dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: Class A Orphans (type: gpcr)
Target: <i>MRGPRX1</i>

Ligand: GPR15L (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.739999771118164 pEC50
Reference (Journal): GPR15L is an epithelial inflammation-derived pruritogen.
Published in: Sci Adv

Ligand: compound 16 [PMID: 31498617] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Discovery of Benzamidine- and 1-Aminoisoquinoline-Based Human MAS-Related G-Protein-Coupled Receptor X1 (MRGPRX1) Agonists.
Published in: J Med Chem

Ligand: chloroquine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1949), UK (2000)
Median affinity: 3.53 pEC50
Reference (Journal): Sensory neuron-specific GPCR Mrgprs are itch receptors mediating chloroquine-induced pruritus.
Published in: Cell

Ligand: bovine adrenal medulla peptide 8-22 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Modulation of ion channels and synaptic transmission by a human sensory neuron-specific G-protein-coupled receptor, SNSR4/mrgX1, heterologously expressed in cultured rat neurons.
Published in: J Neurosci

Ligand: bovine adrenal medulla peptide 8-22 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: bovine adrenal medulla peptide 8-22 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs.
Published in: Nat Neurosci

Ligand: bovine adrenal medulla peptide 8-22 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.68 pKi
Reference (Journal): Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs.
Published in: Nat Neurosci

Ligand: bovine adrenal medulla peptide 8-22 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.99 pKd
Reference (Journal): Proenkephalin A gene products activate a new family of sensory neuron--specific GPCRs.
Published in: Nat Neurosci
Target family: Class A Orphans (type: gpcr)
Target: <i>MRGPRD</i>

Ligand: β-alanine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Median affinity: 4.8 pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: β-alanine (Metabolite)
Interaction type: Agonist
Action: Agonist
Median affinity: 4.36 pEC50
Reference (Journal): Identification of a G protein-coupled receptor specifically responsive to beta-alanine.
Published in: J Biol Chem

Ligand: β-alanine (Metabolite)
Interaction type: Agonist
Action: Agonist
Median affinity: 4.85 pEC50
Reference (Journal): Identification of a G protein-coupled receptor specifically responsive to beta-alanine.
Published in: J Biol Chem

Ligand: β-alanine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Median affinity: 4.8 pEC50
Reference (Journal): Identification of a G protein-coupled receptor specifically responsive to beta-alanine.
Published in: J Biol Chem
Target family: Class A Orphans (type: gpcr)
Target: <i>LGR5</i>

Ligand: R-spondin-4 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pEC50
Reference (Journal): R-spondins function as ligands of the orphan receptors LGR4 and LGR5 to regulate Wnt/beta-catenin signaling.
Published in: Proc Natl Acad Sci USA

Ligand: R-spondin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11 pEC50
Reference (Journal): R-spondins function as ligands of the orphan receptors LGR4 and LGR5 to regulate Wnt/beta-catenin signaling.
Published in: Proc Natl Acad Sci USA

Ligand: R-spondin-2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 12 pEC50
Reference (Journal): R-spondins function as ligands of the orphan receptors LGR4 and LGR5 to regulate Wnt/beta-catenin signaling.
Published in: Proc Natl Acad Sci USA

Ligand: R-spondin-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 11.100000381469727 pEC50
Reference (Journal): R-spondins function as ligands of the orphan receptors LGR4 and LGR5 to regulate Wnt/beta-catenin signaling.
Published in: Proc Natl Acad Sci USA
Target family: Class C Orphans (type: gpcr)
Target: GPRC6 receptor

Ligand: glycine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.6 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: calindol (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor.
Published in: Cell Calcium
Target family: Class C Orphans (type: gpcr)
Target: <i>GPRC5D</i>

Ligand: talquetamab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA & EMA  (2023)
Primary target: no
Median affinity:  -
Reference (Journal): A T-cell-redirecting bispecific G-protein-coupled receptor class 5 member D x CD3 antibody to treat multiple myeloma.
Published in: Blood

Ligand: talquetamab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA & EMA  (2023)
Primary target: no
Median affinity:  -
Reference (Patent): Anti-GPRC5D antibodies, bispecific antigen binding molecules that bind GPRC5D and CD3, and uses thereof
Target family: Class C Orphans (type: gpcr)
Target: GPRC6 receptor

Ligand: NPS 2143 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): Molecular determinants of non-competitive antagonist binding to the mouse GPRC6A receptor.
Published in: Cell Calcium

