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Assay Detail

CHEMBL5217992

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Functional
Antiproliferative activity against human NCI-H358
1
Total Activities
1
Compounds Tested
1
Activity Types
0
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

Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS<sup>G12C</sup> Inhibitor.
Bröker J, Waterson AG, Smethurst C, Kessler D, Böttcher J, Mayer M, Gmaschitz G, Phan J, Little A, Abbott JR, Sun Q, Gmachl M, Rudolph D, Arnhof H, Rumpel K, Savarese F, Gerstberger T, Mischerikow N, Treu M, Herdeis L, Wunberg T, Gollner A, Weinstabl H, Mantoulidis A, Krämer O, McConnell DB, W Fesik S.
J Med Chem (2022) 65 : 14614 -14629
PubMed 36300829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 8.22 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4535757 SOTORASIB 4.0 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4535757 SOTORASIB EC50 = 6.0 nM 8.22