyleneADP (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): 5'-Nucleotidase from smooth muscle of small intestine and from brain. Inhibition of nucleotides.
Published in: Biochemistry
Target family: Adenosine turnover (type: enzyme)
Target: Adenosine kinase

Ligand: ABT702 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): ABT-702 (4-amino-5-(3-bromophenyl)-7-(6-morpholinopyridin-3-yl)pyrido[2, 3-d]pyrimidine), a novel orally effective adenosine kinase inhibitor with analgesic and anti-inflammatory properties: I. In vitro characterization and acute antinociceptive effects in the mouse.
Published in: J Pharmacol Exp Ther

Ligand: A134974 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 10.2 pIC50
Reference (Journal): Effects of A-134974, a novel adenosine kinase inhibitor, on carrageenan-induced inflammatory hyperalgesia and locomotor activity in rats: evaluation of the sites of action.
Published in: J Pharmacol Exp Ther
Target family: Adenosine turnover (type: enzyme)
Target: Adenosine deaminase

Ligand: pentostatin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 10.800000190734863 pIC50
Reference (Journal): Tight-binding inhibitors--IV. Inhibition of adenosine deaminases by various inhibitors.
Published in: Biochem Pharmacol

Ligand: EHNA (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Tight-binding inhibitors--IV. Inhibition of adenosine deaminases by various inhibitors.
Published in: Biochem Pharmacol
Target family: Adenosine turnover (type: enzyme)
Target: S-Adenosylhomocysteine hydrolase

Ligand: DZNep (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 12.300000190734863 pKi
Reference (Journal): 3-Deazaneplanocin: a new and potent inhibitor of S-adenosylhomocysteine hydrolase and its effects on human promyelocytic leukemia cell line HL-60.
Published in: Biochem Biophys Res Commun

Ligand: 3-deazaadenosine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Adenosine analogues as substrates and inhibitors of S-adenosylhomocysteine hydrolase.
Published in: Biochemistry
Target family: Adenosine turnover (type: enzyme)
Target: Ecto-5'-Nucleotidase

Ligand: quemliclustat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 11.300000190734863 pKi
Reference (Journal): An Exceptionally Potent Inhibitor of Human CD73.
Published in: Biochemistry

Ligand: PSB-0963 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pKi
Reference (Journal): Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.
Published in: J Med Chem

Ligand: ORIC-533 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Patent): Cd73 inhibitors

Ligand: oleclumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 11.380000114440918 pKd
Reference (Journal): Inhibition of CD73 AMP hydrolysis by a therapeutic antibody with a dual, non-competitive mechanism of action.
Published in: MAbs
Target family: Adenylyl cyclases (ACs) (type: enzyme)
Target: adenylyl cyclase 6

Ligand: NKY80 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pIC50
Reference (Journal): Isoform selectivity of adenylyl cyclase inhibitors: characterization of known and novel compounds.
Published in: J Pharmacol Exp Ther
Target family: Adenylyl cyclases (ACs) (type: enzyme)
Target: adenylyl cyclase 5

Ligand: NKY80 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.150000095367432 pIC50
Reference (Journal): Type-specific regulation of adenylyl cyclase. Selective pharmacological stimulation and inhibition of adenylyl cyclase isoforms.
Published in: J Biol Chem

Ligand: FD6 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Type-specific regulation of adenylyl cyclase. Selective pharmacological stimulation and inhibition of adenylyl cyclase isoforms.
Published in: J Biol Chem
Target family: Adenylyl cyclases (ACs) (type: enzyme)
Target: adenylyl cyclase 2

Ligand: SKF-83566 (Synthetic organic)
Interaction type: Inhibitor
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Development of a high-throughput screening paradigm for the discovery of small-molecule modulators of adenylyl cyclase: identification of an adenylyl cyclase 2 inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: FD1 (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Type-specific regulation of adenylyl cyclase. Selective pharmacological stimulation and inhibition of adenylyl cyclase isoforms.
Published in: J Biol Chem
Target family: Adenylyl cyclases (ACs) (type: enzyme)
Target: adenylyl cyclase 10

