dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: CatSper and Two-Pore channels (TPC) (type: vgic)
Target: TPC2

Ligand: TPC2-A1-N (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 5.110000133514404 pEC50
Reference (Journal): Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function.
Published in: Elife

Ligand: SG-005 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pIC50
Reference (Journal): Gene editing and synthetically accessible inhibitors reveal role for TPC2 in HCC cell proliferation and tumor growth.
Published in: Cell Chem Biol

Ligand: phosphatidyl (3,5) inositol bisphosphate (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 pEC50
Reference (Journal): TPC proteins are phosphoinositide- activated sodium-selective ion channels in endosomes and lysosomes.
Published in: Cell

Ligand: MT-8 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.590000152587891 pIC50
Reference (Journal): Flavonoids increase melanin production and reduce proliferation, migration and invasion of melanoma cells by blocking endolysosomal/melanosomal TPC2.
Published in: Sci Rep
Target family: CatSper and Two-Pore channels (TPC) (type: vgic)
Target: TPC1

Ligand: verapamil (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 4.639999866485596 pIC50
Reference (Journal): The voltage-gated sodium channel TPC1 confers endolysosomal excitability.
Published in: Nat Chem Biol

Ligand: phosphatidyl (3,5) inositol bisphosphate (Metabolite)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pEC50
Reference (Journal): The voltage-gated sodium channel TPC1 confers endolysosomal excitability.
Published in: Nat Chem Biol

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: Inhibition
Primary target: no
Median affinity: 3.740000009536743 pIC50
Reference (Journal): The voltage-gated sodium channel TPC1 confers endolysosomal excitability.
Published in: Nat Chem Biol
Target family: CatSper and Two-Pore channels (TPC) (type: vgic)
Target: CatSper4

Ligand: ruthenium red (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Median affinity: 5 pIC50
Reference (Journal): Whole-cell patch-clamp measurements of spermatozoa reveal an alkaline-activated Ca2+ channel.
Published in: Nature

Ligand: progesterone (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: no
Median affinity: 8.109999656677246 pEC50
Reference (Journal): The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm.
Published in: Nature

Ligand: progesterone (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: no
Median affinity: 8.109999656677246 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: PGF1α (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature
Target family: CatSper and Two-Pore channels (TPC) (type: vgic)
Target: CatSper4

Ligand: Cd2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Median affinity: 3.7 pIC50
Reference (Journal): Whole-cell patch-clamp measurements of spermatozoa reveal an alkaline-activated Ca2+ channel.
Published in: Nature

Ligand: mibefradil (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997)
Primary target: no
Median affinity:  pIC50
Reference (Journal): The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm.
Published in: Nature

Ligand: Ni2+ (Inorganic)
Interaction type: Channel blocker
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 3.5 pIC50
Reference (Journal): Whole-cell patch-clamp measurements of spermatozoa reveal an alkaline-activated Ca2+ channel.
Published in: Nature

Ligand: NNC55-0396 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: NNC55-0396 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: NNC55-0396 (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: no
Median affinity: 5.7 pIC50
Reference (Journal): The CatSper channel mediates progesterone-induced Ca2+ influx in human sperm.
Published in: Nature

Ligand: PGE1 (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1981)
Median affinity: 6.3 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature

Ligand: PGE2 (Metabolite)
Interaction type: Activator
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1977)
Median affinity: 6.3 pEC50
Reference (Journal): Progesterone activates the principal Ca2+ channel of human sperm.
Published in: Nature
Target family: CatSper and Two-Pore channels (TPC) (type: vgic)
Target: TPC2

Ligand: verapamil (Synthetic organic)
Interaction type: Channel blocker
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1981)
Primary target: no
Median affinity: 5 pIC50
Reference (Journal): TPC proteins are phosphoinositide- activated sodium-selective ion channels in endosomes and lysosomes.
Published in: Cell

Ligand: UM-9 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.019999980926514 pIC50
Reference (Journal): Flavonoids increase melanin production and reduce proliferation, migration and invasion of melanoma cells by blocking endolysosomal/melanosomal TPC2.
Published in: Sci Rep

Ligand: TPC2-A1-P (Synthetic organic)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity: 4.980000019073486 pEC50
Reference (Journal): Agonist-mediated switching of ion selectivity in TPC2 differentially promotes lysosomal function.
Published in: Elife

Ligand: SG-094 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.079999923706055 pIC50
Reference (Journal): Gene editing and synthetically accessible inhibitors reveal role for TPC2 in HCC cell proliferation and tumor growth.
Published in: Cell Chem Biol
Target family: CD33-related SIGLECs (type: other_protein)
Target: CD33

Ligand: gemtuzumab ozogamicin (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2000), EMA (2018)
Primary target: yes
Median affinity:  -
Reference (Journal): Monoclonal antibodies to the myeloid stem cells: therapeutic implications of CMA-676, a humanized anti-CD33 antibody calicheamicin conjugate.
Published in: Leukemia

