Assay Detail

CHEMBL5149552

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Binding

Inhibition of human recombinant SOS2 catalytic domain/human recombinant GST-KRAS G12C mutant expressed in Escherichia coli assessed as inhibition of interaction

ChEMBL ↗

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Target

Unchecked (CHEMBL612545) ↗

Open DB target context

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Unchecked (CHEMBL612545) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Unchecked

CHEMBL612545

Anchored from Assay target.

Protein identity Unchecked

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	0 — Uncurated / Unknown
Curated By	Autocuration

Target

Unchecked (CHEMBL612545) ↗

Type

UNCHECKED

Publication

Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.

Ketcham JM, Haling J, Khare S, Bowcut V, Briere DM, Burns AC, Gunn RJ, Ivetac A, Kuehler J, Kulyk S, Laguer J, Lawson JD, Moya K, Nguyen N, Rahbaek L, Saechao B, Smith CR, Sudhakar N, Thomas NC, Vegar L, Vanderpool D, Wang X, Yan L, Olson P, Christensen JG, Marx MA.
J Med Chem (2022) 65 : 9678 -9690
PubMed 35833726 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	7.68	7.68

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4535474	BAY-293	—	1	7.68

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4535474	BAY-293	IC50	=	21.0	nM	7.68