Target family: Tec family (type: enzyme)
Target: Bruton tyrosine kinase

Ligand: LFM-A13 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4.760000228881836 pIC50
Reference (Journal): Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2, 5-dibromophenyl)propenamide].
Published in: J Biol Chem

Ligand: luxeptinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10 pIC50
Reference (Patent): 2,3-dihydro-isoindole-1-on derivative as BTK kinase suppressant, and pharmaceutical composition including same

Ligand: milrebrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.069999694824219 pIC50
Reference (Journal): Discovery of AS-1763: A Potent, Selective, Noncovalent, and Orally Available Inhibitor of Bruton's Tyrosine Kinase.
Published in: J Med Chem

Ligand: nemtabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation.
Published in: Cancer Discov

Ligand: orelabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2020)
Primary target: no
Median affinity: 8.359999656677246 pIC50
Reference (Patent): Substituted nicotinimide inhibitors of btk and their preparation and use in the treatment of cancer, inflammation and autoimmune disease

Ligand: pirtobrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2023)
Primary target: no
Median affinity: 8.0600004196167 pIC50
Reference (Patent): Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide

Ligand: pirtobrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA & EMA (2023)
Primary target: no
Median affinity: 8.069999694824219 pIC50
Reference (Patent): Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide

Ligand: poseltinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pIC50
Reference (Patent): Novel fused pyrimidine derivatives for inhd3ition of tyrosine kinase activity.

Ligand: PRN694 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pIC50
Reference (Journal): Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.
Published in: J Biol Chem

Ligand: PROTAC 23 [PMID: 38321747] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pKi
Reference (Journal): Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases.
Published in: J Med Chem

Ligand: PROTAC 23 [PMID: 38321747] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Discovery of Novel Potent and Fast BTK PROTACs for the Treatment of Osteoclasts-Related Inflammatory Diseases.
Published in: J Med Chem

Ligand: PTD10 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pIC50
Reference (Journal): Discovery of Novel Bruton’s Tyrosine Kinase PROTACs with Enhanced Selectivity and Cellular Efficacy
Published in: Journal of  Mediconal Chemistry

Ligand: remibrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Novel amino pyrimidine derivatives

Ligand: rilzabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.819999694824219 pIC50
Reference (Patent): PYRAZOLOPYRIMIDINE COMPOUNDS AS KINASE INHIBITORS

Ligand: RN486 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.510000228881836 pKd
Reference (Journal): RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.
Published in: J Pharmacol Exp Ther

Ligand: sofnobrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.40999984741211 pIC50
Reference (Journal): Design and Synthesis of Novel Amino-triazine Analogues as Selective Bruton's Tyrosine Kinase Inhibitors for Treatment of Rheumatoid Arthritis.
Published in: J Med Chem

Ligand: spebrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 pIC50
Reference (Webpage): Clinical Development of AVL - 292: A Potent, Selective Covalent Btk Inhibitor for the Treatment of B Cell Malignancies.

Ligand: sunvozertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2023)
Primary target: no
Median affinity: 8.539999961853027 pIC50
Reference (Patent): Erbb/btk inhibitors

Ligand: TAK-020 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Discovery of the Bruton's Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (<i>S</i>)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3<i>H</i>-1,2,4-triazol-3-one, by Fragment-Based Drug Design.
Published in: J Med Chem

Ligand: tirabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: Japan (2020)
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Patent): Purinone derivative

Ligand: tolebrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.670000076293945 pIC50
Reference (Patent): Tyrosine kinase inhibitors

Ligand: vecabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.140000343322754 pIC50
Reference (Patent): Pyrimidinyl tyrosine kinase inhibitors

Ligand: WZ4002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.369999885559082 pKd
Reference (Journal): Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Published in: Nature

Ligand: zanubrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019), EMA (2021)
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Patent): Substituted pyrazolo[1,5-a]pyrimidines as bruton's tyrosine kinase modulators.

Ligand: ZYBT1 (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.849999904632568 pKi
Reference (Journal): ZYBT1, a potent, irreversible Bruton's Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer.
Published in: Pharmacol Res Perspect

Ligand: ZYBT1 (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): ZYBT1, a potent, irreversible Bruton's Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer.
Published in: Pharmacol Res Perspect