Target family: RAS subfamily (type: enzyme)
Target: KRAS

Ligand: ASP2453 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Characterisation of a novel KRAS G12C inhibitor ASP2453 that shows potent anti-tumour activity in KRAS G12C-mutated preclinical models.
Published in: Br J Cancer

Ligand: AZD4625 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRAS<sup>G12C</sup>.
Published in: J Med Chem

Ligand: BI-0474 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS<sup>G12C</sup> Inhibitor.
Published in: J Med Chem

Ligand: BI-2493 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pKd
Reference (Journal): Pan-KRAS inhibitor disables oncogenic signalling and tumour growth.
Published in: Nature

Ligand: compound 25 [PMID: 32023060] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS<sup>G12C</sup>.
Published in: J Med Chem

Ligand: divarasib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Patent): Fused ring compounds

Ligand: ERAS-5024 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 9.069999694824219 pIC50
Reference (Journal): Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors.
Published in: ACS Med Chem Lett

Ligand: ERAS-5024 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.40999984741211 pIC50
Reference (Journal): Structure-Based Design and Synthesis of Potent and Selective KRAS G12D Inhibitors.
Published in: ACS Med Chem Lett

Ligand: fulzerasib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pIC50
Reference (Patent): Substituted heterocyclic fused cyclic compound, preparation method therefor and pharmaceutical use thereof

Ligand: lonafarnib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2020), EMA (2022)
Primary target: no
Median affinity: 8.279999732971191 pIC50
Reference (Journal): Antitumor activity of SCH 66336, an orally bioavailable tricyclic inhibitor of farnesyl protein transferase, in human tumor xenograft models and wap-ras transgenic mice.
Published in: Cancer Res

Ligand: LUNA18 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.850000381469727 pIC50
Reference (Journal): Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor.
Published in: J Am Chem Soc

Ligand: LUNA18 (Peptide)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.369999885559082 pKd
Reference (Journal): Development of Orally Bioavailable Peptides Targeting an Intracellular Protein: From a Hit to a Clinical KRAS Inhibitor.
Published in: J Am Chem Soc

Ligand: LY3499446 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Patent): Compound for inhibiting krasg12c mutant protein, preparation method therefor, and use thereof

Ligand: MRTX1133 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 12.699999809265137 pKd
Reference (Journal): Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS<sup>G12D</sup> Inhibitor.
Published in: J Med Chem

Ligand: opnurasib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 7.769999980926514 pIC50
Reference (Patent): Pyrazolyl derivatives useful as anti-cancer agents

Ligand: RMC-6236 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.809999942779541 pKd
Reference (Journal): Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Published in: Cancer Discov

Ligand: RMC-6236 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.880000114440918 pKd
Reference (Journal): Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Published in: Cancer Discov

Ligand: RMC-6236 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.440000057220459 pKd
Reference (Journal): Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers.
Published in: Cancer Discov

Ligand: ARS-1620 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.920000076293945 pIC50
Reference (Journal): Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor.
Published in: Cell

Ligand: sotorasib (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2021), EMA (2022)
Primary target: no
Median affinity:  -
Reference (Journal): Discovery of a Covalent Inhibitor of KRAS<sup>G12C</sup> (AMG 510) for the Treatment of Solid Tumors.
Published in: J Med Chem