Ligand: L-serine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.2 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: L-ornithine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: L-lysine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.8 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: L-glutamine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.2 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: L-citrulline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.6 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: L-arginine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.4 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol

Ligand: L-alanine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 3.8 pEC50
Reference (Journal): Deorphanization of GPRC6A: a promiscuous L-alpha-amino acid receptor with preference for basic amino acids.
Published in: Mol Pharmacol
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>7</sub>

Ligand: F7H (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pIC50
Reference (Journal): Structure-Based Ligand Discovery Targeting the Transmembrane Domain of Frizzled Receptor FZD7.
Published in: J Med Chem
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>6</sub>

Ligand: Wnt-5a (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Mutations in frizzled 6 cause isolated autosomal-recessive nail dysplasia.
Published in: Am J Hum Genet

Ligand: Wnt-4 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Wnt-4 activates the canonical beta-catenin-mediated Wnt pathway and binds Frizzled-6 CRD: functional implications of Wnt/beta-catenin activity in kidney epithelial cells.
Published in: Exp Cell Res

Ligand: Wnt-4 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Wnt4 enhances murine hematopoietic progenitor cell expansion through a planar cell polarity-like pathway.
Published in: PLoS ONE

Ligand: Wnt-3a (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Wnt3a stimulation elicits G-protein-coupled receptor properties of mammalian Frizzled proteins.
Published in: Biochem J

Ligand: Wnt-3a (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Mutations in frizzled 6 cause isolated autosomal-recessive nail dysplasia.
Published in: Am J Hum Genet

Ligand: SAG1.3 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pKd
Reference (Journal): Structural insight into small molecule action on Frizzleds.
Published in: Nat Commun
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>5</sub>

Ligand: vantictumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Journal): Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors.
Published in: Proc Natl Acad Sci USA
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>4</sub>

Ligand: norrin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.4 pKd
Reference (Journal): Vascular development in the retina and inner ear: control by Norrin and Frizzled-4, a high-affinity ligand-receptor pair.
Published in: Cell

Ligand: FzM1.8 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist.
Published in: Biochemistry

Ligand: FzM1.8 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Pharmacological folding chaperones act as allosteric ligands of Frizzled4.
Published in: Nat Chem Biol

Ligand: FzM1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Pharmacological folding chaperones act as allosteric ligands of Frizzled4.
Published in: Nat Chem Biol

Ligand: FzM1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pIC50
Reference (Journal): A Negative Allosteric Modulator of WNT Receptor Frizzled 4 Switches into an Allosteric Agonist.
Published in: Biochemistry
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>2</sub>

Ligand: vantictumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Journal): Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors.
Published in: Proc Natl Acad Sci USA
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>1</sub>

Ligand: vantictumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Journal): Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors.
Published in: Proc Natl Acad Sci USA
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>8</sub>

Ligand: vantictumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors.
Published in: Proc Natl Acad Sci USA

Ligand: carbamazepine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Approval source: FDA (1968)
Primary target: no
Median affinity: 4.769999980926514 pKd
Reference (Journal): Antiepileptic Drug Carbamazepine Binds to a Novel Pocket on the Wnt Receptor Frizzled-8.
Published in: J Med Chem
Target family: Class Frizzled GPCRs (type: gpcr)
Target: FZD<sub>7</sub>

Ligand: vantictumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Wnt pathway inhibition via the targeting of Frizzled receptors results in decreased growth and tumorigenicity of human tumors.
Published in: Proc Natl Acad Sci USA

Ligand: SRI37892 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of novel frizzled-7 inhibitors by targeting the receptor's transmembrane domain.
Published in: Oncotarget

Ligand: Fz7-21 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Journal): A selective peptide inhibitor of Frizzled 7 receptors disrupts intestinal stem cells.
Published in: Nat Chem Biol
Target family: Class I transporters (type: transporter)
Target: Glucose transporter  4

Ligand: [3H]2-deoxyglucose (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Class I transporters (type: transporter)
Target: Glucose transporter  2

Ligand: [3H]2-deoxyglucose (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Class I transporters (type: transporter)
Target: Glucose transporter  3

Ligand: [3H]2-deoxyglucose (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -
Target family: Class I transporters (type: transporter)
Target: Glucose transporter  1

Ligand: compound 30 [PMID: 22468970] (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): Development of a novel class of glucose transporter inhibitors.
Published in: J Med Chem

Ligand: [3H]2-deoxyglucose (Synthetic organic)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: Claudins (type: other_protein)
Target: claudin 18

