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Assay Detail

CHEMBL4144044

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

Functional
Antiproliferative activity against human RPMI8226 cells after 72 hrs by Cell-TiterGlo assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type RPMI-8226
Confidence 1 — Organism
Curated By Intermediate

Target

RPMI-8226 (CHEMBL614882)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors.
Sharp PP, Garnier JM, Hatfaludi T, Xu Z, Segal D, Jarman KE, Jousset H, Garnham A, Feutrill JT, Cuzzupe A, Hall P, Taylor S, Walkley CR, Tyler D, Dawson MA, Czabotar P, Wilks AF, Glaser S, Huang DCS, Burns CJ.
ACS Med Chem Lett (2017) 8 : 1298 -1303
PubMed 29259751 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.36 6.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2132936 1 6.59
CHEMBL4177080 1 6.30
CHEMBL4168815 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2132936 EC50 = 258.0 nM 6.59
CHEMBL4177080 EC50 = 495.0 nM 6.30
CHEMBL4168815 EC50 = 631.0 nM 6.20