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Assay Detail

CHEMBL5337474

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

Functional
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 to 96 hrs by alamar blue assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Autocuration

Target

MDA-MB-231 (CHEMBL400)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery and optimization of dihydropteridone derivatives as novel PLK1 and BRD4 dual inhibitor for the treatment of cancer.
Liu J, Huang J, Wang K, Li Y, Li C, Zhu Y, He X, Zhang Y, Zhao Y, Hu C, Xi Z, Tong M, Li Z, Gong P, Hou Y.
Bioorg Med Chem (2024) 101 : 117609 -117609
PubMed 38364599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.57 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5419367 1 8.04
CHEMBL5401381 1 7.91
CHEMBL5418129 1 7.86
CHEMBL5395480 1 7.77
CHEMBL5429440 1 7.76
CHEMBL5417495 1 7.67
CHEMBL5416208 1 7.64
CHEMBL513909 BI-2536 2.0 1 7.54
CHEMBL5421238 1 7.46
CHEMBL5403358 1 7.24
CHEMBL5428087 1 7.22
CHEMBL5394764 1 7.21
CHEMBL5415794 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5419367 IC50 = 9.22 nM 8.04
CHEMBL5401381 IC50 = 12.3 nM 7.91
CHEMBL5418129 IC50 = 13.8 nM 7.86
CHEMBL5395480 IC50 = 16.9 nM 7.77
CHEMBL5429440 IC50 = 17.3 nM 7.76
CHEMBL5417495 IC50 = 21.3 nM 7.67
CHEMBL5416208 IC50 = 22.7 nM 7.64
CHEMBL513909 BI-2536 IC50 = 28.9 nM 7.54
CHEMBL5421238 IC50 = 35.1 nM 7.46
CHEMBL5403358 IC50 = 58.2 nM 7.24
CHEMBL5428087 IC50 = 60.4 nM 7.22
CHEMBL5394764 IC50 = 61.3 nM 7.21
CHEMBL5415794 IC50 = 78.3 nM 7.11