dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: NDR family (type: enzyme)
Target: Serine/threonine kinase 38

Ligand: compound 35 [PMID: 20684608] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
Published in: J Med Chem
Target family: NDR family (type: enzyme)
Target: Serine/threonine kinase 38 like

Ligand: compound 27 [PMID: 21123062] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Fused bicyclic derivatives of 2,4-diaminopyrimidine as c-Met inhibitors.
Published in: Bioorg Med Chem Lett
Target family: NDR family (type: enzyme)
Target: large tumor suppressor kinase 1

Ligand: midostaurin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2017)
Primary target: no
Median affinity: 5.960000038146973 pKd
Reference (Journal): AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Published in: Blood

Ligand: lestaurtinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pKd
Reference (Journal): AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Published in: Blood

Ligand: K-252a (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 pKd
Reference (Journal): The target landscape of clinical kinase drugs.
Published in: Science

Ligand: example 320 [WO2018198077A2] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Patent): 6-6 fused bicyclic heteroaryl compounds and their use as lats inhibitors

Ligand: defactinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.039999961853027 pKd
Reference (Journal): The target landscape of clinical kinase drugs.
Published in: Science

Ligand: BI-847325 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pKd
Reference (Journal): The target landscape of clinical kinase drugs.
Published in: Science

Ligand: AST-487 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.329999923706055 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: A-674563 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.960000038146973 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: TRULI (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Journal): Small-molecule inhibition of Lats kinases may promote Yap-dependent proliferation in postmitotic mammalian tissues.
Published in: Nat Commun
Target family: NDR family (type: enzyme)
Target: large tumor suppressor kinase 2

Ligand: A-674563 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.210000038146973 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: AST-487 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: compound 35 [PMID: 20684608] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Tetrahydroisoquinoline derivatives as highly selective and potent Rho kinase inhibitors.
Published in: J Med Chem

Ligand: GSK690693 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: midostaurin (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2017)
Primary target: no
Median affinity: 5.659999847412109 pKd
Reference (Journal): AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Published in: Blood
Target family: NDR family (type: enzyme)
Target: large tumor suppressor kinase 1

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.380000114440918 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: staurosporine (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.
Published in: Eur J Med Chem

Ligand: PF-3758309 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pKd
Reference (Journal): The target landscape of clinical kinase drugs.
Published in: Science

Ligand: nintedanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2014)
Primary target: no
Median affinity: 4.96999979019165 pKd
Reference (Journal): The target landscape of clinical kinase drugs.
Published in: Science
Target family: Neuropeptide FF/neuropeptide AF receptors (type: gpcr)
Target: NPFF2 receptor

Ligand: pancreatic polypeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification and characterization of two G protein-coupled receptors for neuropeptide FF.
Published in: J Biol Chem

Ligand: pancreatic polypeptide (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Agonist and antagonist activities on human NPFF(2) receptors of the NPY ligands GR231118 and BIBP3226.
Published in: Br J Pharmacol

Ligand: RF9 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): RF9, a potent and selective neuropeptide FF receptor antagonist, prevents opioid-induced tolerance associated with hyperalgesia.
Published in: Proc Natl Acad Sci USA

Ligand: RFRP-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Pharmacological characterization of human NPFF(1) and NPFF(2) receptors expressed in CHO cells by using NPY Y(1) receptor antagonists.
Published in: Eur J Pharmacol

Ligand: RFRP-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Quantitative autoradiographic distribution of NPFF1 neuropeptide FF receptor in the rat brain and comparison with NPFF2 receptor by using [125I]YVP and [(125I]EYF as selective radioligands.
Published in: Neuroscience

Ligand: [125I]EYF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.2 pKd
Reference (Journal): Pharmacological characterization of human NPFF(1) and NPFF(2) receptors expressed in CHO cells by using NPY Y(1) receptor antagonists.
Published in: Eur J Pharmacol

Ligand: [125I]NPFF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Functional differences between NPFF1 and NPFF2 receptor coupling: high intrinsic activities of RFamide-related peptides on stimulation of [35S]GTPgammaS binding.
Published in: Neuropharmacology

Ligand: [3H]EYF (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Characterization of two novel tritiated radioligands for labelling Neuropeptide FF (NPFF(1) and NPFF(2)) receptors.
Published in: Neurochem Int

Ligand: Y-RFRP-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Quantitative autoradiographic distribution of NPFF1 neuropeptide FF receptor in the rat brain and comparison with NPFF2 receptor by using [125I]YVP and [(125I]EYF as selective radioligands.
Published in: Neuroscience

Ligand: Y-RFRP-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8 pKi
Reference (Journal): Pharmacological characterization of human NPFF(1) and NPFF(2) receptors expressed in CHO cells by using NPY Y(1) receptor antagonists.
Published in: Eur J Pharmacol
Target family: Neuropeptide W/neuropeptide B receptors (type: gpcr)
Target: NPBW1 receptor

