dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: 1.-.-.- Oxidoreductases (type: enzyme)
Target: dihydroorotate dehydrogenase (quinone)

Ligand: BRD9185 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.300000190734863 pIC50
Reference (Journal): Discovery of Antimalarial Azetidine-2-carbonitriles That Inhibit <i>P. falciparum</i> Dihydroorotate Dehydrogenase.
Published in: ACS Med Chem Lett

Ligand: brequinar (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Inhibition of pyrimidine de novo synthesis by DUP-785 (NSC 368390).
Published in: Invest New Drugs

Ligand: compound 19 [PMID: 35925768] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): <i>N</i>-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Published in: J Med Chem

Ligand: compound 19 [PMID: 35925768] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.960000038146973 pIC50
Reference (Journal): <i>N</i>-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Published in: J Med Chem

Ligand: compound 19 [PMID: 35925768] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.800000190734863 pIC50
Reference (Journal): <i>N</i>-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Published in: J Med Chem

Ligand: compound 19 [PMID: 35925768] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pIC50
Reference (Journal): <i>N</i>-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Published in: J Med Chem

Ligand: compound 19 [PMID: 35925768] (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 pKd
Reference (Journal): <i>N</i>-Heterocyclic 3-Pyridyl Carboxamide Inhibitors of DHODH for the Treatment of Acute Myelogenous Leukemia.
Published in: J Med Chem
Target family: 1-phosphatidylinositol-3-phosphate 5-kinase family (type: enzyme)
Target: phosphoinositide kinase, FYVE-type zinc finger containing

Ligand: apilimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pIC50
Reference (Journal): PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.
Published in: Chem Biol

Ligand: apilimod (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.190000057220459 pKd
Reference (Journal): PIKfyve, a class III PI kinase, is the target of the small molecular IL-12/IL-23 inhibitor apilimod and a player in Toll-like receptor signaling.
Published in: Chem Biol

Ligand: AMG28 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.65999984741211 pIC50
Reference (Journal): Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of &#x3b2;-Coronaviruses.
Published in: J Med Chem

Ligand: compound 17 [PMID: 36111834] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.15999984741211 pIC50
Reference (Journal): Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of &#x3b2;-Coronaviruses.
Published in: J Med Chem

Ligand: compound 17 [PMID: 36111834] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of &#x3b2;-Coronaviruses.
Published in: J Med Chem
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase beta

Ligand: PIK-93 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 pIC50
Reference (Journal): Maintenance of hormone-sensitive phosphoinositide pools in the plasma membrane requires phosphatidylinositol 4-kinase IIIalpha.
Published in: Mol Biol Cell

Ligand: PIK-93 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.71999979019165 pIC50
Reference (Journal): A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling.
Published in: Cell

Ligand: torin 2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Published in: J Med Chem
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase alpha

Ligand: phenylarsine oxide (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Characterization of type II phosphatidylinositol 4-kinase isoforms reveals association of the enzymes with endosomal vesicular compartments.
Published in: J Biol Chem
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase beta

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Functional expression and characterisation of a new human phosphatidylinositol 4-kinase PI4K230.
Published in: Biochim Biophys Acta
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase alpha

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Functional expression and characterisation of a new human phosphatidylinositol 4-kinase PI4K230.
Published in: Biochim Biophys Acta
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase beta

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and characterization of a wortmannin-sensitive human phosphatidylinositol 4-kinase.
Published in: J Biol Chem
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase alpha

Ligand: wortmannin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Cloning and characterization of a wortmannin-sensitive human phosphatidylinositol 4-kinase.
Published in: J Biol Chem
Target family: 1-phosphatidylinositol 4-kinase family (type: enzyme)
Target: phosphatidylinositol 4-kinase beta

Ligand: compound 22 [WO2019141694A1] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Patent): Pi4kiiibeta inhibitors
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: euchromatic histone lysine methyltransferase 1

Ligand: A-366 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Webpage): A-366: a chemical Probe for G9a/GLP.

Ligand: A-366 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.
Published in: ACS Med Chem Lett

Ligand: BIX-01294 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.420000076293945 pIC50
Reference (Journal): Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
Published in: Mol Cell

Ligand: MS8709 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of the First-in-class G9a/GLP PROTAC Degrader.
Published in: bioRxiv

Ligand: UNC0638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.71999979019165 pIC50
Reference (Journal): A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Published in: Nat Chem Biol

Ligand: UNC0642 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Published in: J Med Chem
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: euchromatic histone lysine methyltransferase 2

Ligand: A-366 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.479999542236328 pIC50
Reference (Journal): Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.
Published in: ACS Med Chem Lett

Ligand: A-366 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.479999542236328 pIC50
Reference (Webpage): A-366: a chemical Probe for G9a/GLP.

