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Assay Detail

CHEMBL5554804

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

Functional
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation measured after 3 days by MTT assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 1 — Organism
Curated By Autocuration

Target

HepG2 (CHEMBL395)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovering New Metallo-Deubiquitinase CSN5 Inhibitors by a Non-Catalytic Activity Assay Platform.
Yan YH, Wei LL, Wu JW, Wei SQ, Jiang YY, Yu JL, Yang LL, Li GB.
J Med Chem (2024) 67 : 14649 -14667
PubMed 39129245 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.90 5.53

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9470 SHIKONIN 1 5.53
CHEMBL28457 ALKANNIN 1 5.31
CHEMBL274056 NAPHTHAZALIN 1 5.30
CHEMBL403516 ACETYLSHIKONIN 1 5.19
CHEMBL9416 ISOBUTYLSHIKONIN 1 5.06
CHEMBL486627 DEOXYSHIKONIN 1 4.98
CHEMBL5566554 1 4.51
CHEMBL5574229 1 4.43
CHEMBL5572586 1 4.41
CHEMBL5575733 1 4.28
CHEMBL5569845 1 -
CHEMBL5572812 1 -
CHEMBL5573752 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9470 SHIKONIN IC50 = 2960.0 nM 5.53
CHEMBL28457 ALKANNIN IC50 = 4860.0 nM 5.31
CHEMBL274056 NAPHTHAZALIN IC50 = 4970.0 nM 5.30
CHEMBL403516 ACETYLSHIKONIN IC50 = 6480.0 nM 5.19
CHEMBL9416 ISOBUTYLSHIKONIN IC50 = 8730.0 nM 5.06
CHEMBL486627 DEOXYSHIKONIN IC50 = 10500.0 nM 4.98
CHEMBL5566554 IC50 = 30800.0 nM 4.51
CHEMBL5574229 IC50 = 37290.0 nM 4.43
CHEMBL5572586 IC50 = 39140.0 nM 4.41
CHEMBL5575733 IC50 = 52070.0 nM 4.28
CHEMBL5569845 IC50 > 100000.0 nM -
CHEMBL5572812 IC50 > 100000.0 nM -
CHEMBL5573752 IC50 > 100000.0 nM -