Ligand: TDI-11861 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.260000228881836 pIC50
Reference (Journal): Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
Published in: J Med Chem

Ligand: TDI-11861 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pKd
Reference (Journal): Design, Synthesis, and Pharmacological Evaluation of Second-Generation Soluble Adenylyl Cyclase (sAC, ADCY10) Inhibitors with Slow Dissociation Rates.
Published in: J Med Chem

Ligand: LRE1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Discovery of LRE1 as a specific and allosteric inhibitor of soluble adenylyl cyclase.
Published in: Nat Chem Biol

Ligand: KH7 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The &quot;soluble&quot; adenylyl cyclase in sperm mediates multiple signaling events required for fertilization.
Published in: Dev Cell
Target family: Adenylyl cyclases (ACs) (type: enzyme)
Target: adenylyl cyclase 1

Ligand: ST034307 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.639999866485596 pIC50
Reference (Journal): Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties.
Published in: Sci Signal

Ligand: compound 45 [PMID: 8709105] (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 7.679999828338623 pIC50
Reference (Journal): Forskolin carbamates: binding and activation studies with type I adenylyl cyclase.
Published in: J Med Chem
Target family: Adenylyl cyclases (ACs) (type: enzyme)
Target: adenylyl cyclase 5

Ligand: NKY80 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 5.150000095367432 pIC50
Reference (Journal): Isoform selectivity of adenylyl cyclase inhibitors: characterization of known and novel compounds.
Published in: J Pharmacol Exp Ther
Target family: Adhesion Class GPCRs (type: gpcr)
Target: ADGRL3

Ligand: FLRT3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKd
Reference (Journal): FLRT proteins are endogenous latrophilin ligands and regulate excitatory synapse development.
Published in: Neuron
Target family: Adhesion Class GPCRs (type: gpcr)
Target: ADGRB1

Ligand: phosphatidylserine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): BAI1 is an engulfment receptor for apoptotic cells upstream of the ELMO/Dock180/Rac module.
Published in: Nature
Target family: Adhesion Class GPCRs (type: gpcr)
Target: ADGRG3

Ligand: beclometasone dipropionate (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: EMA (2017)
Median affinity: 8.5 pEC50
Reference (Journal): Signaling property study of adhesion G-protein-coupled receptors.
Published in: FEBS Lett
Target family: Adhesion Class GPCRs (type: gpcr)
Target: ADGRL1

Ligand: α-latrotoxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Mutant alpha-latrotoxin (LTXN4C) does not form pores and causes secretion by receptor stimulation: this action does not require neurexins.
Published in: J Biol Chem

Ligand: α-latrotoxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): alpha-Latrotoxin stimulates exocytosis by the interaction with a neuronal G-protein-coupled receptor.
Published in: Neuron

Ligand: lasso D (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.8 pKd
Reference (Journal): Latrophilin 1 and its endogenous ligand Lasso/teneurin-2 form a high-affinity transsynaptic receptor pair with signaling capabilities.
Published in: Proc Natl Acad Sci USA

Ligand: LTX(N4C) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.6 pKd
Reference (Journal): Mutant alpha-latrotoxin (LTXN4C) does not form pores and causes secretion by receptor stimulation: this action does not require neurexins.
Published in: J Biol Chem
Target family: Adhesion Class GPCRs (type: gpcr)
Target: ADGRL2

Ligand: α-latrotoxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.85 pKd
Reference (Journal): A novel ubiquitously expressed alpha-latrotoxin receptor is a member of the CIRL family of G-protein-coupled receptors.
Published in: J Biol Chem
Target family: Adrenoceptors (type: gpcr)
Target: &beta;<sub>2</sub>-adrenoceptor

Ligand: butoxamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol
Target family: Akt (Protein kinase B, PKB) family (type: enzyme)
Target: AKT serine/threonine kinase 2

Ligand: capivasertib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2023)
Primary target: yes
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Discovery of 4-Amino-N-[(1S)-1-(4-chlorophenyl)-3-hydroxypropyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide (AZD5363), an Orally Bioavailable, Potent Inhibitor of Akt Kinases.
Published in: J Med Chem