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Assay Detail

CHEMBL5156610

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Functional
Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition by Celltiter-Glo assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CWR22R
Confidence 1 — Organism
Curated By Autocuration

Target

CWR22R (CHEMBL612657)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer.
Xiang Q, Wang C, Wu T, Zhang C, Hu Q, Luo G, Hu J, Zhuang X, Zou L, Shen H, Wu X, Zhang Y, Kong X, Liu J, Xu Y.
J Med Chem (2022) 65 : 785 -810
PubMed 34962793 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.74 6.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4785363 INOBRODIB 1.0 1 6.38
CHEMBL5179520 1 5.69
CHEMBL5191045 1 5.62
CHEMBL5204688 1 5.53
CHEMBL3814752 1 5.50
CHEMBL5192803 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4785363 INOBRODIB IC50 = 420.0 nM 6.38
CHEMBL5179520 IC50 = 2040.0 nM 5.69
CHEMBL5191045 IC50 = 2390.0 nM 5.62
CHEMBL5204688 IC50 = 2930.0 nM 5.53
CHEMBL3814752 IC50 = 3130.0 nM 5.50
CHEMBL5192803 IC50 > 5000.0 nM -