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

Ligand: ibrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: no
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med

Ligand: JNJ-28312141 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.059999942779541 pIC50
Reference (Journal): JNJ-28312141, a novel orally active colony-stimulating factor-1 receptor/FMS-related receptor tyrosine kinase-3 receptor tyrosine kinase inhibitor with potential utility in solid tumors, bone metastases, and acute myeloid leukemia.
Published in: Mol Cancer Ther

Ligand: Lck inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck II.
Published in: Bioorg Med Chem Lett

Ligand: nefextinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.260000228881836 pIC50
Reference (Patent): Fused pyrimidine compound, and intermediate, preparation method, composition and application of

Ligand: neolymphostin A (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.340000152587891 pKd
Reference (Journal): Neolymphostin A Is a Covalent Phosphoinositide 3-Kinase (PI3K)/Mammalian Target of Rapamycin (mTOR) Dual Inhibitor That Employs an Unusual Electrophilic Vinylogous Ester.
Published in: J Med Chem

Ligand: pexidartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2019)
Primary target: no
Median affinity: 6.070000171661377 pIC50
Reference (Journal): Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor.
Published in: N Engl J Med

Ligand: PP1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation.
Published in: J Biol Chem

Ligand: PP2 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation.
Published in: J Biol Chem

Ligand: saracatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Published in: J Med Chem

Ligand: SU6656 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.820000171661377 pIC50
Reference (Journal): The selectivity of protein kinase inhibitors: a further update.
Published in: Biochem J

Ligand: TAK-020 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 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: WH-4-023 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Published in: J Med Chem

Ligand: xiliertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.75 pIC50
Reference (Journal): Anti-tumor efficacy of theliatinib in esophageal cancer patient-derived xenografts models with epidermal growth factor receptor (EGFR) overexpression and gene amplification.
Published in: Oncotarget

Ligand: ZAK inhibitor 6p (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 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