Target family: Type I RTKs: ErbB (epidermal growth factor) receptor family (type: catalytic_receptor)
Target: erb-b2 receptor tyrosine kinase 4

Ligand: acalabrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2020)
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med

Ligand: AEE788 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.590000152587891 pIC50
Reference (Journal): AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity.
Published in: Cancer Res

Ligand: allitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.100000381469727 pIC50
Reference (Journal): AST1306, a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, exhibits antitumor activity both in vitro and in vivo.
Published in: PLoS ONE

Ligand: betacellulin (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: BMS-599626 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 pIC50
Reference (Journal): Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.
Published in: J Med Chem

Ligand: compound 38 [PMID: 24915291] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.479999542236328 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 9 [PMID: 26006010] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.190000057220459 pIC50
Reference (Journal): Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Published in: Nat Chem Biol

Ligand: dacomitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 7.130000114440918 pIC50
Reference (Journal): Irreversible protein kinase inhibitors: balancing the benefits and risks.
Published in: J Med Chem

Ligand: EGFR/ErbB-2/ErbB-4 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Published in: J Med Chem

Ligand: epiregulin (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: HB-EGF (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: ibrutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: no
Median affinity: 8.470000267028809 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med

Ligand: neuregulin-1 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: neuregulin-2 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: neuregulin-3 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: neuregulin-4 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity:  -

Ligand: pirotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.720000267028809 pIC50
Reference (Patent): Quinazoline derivatives substituted by aniline, preparation method and use thereof

Ligand: poziotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.630000114440918 pIC50
Reference (Journal): Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer.
Published in: Cancer Lett

Ligand: tucatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: no
Median affinity: 6.510000228881836 pIC50
Reference (Journal): Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models.
Published in: Mol Cancer Ther

Ligand: xiliertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 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: WZ4002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pKd
Reference (Journal): Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Published in: Nature