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Assay Detail

CHEMBL5125682

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

Functional
Antiproliferative activity against human JJN-3R cells assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
14
Total Activities
14
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: Optimization of Pharmacokinetic Properties.
Hill MD, Fang H, Norris D, Delucca GV, Huang H, DeBenedetto M, Quesnelle C, Schmitz WD, Tokarski JS, Sheriff S, Yan C, Fanslau C, Haarhoff Z, Huang C, Kramer M, Madari S, Menard K, Monereau L, Morrison J, Raghavan N, Shields EE, Simmermacher-Mayer J, Sinz M, Tye CK, Westhouse R, Xie C, Zhang H, Zhang L, Zvyaga T, Lee F, Gavai AV, Degnan AP.
ACS Med Chem Lett (2022) 13 : 1165 -1171
PubMed 35859878 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 8.17 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5209210 1 8.52
CHEMBL4297458 EZOBRESIB 2.0 1 8.44
CHEMBL5207310 1 8.40
CHEMBL5204989 1 8.30
CHEMBL5209351 1 8.30
CHEMBL4077176 1 8.30
CHEMBL4859923 1 8.22
CHEMBL5185824 1 8.22
CHEMBL5189057 1 8.15
CHEMBL5206537 1 8.15
CHEMBL5201345 1 8.05
CHEMBL5171108 1 8.00
CHEMBL5179686 1 7.89
CHEMBL5172933 1 7.41

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5209210 IC50 = 3.0 nM 8.52
CHEMBL4297458 EZOBRESIB IC50 = 3.6 nM 8.44
CHEMBL5207310 IC50 = 4.0 nM 8.40
CHEMBL5204989 IC50 = 5.0 nM 8.30
CHEMBL5209351 IC50 = 5.0 nM 8.30
CHEMBL4077176 IC50 = 5.0 nM 8.30
CHEMBL4859923 IC50 = 6.0 nM 8.22
CHEMBL5185824 IC50 = 6.0 nM 8.22
CHEMBL5189057 IC50 = 7.0 nM 8.15
CHEMBL5206537 IC50 = 7.0 nM 8.15
CHEMBL5201345 IC50 = 9.0 nM 8.05
CHEMBL5171108 IC50 = 10.0 nM 8.00
CHEMBL5179686 IC50 = 13.0 nM 7.89
CHEMBL5172933 IC50 = 39.0 nM 7.41