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

Ligand: cinsebrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Patent): Kinase inhibitors

Ligand: CNX-774 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Irreversible protein kinase inhibitors: balancing the benefits and risks.
Published in: J Med Chem

Ligand: compound 25 [PMID: 31260299] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.279999732971191 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: compound 2c [PMID: 24900538] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.460000038146973 pIC50
Reference (Journal): Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
Published in: ACS Med Chem Lett

Ligand: compound 31 [PMID: 24915291] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.359999656677246 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 36 [PMID: 21958547] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.710000038146973 pIC50
Reference (Journal): Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
Published in: Bioorg Med Chem Lett

Ligand: compound 38 [PMID: 24915291] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.359999656677246 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 4g [PMID: 30893553] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.279999732971191 pIC50
Reference (Journal): Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton's Tyrosine Kinase (BTK).
Published in: J Med Chem

Ligand: compound 71 [WO2018191577A1] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Benzoazepine analogs as inhibiting agents for bruton's tyrosine kinase

Ligand: compound 9 [PMID: 26006010] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.720000267028809 pIC50
Reference (Journal): Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Published in: Nat Chem Biol

Ligand: DD-03-171 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pIC50
Reference (Journal): Bruton tyrosine kinase degradation as a therapeutic strategy for cancer.
Published in: Blood

Ligand: elsubrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Primary carboxamides as BTK inhibitors

Ligand: evobrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity.

Ligand: Example A225 [WO2012170976A2] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Compositions and methods for the production of pyrimidine and pyridine compounds with btk inhibitory activity.

Ligand: fenebrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Heteroaryl pyridone and aza-pyridone compounds as inhibitors of btk activity

Ligand: GDC-0834 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Potent and selective Bruton's tyrosine kinase inhibitors: discovery of GDC-0834.
Published in: Bioorg Med Chem Lett

Ligand: ibrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: yes
Median affinity: 8.819999694824219 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med

Ligand: ibrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: yes
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Discovery of selective irreversible inhibitors for Bruton's tyrosine kinase.
Published in: ChemMedChem

Ligand: JNJ-64264681 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.25 pIC50
Reference (Journal): Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Published in: J Med Chem

Ligand: JNJ-64264681 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.309999942779541 pKi
Reference (Journal): Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Published in: J Med Chem