Ligand: des-Br-neuropeptide B-29 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7.
Published in: J Biol Chem

Ligand: des-Br-neuropeptide B-29 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: des-Br-neuropeptide B-23 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: des-Br-neuropeptide B-23 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pIC50
Reference (Journal): Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7.
Published in: J Biol Chem

Ligand: Ava5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Primary target: no
Median affinity:  pKi
Reference (Journal): Development of a potent and selective GPR7 (NPBW1) agonist: a systematic structure-activity study of neuropeptide B.
Published in: J Pept Sci

Ligand: Ava3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Primary target: no
Median affinity:  pKi
Reference (Journal): Development of a potent and selective GPR7 (NPBW1) agonist: a systematic structure-activity study of neuropeptide B.
Published in: J Pept Sci

Ligand: neuropeptide W-30 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.6 pIC50
Reference (Journal): Identification of neuropeptide W as the endogenous ligand for orphan G-protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: [125I]NPW-23 (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): Identification and cellular localisation of NPW1 (GPR7) receptors for the novel neuropeptide W-23 by [125I]-NPW radioligand binding and immunocytochemistry.
Published in: Brain Res

Ligand: [125I]NPW-23 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): Identification and cellular localisation of NPW1 (GPR7) receptors for the novel neuropeptide W-23 by [125I]-NPW radioligand binding and immunocytochemistry.
Published in: Brain Res

Ligand: [125I][Tyr11]des-Br-NPB-23 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.4 pKd
Reference (Journal): Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7.
Published in: J Biol Chem
Target family: Neuropeptide W/neuropeptide B receptors (type: gpcr)
Target: NPBW2 receptor

Ligand: neuropeptide B-23 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pIC50
Reference (Journal): Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: neuropeptide B-29 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: neuropeptide W-23 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.6 pIC50
Reference (Journal): Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: neuropeptide W-30 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.4 pIC50
Reference (Journal): Identification of natural ligands for the orphan G protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem

Ligand: [125I]NPW-23 (human) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.7 pKd
Reference (Journal): Identification of neuropeptide W as the endogenous ligand for orphan G-protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem
Target family: Neuropeptide W/neuropeptide B receptors (type: gpcr)
Target: NPBW1 receptor

Ligand: neuropeptide B-29 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pIC50
Reference (Journal): Identification of a neuropeptide modified with bromine as an endogenous ligand for GPR7.
Published in: J Biol Chem

Ligand: neuropeptide W-23 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pIC50
Reference (Journal): Identification of neuropeptide W as the endogenous ligand for orphan G-protein-coupled receptors GPR7 and GPR8.
Published in: J Biol Chem
Target family: Neuropeptide Y receptors (type: gpcr)
Target: Y<sub>1</sub> receptor

Ligand: BIBP3226 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The functional investigation of a human adenocarcinoma cell line, stably transfected with the neuropeptide Y Y1 receptor.
Published in: Br J Pharmacol

Ligand: BIBO3304 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pIC50
Reference (Journal): Subtype selectivity of the novel nonpeptide neuropeptide Y Y1 receptor antagonist BIBO 3304 and its effect on feeding in rodents.
Published in: Br J Pharmacol

Ligand: BIBO3304 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 pIC50
Reference (Journal): [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors.
Published in: Br J Pharmacol

Ligand: [Ala31,Aib32]NPY (pig) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pIC50
Reference (Journal): Ala31-Aib32: identification of the key motif for high affinity and selectivity of neuropeptide Y at the Y5-receptor.
Published in: Biochemistry

Ligand: peptide YY (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10.2 pKi
Reference (Journal): [125I]Leu31, Pro34-PYY is a high affinity radioligand for rat PP1/Y4 and Y1 receptors: evidence for heterogeneity in pancreatic polypeptide receptors.
Published in: Peptides
Target family: Neuropilins and Plexins (type: other_protein)
Target: neuropilin 1

Ligand: EG01377 (Synthetic organic)
Interaction type: None
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 5.880000114440918 pKd
Reference (Journal): Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells.
Published in: J Med Chem

Ligand: EG01377 (Synthetic organic)
Interaction type: None
Action: Competitive
Ligand approved: no
Primary target: yes
Median affinity: 6.21999979019165 pIC50
Reference (Journal): Small Molecule Neuropilin-1 Antagonists Combine Antiangiogenic and Antitumor Activity with Immune Modulation through Reduction of Transforming Growth Factor Beta (TGFβ) Production in Regulatory T-Cells.
Published in: J Med Chem

Ligand: EG00229 (Synthetic organic)
Interaction type: None
Action: Competitive
Ligand approved: no
Primary target: no
Median affinity: 5.050000190734863 pIC50
Reference (Journal): Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
Published in: J Med Chem
Target family: Neutral amino acid transporter subfamily (type: transporter)
Target: B<sup>0</sup>AT1

