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Assay Detail

CHEMBL5554813

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Functional
Antiproliferative activity against human A-375 cells assessed as inhibition of cell proliferation measured after 3 days by MTT assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-375
Confidence 1 — Organism
Curated By Autocuration

Target

A-375 (CHEMBL613859)
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 6 5.62 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9470 SHIKONIN 1 6.16
CHEMBL28457 ALKANNIN 1 5.85
CHEMBL9416 ISOBUTYLSHIKONIN 1 5.77
CHEMBL403516 ACETYLSHIKONIN 1 5.72
CHEMBL486627 DEOXYSHIKONIN 1 5.17
CHEMBL274056 NAPHTHAZALIN 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9470 SHIKONIN IC50 = 700.0 nM 6.16
CHEMBL28457 ALKANNIN IC50 = 1420.0 nM 5.85
CHEMBL9416 ISOBUTYLSHIKONIN IC50 = 1710.0 nM 5.77
CHEMBL403516 ACETYLSHIKONIN IC50 = 1910.0 nM 5.72
CHEMBL486627 DEOXYSHIKONIN IC50 = 6830.0 nM 5.17
CHEMBL274056 NAPHTHAZALIN IC50 = 8850.0 nM 5.05