Ligand: BIX-01294 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.769999980926514 pIC50
Reference (Journal): Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
Published in: Mol Cell

Ligand: BRD9539 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pIC50
Reference (Journal): A small-molecule probe of the histone methyltransferase G9a induces cellular senescence in pancreatic adenocarcinoma.
Published in: ACS Chem Biol

Ligand: CM-272 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.
Published in: Nat Commun

Ligand: MS8709 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of the First-in-class G9a/GLP PROTAC Degrader.
Published in: bioRxiv

Ligand: UNC0321 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.199999809265137 pKi
Reference (Journal): Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines.
Published in: J Med Chem

Ligand: UNC0638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Published in: Nat Chem Biol

Ligand: UNC0638 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pKi
Reference (Journal): A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells.
Published in: Nat Chem Biol

Ligand: UNC0642 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Published in: J Med Chem
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: lysine methyltransferase 5A

Ligand: Cdk4 inhibitor III (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Small-molecule inhibitors of SETD8 with cellular activity.
Published in: ACS Chem Biol

Ligand: nahuoic acid A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pKi
Reference (Journal): Nahuoic acid A produced by a Streptomyces sp. isolated from a marine sediment is a selective SAM-competitive inhibitor of the histone methyltransferase SETD8.
Published in: Org Lett
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: lysine methyltransferase 5B

Ligand: A-196 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Webpage): A-196 A selective chemical probe for SUV420H1/H2
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: lysine methyltransferase 5C

Ligand: A-196 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.840000152587891 pIC50
Reference (Webpage): A-196 A selective chemical probe for SUV420H1/H2
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: nuclear receptor binding SET domain protein 1

Ligand: compound 15a [PMID: 36642961] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.159999847412109 pIC50
Reference (Journal): Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Published in: J Med Chem
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: nuclear receptor binding SET domain protein 2

Ligand: compound 15a [PMID: 36642961] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.639999866485596 pIC50
Reference (Journal): Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Published in: J Med Chem

Ligand: LLC0424 (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of LLC0424 as a Potent and Selective <i>in Vivo</i> NSD2 PROTAC Degrader.
Published in: J Med Chem
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: SET and MYND domain containing 2

Ligand: AZ505 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Structural basis of substrate methylation and inhibition of SMYD2.
Published in: Structure

Ligand: BAY-598 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.570000171661377 pIC50
Reference (Webpage): BAY-598 A selective chemical probe for SMYD2

Ligand: LLY-507 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Webpage): LLY-507: A chemical probe for SMYD2 protein lysine methyltransferase.
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: SUV39H1 histone lysine methyltransferase

Ligand: chaetocin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Chaetocin is a nonspecific inhibitor of histone lysine methyltransferases.
Published in: Nat Chem Biol

Ligand: chaetocin (Natural product)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
Published in: Nat Chem Biol
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: SUV39H2 histone lysine methyltransferase

Ligand: example 203 [WO2017058503A1] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.75 pIC50
Reference (Patent): Bicyclic compound and use thereof for inhibiting suv39h2
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: SET domain containing 7, histone lysine methyltransferase

Ligand: (R)-PFI-2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.479999542236328 pKi
Reference (Journal): (R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells.
Published in: Proc Natl Acad Sci USA
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: DOT1 like histone lysine methyltransferase

Ligand: bromo-deaza-SAH (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.420000076293945 pKi
Reference (Journal): Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Published in: Bioorg Med Chem

Ligand: bromo-deaza-SAH (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.110000133514404 pIC50
Reference (Journal): Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Published in: Bioorg Med Chem

Ligand: compound 13 [Chen et al., 2016] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKi
Reference (Journal): Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach.
Published in: ACS Med Chem Lett

Ligand: EPZ004777 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor.
Published in: Cancer Cell

Ligand: pinometostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKi
Reference (Journal): Potent inhibition of DOT1L as treatment of MLL-fusion leukemia.
Published in: Blood

Ligand: SGC0946 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitors.
Published in: Nat Commun
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: enhancer of zeste 1 polycomb repressive complex 2 subunit

Ligand: GSK343 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.619999885559082 pIC50
Reference (Journal): Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
Published in: ACS Med Chem Lett

Ligand: tulmimetostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.220000267028809 pIC50
Reference (Patent): Ezh2 inhibition in combination therapies for the treatment of cancers

Ligand: valemetostat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2022)
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Novel orally bioavailable EZH1/2 dual inhibitors with greater antitumor efficacy than an EZH2 selective inhibitor.
Published in: Cancer Sci
Target family: 2.1.1.43 Histone methyltransferases (HMTs) (type: enzyme)
Target: enhancer of zeste 2 polycomb repressive complex 2 subunit

Ligand: compound 15a [PMID: 36642961] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
Reference (Journal): Structural Modification and Pharmacological Evaluation of Substituted Quinoline-5,8-diones as Potent NSD2 Inhibitors.
Published in: J Med Chem

Ligand: CPI-1205 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas.
Published in: J Med Chem

Ligand: EBI-2511 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma.
Published in: ACS Med Chem Lett

Ligand: EI1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.029999732971191 pIC50
Reference (Journal): Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation.
Published in: Proc Natl Acad Sci USA
Target family: 2.1.1.- Methyltransferases (type: enzyme)
Target: DNA methyltransferase 1

Ligand: bromo-deaza-SAH (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.019999980926514 pKi
Reference (Journal): Bromo-deaza-SAH: a potent and selective DOT1L inhibitor.
Published in: Bioorg Med Chem

Ligand: CM-272 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pIC50
Reference (Journal): Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies.
Published in: Nat Commun

Ligand: GSK3685032 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.639999866485596 pIC50
Reference (Journal): Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia
Published in: Nature Cancer

Ligand: SGI-1027 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.070000171661377 pIC50
Reference (Journal): Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells.
Published in: J Med Chem