Assay Detail

CHEMBL4701896

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Binding

Inhibition of KRAS G12C mutant in human MIA PaCa-2 cells assessed as reduction in p-ERK levels

ChEMBL ↗

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Target

GTPase KRas (CHEMBL2189121) ↗

Open DB target context

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GTPase KRas (CHEMBL2189121) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target GTPase KRas

CHEMBL2189121

Anchored from Assay target.

Protein identity GTPase KRas

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
Cell Type	MIA PaCa-2
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

GTPase KRas (CHEMBL2189121) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.

LaMarche MJ,Acker M,Argintaru A,Bauer D,Boisclair J,Chan H,Chen CH,Chen YN,Chen Z,Deng Z,Dore M,Dunstan D,Fan J,Fekkes P,Firestone B,Fodor M,Garcia-Fortanet J,Fortin PD,Fridrich C,Giraldes J,Glick M,Grunenfelder D,Hao HX,Hentemann M,Ho S,Jouk A,Kang ZB,Karki R,Kato M,Keen N,Koenig R,LaBonte LR,Larrow J,Liu G,Liu S,Majumdar D,Mathieu S,Meyer MJ,Mohseni M,Ntaganda R,Palermo M,Perez L,Pu M,Ramsey T,Reilly J,Sarver P,Sellers WR,Sendzik M,Shultz MD,Slisz J,Slocum K,Smith T,Spence S,Stams T,Straub C,Tamez V,Toure BB,Towler C,Wang P,Wang H,Williams SL,Yang F,Yu B,Zhang JH,Zhu S
J Med Chem (2020) 63 : 13578 -13594
PubMed 32910655 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	8.00	8.00

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4594350	ADAGRASIB	4.0	1	8.00

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4594350	ADAGRASIB	IC50	=	10.0	nM	8.00