Ligand: lintuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 10 pKd
Reference (Journal): Biological and immunological features of humanized M195 (anti-CD33) monoclonal antibodies.
Published in: Cancer Res

Ligand: vadastuximab talirine (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 pKd
Reference (Journal): SGN-CD33A: a novel CD33-targeting antibody-drug conjugate using a pyrrolobenzodiazepine dimer is active in models of drug-resistant AML.
Published in: Blood
Target family: CD33-related SIGLECs (type: other_protein)
Target: sialic acid binding Ig like lectin 10

Ligand: MK-7110 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Methods of use of soluble cd24 for therapy of rheumatoid arthritis
Target family: CDK1 subfamily (type: enzyme)
Target: cyclin dependent kinase 3

Ligand: RGB-286638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs.
Published in: Leukemia

Ligand: zotiraciclib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties.
Published in: Leukemia
Target family: CDK8 subfamily (type: enzyme)
Target: cyclin dependent kinase 19

Ligand: CCT251545 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.600000381469727 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: compound 51 [Mallinger et al., 2016] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.25 pIC50
Reference (Journal): 2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.
Published in: ACS Med Chem Lett

Ligand: cortistatin A (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pKd
Reference (Journal): Cortistatin A is a high-affinity ligand of protein kinases ROCK, CDK8, and CDK11.
Published in: Angew Chem Int Ed Engl

Ligand: JH-VIII-49 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.
Published in: ACS Med Chem Lett

Ligand: linifanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: pexidartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
Published in: N Engl J Med

Ligand: ponatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2012), EMA (2013)
Primary target: no
Median affinity: 7.920000076293945 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol

Ligand: sorafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2006)
Primary target: no
Median affinity: 6.989999771118164 pKd
Reference (Journal): A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
Published in: Nat Chem Biol
Target family: CD molecules (type: other_protein)
Target: programmed cell death 1 (CD279)

Ligand: cemiplimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: yes
Median affinity: 8.210000038146973 pKd
Reference (Journal): Characterization of the Anti-PD-1 Antibody REGN2810 and Its Antitumor Activity in Human <i>PD-1</i> Knock-In Mice.
Published in: Mol Cancer Ther

Ligand: cemiplimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 9.279999732971191 pKd
Reference (Journal): Characterization of the Anti-PD-1 Antibody REGN2810 and Its Antitumor Activity in Human <i>PD-1</i> Knock-In Mice.
Published in: Mol Cancer Ther

Ligand: cadonilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: China NMPA (2022)
Primary target: yes
Median affinity: 10.289999961853027 pEC50
Reference (Journal): Cadonilimab, a tetravalent PD-1/CTLA-4 bispecific antibody with trans-binding and enhanced target binding avidity.
Published in: MAbs

Ligand: AUNP-12 (Peptide)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.140000343322754 pEC50
Reference (Patent): Immunosuppression modulating compounds
Target family: CD molecules (type: other_protein)
Target: Natural cytotoxicity triggering receptor 3 (CD337)

Ligand: Natural cytotoxicity triggering receptor 3 ligand 1 (Peptide)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: Large proline-rich protein BAG6 (Peptide)
Interaction type: Activator
Action: Activation
Ligand approved: no
Primary target: no
Median affinity:  -
Target family: CD molecules (type: other_protein)
Target: leukocyte immunoglobulin like receptor A4 (CD85g)

Ligand: anti-ILT7 antibody (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Patent): Anti-ILT7 antibody
Target family: CD molecules (type: other_protein)
Target: LAG3 (CD223)

Ligand: relatlimab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: yes
Approval source: EMA & FDA (2022)
Primary target: yes
Median affinity:  -
Reference (Patent): Optimization of antibodies that bind lymphocyte activation gene-3 (lag-3), and uses thereof
Target family: CD molecules (type: other_protein)
Target: killer cell lectin like receptor C1 (CD159a)

Ligand: monalizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 10.569999694824219 pKd
Reference (Patent): Treatment regimens using anti-nkg2a antibodies
Target family: CD molecules (type: other_protein)
Target: ICOS (CD278)

Ligand: feladilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 9.020000457763672 pKd
Reference (Patent): Agonistic icos binding proteins

Ligand: feladilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.869999885559082 pKd
Reference (Patent): Agonistic icos binding proteins
Target family: CD molecules (type: other_protein)
Target: Fc fragment of IgG receptor IIIa

Ligand: bemarituzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.039999961853027 pKd
Reference (Journal): Population pharmacokinetic analysis of phase 1 bemarituzumab data to support phase 2 gastroesophageal adenocarcinoma FIGHT trial.
Published in: Cancer Chemother Pharmacol

Ligand: AFM13 (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  pKd
Reference (Journal): A novel tetravalent bispecific TandAb (CD30/CD16A) efficiently recruits NK cells for the lysis of CD30+ tumor cells.
Published in: MAbs
Target family: CD molecules (type: other_protein)
Target: Fc fragment of IgA receptor