Ligand: cinromide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Identification and Characterization of Inhibitors of a Neutral Amino Acid Transporter, SLC6A19, Using Two Functional Cell-Based Assays.
Published in: SLAS Discov

Ligand: inhibitor CB3 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.309999942779541 pIC50
Reference (Journal): Novel Chemical Scaffolds to Inhibit the Neutral Amino Acid Transporter B<sup>0</sup>AT1 (SLC6A19), a Potential Target to Treat Metabolic Diseases.
Published in: Front Pharmacol

Ligand: inhibitor E18 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.46999979019165 pIC50
Reference (Journal): Novel Chemical Scaffolds to Inhibit the Neutral Amino Acid Transporter B<sup>0</sup>AT1 (SLC6A19), a Potential Target to Treat Metabolic Diseases.
Published in: Front Pharmacol

Ligand: inhibitor E4 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.110000133514404 pIC50
Reference (Journal): Novel Chemical Scaffolds to Inhibit the Neutral Amino Acid Transporter B<sup>0</sup>AT1 (SLC6A19), a Potential Target to Treat Metabolic Diseases.
Published in: Front Pharmacol

Ligand: nimesulide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Primary target: no
Median affinity: 4.639999866485596 pIC50
Reference (Journal): Nimesulide binding site in the B0AT1 (SLC6A19) amino acid transporter. Mechanism of inhibition revealed by proteoliposome transport assay and molecular modelling.
Published in: Biochem Pharmacol
Target family: Neutral amino acid transporter subfamily (type: transporter)
Target: B<sup>0</sup>AT2

Ligand: loratadine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 5.400000095367432 pIC50
Reference (Journal): Loratadine and analogues: discovery and preliminary structure-activity relationship of inhibitors of the amino acid transporter B(0)AT2.
Published in: J Med Chem
Target family: Neutral amino acid transporter subfamily (type: transporter)
Target: B<sup>0</sup>AT1

Ligand: benzatropine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1954)
Primary target: no
Median affinity: 4.360000133514404 pIC50
Reference (Journal): Identification of novel inhibitors of the amino acid transporter B<sup>0</sup> AT1 (SLC6A19), a potential target to induce protein restriction and to treat type 2 diabetes.
Published in: Br J Pharmacol
Target family: Neutral sphingomyelinase coupling factors (type: enzyme)
Target: embryonic ectoderm development

Ligand: A-395 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
Published in: Nat Chem Biol

Ligand: AZ14117230 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.270000457763672 pKd
Reference (Journal): EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex.
Published in: Cell Chem Biol

Ligand: MAK683 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Patent): Triazolopyrimidine compounds and uses thereof

Ligand: pociredir (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKd
Reference (Patent): MACROCYCLIC AZOLOPYRIDINE DERIVATIVES AS EED AND PRC2 MODULATORS
Target family: NF-kappa B TF proteins (type: other_protein)
Target: RELA proto-oncogene, NF-kB subunit

Ligand: compound 11 [PMID: 30694059] (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.050000190734863 pIC50
Reference (Journal): Amides and Flavonoids from the Fruit and Leaf Extracts of Melodorum siamensis.
Published in: J Nat Prod

Ligand: RelA inhibitor A55 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 5.539999961853027 pKd
Reference (Journal): Identification of a Selective RelA Inhibitor Based on DSE-FRET Screening Methods.
Published in: Int J Mol Sci
Target family: Nicotinic acetylcholine receptors  (nACh) (type: lgic)
Target: nicotinic acetylcholine receptor &alpha;7 subunit

Ligand: [3H]AZ11637326 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.640000343322754 pKd
Reference (Journal): In vitro binding characteristics of [3H]AZ11637326, a novel alpha7-selective neuronal nicotinic receptor agonist radioligand.
Published in: Eur J Pharmacol

Ligand: [3H]α-bungarotoxin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd

Ligand: [3H]A-585539 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.149999618530273 pKd
Reference (Journal): [3H]A-585539 [(1S,4S)-2,2-dimethyl-5-(6-phenylpyridazin-3-yl)-5-aza-2-azoniabicyclo[2.2.1]heptane], a novel high-affinity alpha7 neuronal nicotinic receptor agonist: radioligand binding characterization to rat and human brain.
Published in: J Pharmacol Exp Ther

Ligand: [125I]α-bungarotoxin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Target family: Nicotinic acetylcholine receptors  (nACh) (type: lgic)
Target: nicotinic acetylcholine receptor &alpha;3 subunit

Ligand: α-conotoxin AuIB (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: A-867744 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): In vitro pharmacological characterization of a novel allosteric modulator of alpha 7 neuronal acetylcholine receptor, 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744), exhibiting unique pharmacological profile.
Published in: J Pharmacol Exp Ther