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

Ligand: abivertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.109999656677246 pIC50
Reference (Journal): AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients.
Published in: Mol Cancer Ther

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

Ligand: AEE788 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 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: afatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2013)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models.
Published in: Oncogene

Ligand: afatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2013)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification.
Published in: J Med Chem

Ligand: afatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: EMA & FDA (2013)
Primary target: yes
Median affinity: 9.600000381469727 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: AG 112 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.900000095367432 pIC50
Reference (Journal): Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
Published in: J Med Chem

Ligand: AG1478 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Use of a pharmacophore model for the design of EGFR tyrosine kinase inhibitors: isoflavones and 3-phenyl-4(1H)-quinolones.
Published in: J Med Chem

Ligand: AG 490 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.400000095367432 pIC50
Reference (Journal): Tyrphostins. 2. Heterocyclic and alpha-substituted benzylidenemalononitrile tyrphostins as potent inhibitors of EGF receptor and ErbB2/neu tyrosine kinases.
Published in: J Med Chem

Ligand: AG 9 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 3.4000000953674316 pKi
Reference (Journal): Tyrphostins I: synthesis and biological activity of protein tyrosine kinase inhibitors.
Published in: J Med Chem

Ligand: allitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 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: amivantamab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA & EMA (2021)
Primary target: yes
Median affinity: 8.850000381469727 pKd
Reference (Journal): Impact of Cell-surface Antigen Expression on Target Engagement and Function of an Epidermal Growth Factor Receptor × c-MET Bispecific Antibody.
Published in: J Biol Chem

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

Ligand: asandeutertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.920000076293945 pIC50
Reference (Patent): 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof

Ligand: asandeutertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.699999809265137 pIC50
Reference (Patent): 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof

Ligand: asandeutertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Patent): 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof

Ligand: aumolertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2020)
Primary target: no
Median affinity: 8.720000267028809 pIC50
Reference (Patent): Egfr inhibitor, and preparation and application thereof

Ligand: AZ5104 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Recent progress on third generation covalent EGFR inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: BDTX-1535 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Alkynyl quinazoline compounds

Ligand: BDTX-1535 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Alkynyl quinazoline compounds

Ligand: BDTX-1535 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Patent): Alkynyl quinazoline compounds

Ligand: befotertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China NMPA (2023)
Primary target: no
Median affinity:  -
Reference (Patent): Pyrimidine or pyridine compound, and preparation method and pharmaceutical application thereof

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

Ligand: BI-4020 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.220000267028809 pIC50
Reference (Journal): Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors.
Published in: J Med Chem

Ligand: BI-4142 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.570000171661377 pIC50
Reference (Journal): Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling.
Published in: Nat Cancer

Ligand: BMS-599626 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.489999771118164 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: BMS-690514 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2.
Published in: J Pharm Sci

Ligand: BPIQ-I (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 10.600000381469727 pIC50
Reference (Journal): Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.
Published in: J Med Chem

Ligand: brigatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 6.889999866485596 pIC50
Reference (Journal): Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.
Published in: Proc Natl Acad Sci USA

Ligand: C34 [Zhu et al., 2023] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.96999979019165 pIC50
Reference (Journal): Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance
Published in: J Med Chem

Ligand: C34 [Zhu et al., 2023] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.289999961853027 pIC50
Reference (Journal): Discovery of Novel Fourth-Generation EGFR Inhibitors to Overcome C797S-Mediated Resistance
Published in: J Med Chem

Ligand: canertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.819999694824219 pIC50
Reference (Journal): Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions.
Published in: J Med Chem

Ligand: canertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.720000267028809 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: cetuximab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: Switzerland (2003), EMA & FDA (2004)
Primary target: yes
Median affinity: 9.40999984741211 pKd
Reference (Patent): Epidermal growth factor; nucleic acids, protein which binds to epidermal growth factor receptors; genetic engineering.

Ligand: CH7233163 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.550000190734863 pIC50
Reference (Journal): CH7233163 Overcomes Osimertinib-Resistant EGFR-Del19/T790M/C797S Mutation.
Published in: Mol Cancer Ther

Ligand: compound 17b [PMID: 35286086] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Gefitinib-Tamoxifen Hybrid Ligands as Potent Agents against Triple-Negative Breast Cancer.
Published in: J Med Chem

Ligand: compound 18j [PMID: 35446588] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.630000114440918 pIC50
Reference (Journal): Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Published in: J Med Chem

Ligand: compound 18j [PMID: 35446588] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pIC50
Reference (Journal): Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations.
Published in: J Med Chem

