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Assay Detail

CHEMBL4224366

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

Functional
Induction of apoptosis in human HT-29 cells harboring BRAF/KRAS mutant by caspase activation assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Intermediate

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.
Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R.
Bioorg Med Chem Lett (2018) 28 : 2029 -2034
PubMed 29748051 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.07 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3645231 1 7.10
CHEMBL3645235 1 7.10
CHEMBL3590107 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3645231 IC50 = 79.0 nM 7.10
CHEMBL3645235 IC50 = 80.0 nM 7.10
CHEMBL3590107 IC50 = 96.0 nM 7.02