Target family: Tec family (type: enzyme)
Target: tec protein tyrosine kinase

Ligand: ZYBT1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 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

Ligand: PRN694 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 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: nemtabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation.
Published in: Cancer Discov

Ligand: JNJ-64264681 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pIC50
Reference (Journal): Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Published in: J Med Chem

Ligand: ibrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: no
Median affinity: 8.149999618530273 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med

Ligand: compound 9 [PMID: 26006010] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.470000267028809 pIC50
Reference (Journal): Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Published in: Nat Chem Biol

Ligand: compound 38 [PMID: 24915291] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.
Published in: J Med Chem

Ligand: compound 31 [PMID: 24915291] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.09000015258789 pIC50
Reference (Journal): Discovery of a series of 2,5-diaminopyrimidine covalent irreversible inhibitors of Bruton's tyrosine kinase with in vivo antitumor activity.
Published in: J Med Chem

Ligand: compound 25 [PMID: 31260299] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.639999866485596 pIC50
Reference (Journal): Discovery of 4-Aminoquinoline-3-carboxamide Derivatives as Potent Reversible Bruton's Tyrosine Kinase Inhibitors for the Treatment of Rheumatoid Arthritis.
Published in: J Med Chem

Ligand: acalabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2020)
Primary target: no
Median affinity: 7.03000020980835 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med