Ligand: compound 19a [PMID: 30503936] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.28000020980835 pIC50
Reference (Journal): Discovery of N<sup>1</sup>-(4-((7-(3-(4-ethylpiperazin-1-yl)propoxy)-6-methoxyquinolin-4-yl)oxy)-3,5-difluorophenyl)-N<sup>3</sup>-(2-(2,6-difluorophenyl)-4-oxothiazolidin-3-yl)urea as a multi-tyrosine kinase inhibitor for drug-sensitive and drug-resistant cancers treatment.
Published in: Eur J Med Chem

Ligand: compound 38 [PMID: 24915291] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.149999618530273 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 52 [PMID: 36749735] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.820000171661377 pIC50
Reference (Journal): Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer.
Published in: J Med Chem

Ligand: compound 52 [PMID: 36749735] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Development of Furanopyrimidine-Based Orally Active Third-Generation EGFR Inhibitors for the Treatment of Non-Small Cell Lung Cancer.
Published in: J Med Chem

Ligand: compound 56 [PMID: 8568816] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 11.220000267028809 pIC50
Reference (Journal): Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.
Published in: J Med Chem

Ligand: compound 6g [PMID: 30633509] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 pIC50
Reference (Journal): Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
Published in: J Med Chem

Ligand: CUDC-101 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.619999885559082 pIC50
Reference (Journal): Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
Published in: J Med Chem

Ligand: dacomitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2018), EMA (2019)
Primary target: no
Median affinity: 8.220000267028809 pIC50
Reference (Journal): Irreversible protein kinase inhibitors: balancing the benefits and risks.
Published in: J Med Chem

Ligand: DBPR112 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.320000171661377 pIC50
Reference (Journal): Discovery of a Furanopyrimidine-Based Epidermal Growth Factor Receptor Inhibitor (DBPR112) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer.
Published in: J Med Chem

Ligand: dosimertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pIC50
Reference (Journal): Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer.
Published in: J Med Chem

Ligand: dosimertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.940000057220459 pIC50
Reference (Journal): Discovery of Dosimertinib, a Highly Potent, Selective, and Orally Efficacious Deuterated EGFR Targeting Clinical Candidate for the Treatment of Non-Small-Cell Lung Cancer.
Published in: J Med Chem

Ligand: dovitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pIC50
Reference (Journal): CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma.
Published in: Blood

Ligand: EAI045 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors.
Published in: Nature

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

Ligand: EGFR/ErbB-2/ErbB-4 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 9.520000457763672 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: EGFR/ErbB-2 inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and C-erbB-2.
Published in: Bioorg Med Chem Lett

Ligand: EGFR inhibitor (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.679999828338623 pIC50
Reference (Journal): A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
Published in: Proc Natl Acad Sci USA

Ligand: EGFR inhibitor 57 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pIC50
Reference (Journal): Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Published in: J Med Chem

Ligand: EGFR inhibitor 57 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
Published in: J Med Chem

Ligand: EP26 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.429999828338623 pIC50
Reference (Journal): Discovery of Novel Small-Molecule-Based Potential PD-L1/EGFR Dual Inhibitors with High Druggability for Glioblastoma Immunotherapy.
Published in: J Med Chem

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

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

Ligand: erlotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2004), EMA (2005)
Primary target: yes
Median affinity: 9.170000076293945 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: erlotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2004), EMA (2005)
Primary target: yes
Median affinity: 9 pIC50
Reference (Journal): Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: example 10 [CN110740999A] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Patent): N2, N4-diphenylpyrimidine-2, 4-diamine derivative, process for producing the same, and pharmaceutical composition for preventing or treating cancer comprising the same as active ingredient

Ligand: example 10 [CN110740999A] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.369999885559082 pIC50
Reference (Patent): N2, N4-diphenylpyrimidine-2, 4-diamine derivative, process for producing the same, and pharmaceutical composition for preventing or treating cancer comprising the same as active ingredient

Ligand: example 10 [CN110740999A] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pIC50
Reference (Patent): N2, N4-diphenylpyrimidine-2, 4-diamine derivative, process for producing the same, and pharmaceutical composition for preventing or treating cancer comprising the same as active ingredient

Ligand: example 10 [CN110740999A] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.149999618530273 pIC50
Reference (Patent): N2, N4-diphenylpyrimidine-2, 4-diamine derivative, process for producing the same, and pharmaceutical composition for preventing or treating cancer comprising the same as active ingredient

Ligand: falnidamol (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives.
Published in: J Pharmacol Exp Ther

Ligand: firmonertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2021)
Primary target: no
Median affinity:  -
Reference (Patent): Pyridinylaminopyrimidine derivatives, preparation process and use thereof.

