Target family: Src family (type: enzyme)
Target: BLK proto-oncogene, Src family tyrosine kinase

Ligand: ZAK inhibitor 6p (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pKd
Reference (Journal): Design, Synthesis, and Structure-Activity Relationships of 1,2,3-Triazole Benzenesulfonamides as New Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors.
Published in: J Med Chem

Ligand: WZ4002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.699999809265137 pKd
Reference (Journal): Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Published in: Nature

Ligand: PRN694 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.900000095367432 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: 8.010000228881836 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: 5.5 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: 10 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: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.
Published in: J Med Chem

Ligand: eCF506 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.270000457763672 pIC50
Reference (Journal): Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.
Published in: J Med Chem

Ligand: compound 9 [PMID: 26006010] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.170000076293945 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: 8.380000114440918 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: 8.569999694824219 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 2 [PMID: 15546730] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Journal): Discovery of novel 2-(aminoheteroaryl)-thiazole-5-carboxamides as potent and orally active Src-family kinase p56(Lck) inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: compound 25 [PMID: 31260299] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 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: CEP-11981 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
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: 6 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med