Ligand: zolbetuximab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Claudin-18 splice variant 2 is a pan-cancer target suitable for therapeutic antibody development.
Published in: Clin Cancer Res

Ligand: ZWB67 (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Preclinical characterization of a Fab-like CD3/CLDN18.2 XFab&#xae; bispecific antibody against solid tumors.
Published in: Immunobiology
Target family: ClC family (type: other_ic)
Target: ClC-Kb

Ligand: DIDS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -
Target family: ClC family (type: other_ic)
Target: ClC-Ka

Ligand: niflumic acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Median affinity:  pIC50

Ligand: niflumic acid (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Median affinity:  pEC50

Ligand: DIDS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: 3-phenyl-CPP (Synthetic organic)
Interaction type: Channel blocker
Action: None
Median affinity:  -
Target family: ClC family (type: other_ic)
Target: ClC-7

Ligand: NS5818 (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.3 pIC50
Reference (Journal): The G215R mutation in the Cl-/H+-antiporter ClC-7 found in ADO II osteopetrosis does not abolish function but causes a severe trafficking defect.
Published in: PLoS ONE

Ligand: NPPB (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 3.8 pIC50
Reference (Journal): The G215R mutation in the Cl-/H+-antiporter ClC-7 found in ADO II osteopetrosis does not abolish function but causes a severe trafficking defect.
Published in: PLoS ONE

Ligand: DIDS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.4 pIC50
Reference (Journal): The G215R mutation in the Cl-/H+-antiporter ClC-7 found in ADO II osteopetrosis does not abolish function but causes a severe trafficking defect.
Published in: PLoS ONE
Target family: ClC family (type: other_ic)
Target: ClC-6

Ligand: DIDS (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 3 pIC50
Target family: ClC family (type: other_ic)
Target: ClC-4

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.3 pIC50
Reference (Journal): Insights into the ClC-4 transport mechanism from studies of Zn2+ inhibition.
Published in: Biophys J

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Median affinity: 4.2 pIC50
Reference (Journal): Insights into the ClC-4 transport mechanism from studies of Zn2+ inhibition.
Published in: Biophys J
Target family: ClC family (type: other_ic)
Target: ClC-3

Ligand: phloretin (Natural product)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 4.5 pIC50
Target family: ClC family (type: other_ic)
Target: ClC-2

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: omeprazole (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA (1989)
Median affinity:  -

Ligand: NPPB (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: lubiprostone (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Approval source: FDA (2006)
Primary target: yes
Median affinity:  -

Ligand: GaTx2 (Peptide)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity: 10.8 pKd

Ligand: diphenylamine-2-carboxylic acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Median affinity:  -

Ligand: arachidonic acid (Metabolite)
Interaction type: Activator
Action: None
Ligand approved: no
Median affinity:  -
Target family: ClC family (type: other_ic)
Target: ClC-1

Ligand: Zn2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: NMD670 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pEC50
Reference (Journal): The ClC-1 chloride channel inhibitor NMD670 improves skeletal muscle function in rat models and patients with myasthenia gravis.
Published in: Sci Transl Med

Ligand: niflumic acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: yes
Median affinity:  -

Ligand: S-(-)CPP (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: S-(-)CPB (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: fenofibric acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: None
Median affinity:  -

Ligand: 9-anthroic acid (Synthetic organic)
Interaction type: Channel blocker
Action: None
Ligand approved: no
Median affinity:  -
Target family: ClC family (type: other_ic)
Target: ClC-Kb

Ligand: 3-phenyl-CPP (Synthetic organic)
Interaction type: Channel blocker
Action: None
Median affinity:  -

Ligand: niflumic acid (Synthetic organic)
Interaction type: Activator
Action: None
Ligand approved: yes
Median affinity:  pEC50
Target family: CLK family (type: enzyme)
Target: CDC like kinase 3

Ligand: cirtuvivint (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pIC50
Reference (Patent): Methods of treating cartilage disorders through inhibition of clk and dyrk

Ligand: compound 3b [PMID: 23454515] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.260000228881836 pIC50
Reference (Journal): Chemical synthesis and biological validation of immobilized protein kinase inhibitory Leucettines.
Published in: Eur J Med Chem

Ligand: KH-CB19 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.28000020980835 pIC50
Reference (Journal): Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing.
Published in: Chem Biol

Ligand: leucettine L41 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.350000381469727 pIC50
Reference (Journal): Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.
Published in: J Med Chem