Target family: Type I RTKs: ErbB (epidermal growth factor) receptor family (type: catalytic_receptor)
Target: epidermal growth factor receptor

Ligand: PD 158780 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Tyrosine kinase inhibitors. 12. Synthesis and structure-activity relationships for 6-substituted 4-(phenylamino)pyrimido[5,4-d]pyrimidines designed as inhibitors of the epidermal growth factor receptor.
Published in: J Med Chem

Ligand: PD166285 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.059999942779541 pKi
Reference (Journal): In vitro pharmacological characterization of PD 166285, a new nanomolar potent and broadly active protein tyrosine kinase inhibitor.
Published in: J Pharmacol Exp Ther

Ligand: PD 174265 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.350000381469727 pIC50
Reference (Journal): Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.
Published in: Proc Natl Acad Sci USA

Ligand: pelitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.
Published in: Bioorg Med Chem Lett

Ligand: pelitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
Published in: Bioorg Med Chem

Ligand: PF-670462 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.820000171661377 pIC50
Reference (Journal): An inhibitor of casein kinase I epsilon induces phase delays in circadian rhythms under free-running and entrained conditions.
Published in: J Pharmacol Exp Ther

Ligand: pirotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Quinazoline derivatives substituted by aniline, preparation method and use thereof

Ligand: PKI166 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.430000305175781 pIC50
Reference (Journal): Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.
Published in: Eur J Med Chem

Ligand: poziotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.100000381469727 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: PP1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 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: PP121 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.590000152587891 pIC50
Reference (Journal): Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Published in: Nat Chem Biol

Ligand: pyrotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Irreversible inhibition
Ligand approved: yes
Approval source: China (2018)
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery and development of pyrotinib: A novel irreversible EGFR/HER2 dual tyrosine kinase inhibitor with favorable safety profiles for the treatment of breast cancer.
Published in: Eur J Pharm Sci

Ligand: ralimetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pIC50
Reference (Journal): Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor.
Published in: Cell Chem Biol

Ligand: ralimetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.739999771118164 pIC50
Reference (Journal): Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor.
Published in: Cell Chem Biol

Ligand: ralimetinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.21999979019165 pIC50
Reference (Journal): Inhibition of a lower potency target drives the anticancer activity of a clinical p38 inhibitor.
Published in: Cell Chem Biol

Ligand: rezivertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Substituted 2-anilinopyrimidine derivatives as EGFR modulators

Ligand: rociletinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pKi
Reference (Journal): Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.
Published in: Cancer Discov

Ligand: sapitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.399999618530273 pIC50
Reference (Journal): Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.
Published in: ACS Med Chem Lett

Ligand: selatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pIC50
Reference (Journal): Discovery of a potent dual EGFR/HER-2 inhibitor L-2 (selatinib) for the treatment of cancer.
Published in: Eur J Med Chem

Ligand: sunvozertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2023)
Primary target: no
Median affinity: 7.090000152587891 pIC50
Reference (Patent): Erbb/btk inhibitors

Ligand: tarloxotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Targeting the hypoxic fraction of tumours using hypoxia-activated prodrugs.
Published in: Cancer Chemother Pharmacol

Ligand: tesevatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Inhibition of the T790M gatekeeper mutant of the epidermal growth factor receptor by EXEL-7647.
Published in: Clin Cancer Res

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

Ligand: tigozertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Patent): Inhibitors of mutant forms of EGFR

Ligand: TQB3804 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pIC50
Reference (Patent): Aryl-phosphorus-oxygen compound as egfr kinase inhibitor

Ligand: TQB3804 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.65999984741211 pIC50
Reference (Patent): Aryl-phosphorus-oxygen compound as egfr kinase inhibitor

Ligand: tucatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2021)
Primary target: no
Median affinity: 6.349999904632568 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: tuxobertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Tyrosine kinase inhibitor compositions, methods of making and methods of use

Ligand: vandetanib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2011), EMA (2012)
Primary target: no
Median affinity: 6.519999980926514 pIC50
Reference (Journal): ZD6474, an orally available inhibitor of KDR tyrosine kinase activity, efficiently blocks oncogenic RET kinases.
Published in: Cancer Res

Ligand: WZ4002 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.340000152587891 pKd
Reference (Journal): Novel mutant-selective EGFR kinase inhibitors against EGFR T790M.
Published in: Nature

Ligand: xiliertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.300000190734863 pKi
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: zipalertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations.
Published in: Mol Cancer Ther

Ligand: zipalertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations.
Published in: Mol Cancer Ther

Ligand: zipalertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.130000114440918 pIC50
Reference (Journal): TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations.
Published in: Mol Cancer Ther

Ligand: ZM-306416 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery.
Published in: J Biomol Screen

Ligand: zongertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.239999771118164 pIC50
Reference (Patent): [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors

Ligand: zorifertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.140000343322754 pIC50
Reference (Journal): Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.
Published in: J Med Chem

Ligand: zorifertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.520000457763672 pIC50
Reference (Journal): Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.
Published in: J Med Chem