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Assay Detail

CHEMBL5226038

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

Functional
Antiproliferative activity against human MIA PaCa-2 cells harboring G12C mutant assessed as cell growth inhibition incubated for 7 days by Celltiter-Glo 3D cell viability assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MIA PaCa-2
Confidence 1 — Organism
Curated By Autocuration

Target

MIA PaCa-2 (CHEMBL614725)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Bioevaluation of Pyrido[2,3-<i>d</i>]pyrimidin-7-ones as Potent SOS1 Inhibitors.
Liu M, Zhou G, Su W, Gu Y, Gao M, Wang K, Huo R, Li Y, Zhou Z, Chen K, Zheng M, Zhang S, Xu T.
ACS Med Chem Lett (2023) 14 : 183 -190
PubMed 36793426 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.86 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5274267 1 7.56
CHEMBL4519023 1 7.52
CHEMBL5280533 1 7.13
CHEMBL5290547 1 7.04
CHEMBL5275216 1 7.04
CHEMBL5286601 1 6.81
CHEMBL5280431 1 6.80
CHEMBL5266985 1 6.72
CHEMBL5269963 1 6.50
CHEMBL5267612 1 6.47
CHEMBL5284292 1 6.37
CHEMBL5275839 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5274267 IC50 = 27.7 nM 7.56
CHEMBL4519023 IC50 = 30.0 nM 7.52
CHEMBL5280533 IC50 = 74.8 nM 7.13
CHEMBL5290547 IC50 = 92.0 nM 7.04
CHEMBL5275216 IC50 = 90.1 nM 7.04
CHEMBL5286601 IC50 = 156.0 nM 6.81
CHEMBL5280431 IC50 = 160.0 nM 6.80
CHEMBL5266985 IC50 = 190.0 nM 6.72
CHEMBL5269963 IC50 = 317.0 nM 6.50
CHEMBL5267612 IC50 = 340.0 nM 6.47
CHEMBL5284292 IC50 = 429.0 nM 6.37
CHEMBL5275839 IC50 = 459.0 nM 6.34