Ligand: gefitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2003), EMA (2009)
Primary target: no
Median affinity: 8.960000038146973 pKd
Reference (Journal): Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
Published in: J Med Chem

Ligand: gefitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2003), EMA (2009)
Primary target: yes
Median affinity: 8.300000190734863 pKi
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: gefitinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2003), EMA (2009)
Primary target: yes
Median affinity: 9 pKd
Reference (Journal): Comprehensive analysis of kinase inhibitor selectivity.
Published in: Nat Biotechnol

Ligand: HB-EGF (Peptide)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: 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: 8.279999732971191 pIC50
Reference (Journal): Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia.
Published in: N Engl J Med

Ligand: icotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: China (2011)
Primary target: yes
Median affinity: 7.349999904632568 pIC50
Reference (Journal): Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.
Published in: Bioorg Med Chem Lett

Ligand: JAK3 inhibitor II (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pIC50
Reference (Journal): The specificity of JAK3 kinase inhibitors.
Published in: Blood

Ligand: JBJ-04-125-02 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.59000015258789 pIC50
Reference (Journal): Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor.
Published in: Cancer Discov

Ligand: JBJ-09-063 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 10.079999923706055 pIC50
Reference (Journal): An allosteric inhibitor against the therapy-resistant mutant forms of EGFR in non-small cell lung cancer.
Published in: Nat Cancer

Ligand: JND3229 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.239999771118164 pIC50
Reference (Journal): Discovery of JND3229 as a New EGFR<sup>C797S</sup> Mutant Inhibitor with In Vivo Monodrug Efficacy.
Published in: ACS Med Chem Lett

Ligand: lapatinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2007), EMA (2008)
Primary target: yes
Median affinity: 8 pIC50
Reference (Journal): The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo.
Published in: Mol Cancer Ther

Ligand: lazertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: S. Korea (2021)
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Patent): Compounds and compositions for modulating EGFR mutant kinase activities.

Ligand: lifirafenib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.539999961853027 pIC50
Reference (Journal): BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers.
Published in: Mol Cancer Ther

Ligand: mavelertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.510000228881836 pIC50
Reference (Journal): Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Published in: J Med Chem

Ligand: mifanertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Patent): Aminoquinazoline derivative and use thereof in preparing anti-malignant tumor medicament

Ligand: MM-151 (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Optimizing properties of antireceptor antibodies using kinetic computational models and experiments.
Published in: Meth Enzymol

Ligand: MM-151 (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: no
Primary target: yes
Median affinity:  -
Reference (Journal): Enhanced Targeting of the EGFR Network with MM-151, an Oligoclonal Anti-EGFR Antibody Therapeutic.
Published in: Mol Cancer Ther

Ligand: mobocertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2021)
Primary target: no
Median affinity: 7 pIC50
Reference (Patent): Heteroaryl compounds for kinase inhibition

Ligand: MS154 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.739999771118164 pKd
Reference (Journal): Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
Published in: J Med Chem

Ligand: MS39 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.960000038146973 pKd
Reference (Journal): Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.
Published in: J Med Chem

Ligand: naquotinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Pyrazine carboxamide compound

Ligand: nazartinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9 pIC50
Reference (Patent): Egfr inhibitor forms

Ligand: necitumumab (Antibody)
Interaction type: Antibody
Action: Binding
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: yes
Median affinity: 9.489999771118164 pKd
Reference (Patent): Used in treating neoplastic diseases and hyperproliferative disorders.

Ligand: neratinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2017), EMA (2018)
Primary target: no
Median affinity: 7.039999961853027 pIC50
Reference (Journal): Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.
Published in: Cancer Res

Ligand: olmutinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: South Korea (2016)
Primary target: no
Median affinity:  pIC50
Reference (Patent): Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity

Ligand: orantinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 4 pIC50
Reference (Journal): 5-Substituted pyrido[2,3-d]pyrimidine, an inhibitor against three receptor tyrosine kinases.
Published in: Bioorg Med Chem Lett

Ligand: osimertinib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2015), EMA (2016)
Primary target: no
Median affinity: 6.309999942779541 pIC50
Reference (Journal): Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer.
Published in: J Hematol Oncol

Ligand: panitumumab (Antibody)
Interaction type: Antibody
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2006), EMA (2007)
Primary target: yes
Median affinity: 10.300000190734863 pKd
Reference (Journal): Preclinical and clinical evaluations of ABX-EGF, a fully human anti-epidermal growth factor receptor antibody.
Published in: Int J Radiat Oncol Biol Phys