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Assay Detail

CHEMBL5029807

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

Functional
Antiproliferative activity against human JJN-3R cells assessed as reduction in cell viability
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type JJN-3R
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of BET inhibitors as potential treatments for cancer: A new carboline chemotype.
Hill MD, Quesnelle C, Tokarski J, Fang H, Fanslau C, Haarhoff Z, Kramer M, Madari S, Wiebesiek A, Morrison J, Simmermacher-Mayer J, Sinz M, Westhouse R, Xie C, Zhao J, Huang L, Sheriff S, Yan C, Marsilio F, Everlof G, Zvyaga T, Lee F, Gavai AV, Degnan AP.
Bioorg Med Chem Lett (2021) 51 : 128376 -128376
PubMed 34560263 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.02 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5089688 1 8.74
CHEMBL5075294 1 8.62
CHEMBL4297458 EZOBRESIB 2.0 1 8.44
CHEMBL5084636 1 8.35
CHEMBL5084198 1 8.28
CHEMBL5086429 1 8.21
CHEMBL5091333 1 8.12
CHEMBL5090513 1 7.92
CHEMBL5080039 1 7.66
CHEMBL5090808 1 7.29
CHEMBL5069754 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5089688 IC50 = 1.8 nM 8.74
CHEMBL5075294 IC50 = 2.4 nM 8.62
CHEMBL4297458 EZOBRESIB IC50 = 3.6 nM 8.44
CHEMBL5084636 IC50 = 4.5 nM 8.35
CHEMBL5084198 IC50 = 5.3 nM 8.28
CHEMBL5086429 IC50 = 6.2 nM 8.21
CHEMBL5091333 IC50 = 7.6 nM 8.12
CHEMBL5090513 IC50 = 12.0 nM 7.92
CHEMBL5080039 IC50 = 22.0 nM 7.66
CHEMBL5090808 IC50 = 51.0 nM 7.29
CHEMBL5069754 IC50 = 260.0 nM 6.58