Ligand: BsAb (CD89-CD20) (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 8.489999771118164 pKd
Reference (Journal): CD89-mediated recruitment of macrophages via a bispecific antibody enhances anti-tumor efficacy.
Published in: Oncoimmunology
Target family: CD molecules (type: other_protein)
Target: endoglin (CD105)

Ligand: carotuximab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9 pKd
Reference (Patent): Endoglin antibodies
Target family: CD molecules (type: other_protein)
Target: cytotoxic T-lymphocyte-associated protein 4 (CD152)

Ligand: tremelimumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2022), EMA (2023)
Primary target: yes
Median affinity: 8.90999984741211 pKd
Reference (Patent): Human monoclonal antibodies to CTLA-4.

Ligand: nurulimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Human CTLA-4 antibodies

Ligand: ipilimumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA and EMA (2011)
Primary target: yes
Median affinity: 9 pKd
Reference (Patent): Human ctla-4 antibodies and their uses.

Ligand: cadonilimab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: China NMPA (2022)
Primary target: yes
Median affinity: 10.100000381469727 pEC50
Reference (Journal): Cadonilimab, a tetravalent PD-1/CTLA-4 bispecific antibody with trans-binding and enhanced target binding avidity.
Published in: MAbs
Target family: CD molecules (type: other_protein)
Target: CS1 (CD319)

Ligand: elotuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: yes
Median affinity: 8.050000190734863 pKd
Reference (Patent): Therapeutic use of anti-CS1 antibodies.
Target family: CD molecules (type: other_protein)
Target: CD86

Ligand: belatacept (Peptide)
Interaction type: Fusion protein
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2011)
Primary target: yes
Median affinity:  -
Reference (Journal): Assessment of belatacept-mediated costimulation blockade through evaluation of CD80/86-receptor saturation.
Published in: Transplantation

Ligand: abatacept (Peptide)
Interaction type: Fusion protein
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2005)
Primary target: yes
Median affinity: 7.920000076293945 pKd
Reference (Journal): Update on the use of abatacept for the treatment of rheumatoid arthritis.
Published in: Expert Rev Clin Immunol

Ligand: abatacept (Peptide)
Interaction type: Fusion protein
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2005)
Primary target: yes
Median affinity: 7.920000076293945 pKd
Reference (Journal): CTLA-4 is a second receptor for the B cell activation antigen B7.
Published in: J Exp Med
Target family: CD molecules (type: other_protein)
Target: CD80

Ligand: belatacept (Peptide)
Interaction type: Fusion protein
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2011)
Primary target: yes
Median affinity:  -
Reference (Journal): Assessment of belatacept-mediated costimulation blockade through evaluation of CD80/86-receptor saturation.
Published in: Transplantation

Ligand: abatacept (Peptide)
Interaction type: Fusion protein
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2005)
Primary target: yes
Median affinity: 7.920000076293945 pKd
Reference (Journal): Update on the use of abatacept for the treatment of rheumatoid arthritis.
Published in: Expert Rev Clin Immunol

Ligand: abatacept (Peptide)
Interaction type: Fusion protein
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2005), EMA (2005)
Primary target: yes
Median affinity: 7.920000076293945 pKd
Reference (Journal): CTLA-4 is a second receptor for the B cell activation antigen B7.
Published in: J Exp Med
Target family: CD molecules (type: other_protein)
Target: CD79B

Ligand: polatuzumab vedotin (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2019), EMA (2020)
Primary target: yes
Median affinity:  -
Reference (Patent): Anti-CD79B antibodies and immunoconjugates and methods of use.
Target family: CD molecules (type: other_protein)
Target: CD74

Ligand: milatuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 pKd
Reference (Journal): Anti-CD74 antibody-doxorubicin conjugate, IMMU-110, in a human multiple myeloma xenograft and in monkeys.
Published in: Clin Cancer Res
Target family: CD molecules (type: other_protein)
Target: CD66e (CEACAM5)

Ligand: labetuzumab govitecan (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -

Ligand: labetuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -
Target family: CD molecules (type: other_protein)
Target: CD6

Ligand: itolizumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: DCGI (India; 2013)
Primary target: yes
Median affinity: 7.21999979019165 pKi
Reference (Journal): Towards the definition of a chimpanzee and human conserved CD6 domain 1 epitope recognized by T1 monoclonal antibody.
Published in: Hybridoma (Larchmt)
Target family: CD molecules (type: other_protein)
Target: CD52

Ligand: alemtuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2001), EMA (2013)
Primary target: yes
Median affinity:  -
Reference (Journal): Levels of expression of CD52 in normal and leukemic B and T cells: correlation with in vivo therapeutic responses to Campath-1H.
Published in: Leuk Res

Ligand: alemtuzumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2001), EMA (2013)
Primary target: yes
Median affinity:  -
Reference (Patent): Recombinant antibody composition.