Assay Detail

CHEMBL5335134

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional

Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay

ChEMBL ↗

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Target

NCI-H358 (CHEMBL614135) ↗

Open DB target context

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NCI-H358 (CHEMBL614135) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target NCI-H358

CHEMBL614135

Anchored from Assay target.

Protein identity NCI-H358

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	Functional
Organism	Homo sapiens
Cell Type	NCI-H358
Confidence	1 — Organism
Curated By	Autocuration

Target

NCI-H358 (CHEMBL614135) ↗

Type	CELL-LINE
Organism	Homo sapiens

Publication

Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRAS<sup>G12C</sup> with Demonstrable CNS Penetration.

Kettle JG, Bagal SK, Barratt D, Bodnarchuk MS, Boyd S, Braybrooke E, Breed J, Cassar DJ, Cosulich S, Davies M, Davies NL, Deng C, Eatherton A, Evans L, Feron LJ, Fillery S, Gleave ES, Goldberg FW, Cortés González MA, Guerot C, Haider A, Harlfinger S, Howells R, Jackson A, Johnström P, Kemmitt PD, Koers A, Kondrashov M, Lamont GM, Lamont S, Lewis HJ, Liu L, Mylrea M, Nash S, Niedbala MJ, Peter A, Phillips C, Pike K, Raubo P, Robb GR, Ross S, Sanders MG, Schou M, Simpson I, Steward O.
J Med Chem (2023) 66 : 9147 -9160
PubMed 37395055 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	3	8.38	9.00

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4535757	SOTORASIB	4.0	1	9.00
CHEMBL4594350	ADAGRASIB	4.0	1	8.22
CHEMBL5417514	—	—	1	7.92

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4535757	SOTORASIB	IC50	=	1.0	nM	9.00
CHEMBL4594350	ADAGRASIB	IC50	=	6.0	nM	8.22
CHEMBL5417514	—	IC50	=	12.0	nM	7.92