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Assay Detail

CHEMBL904912

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Functional
Antiproliferative activity against HMVE cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

An adamantyl-substituted retinoid-derived molecule that inhibits cancer cell growth and angiogenesis by inducing apoptosis and binds to small heterodimer partner nuclear receptor: effects of modifying its carboxylate group on apoptosis, proliferation, and protein-tyrosine phosphatase activity.
Dawson MI, Xia Z, Liu G, Ye M, Fontana JA, Farhana L, Patel BB, Arumugarajah S, Bhuiyan M, Zhang XK, Han YH, Stallcup WB, Fukushi J, Mustelin T, Tautz L, Su Y, Harris DL, Waleh N, Hobbs PD, Jong L, Chao WR, Schiff LJ, Sani BP.
J Med Chem (2007) 50 : 2622 -2639
PubMed 17489579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.59 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442016 ADAROTENE 1 7.00
CHEMBL1180 O-DEMETHYLATED ADAPALENE 1 6.52
CHEMBL176252 1 6.52
CHEMBL118143 1 6.30
CHEMBL225848 1 -
CHEMBL77961 1 -
CHEMBL225847 1 -
CHEMBL388758 1 -
CHEMBL38 TRETINOIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442016 ADAROTENE IC50 = 100.0 nM 7.00
CHEMBL1180 O-DEMETHYLATED ADAPALENE IC50 = 300.0 nM 6.52
CHEMBL176252 IC50 = 300.0 nM 6.52
CHEMBL118143 IC50 = 500.0 nM 6.30
CHEMBL225848 IC50 > 500.0 nM -
CHEMBL77961 IC50 > 500.0 nM -
CHEMBL225847 IC50 > 500.0 nM -
CHEMBL388758 IC50 > 500.0 nM -
CHEMBL38 TRETINOIN IC50 > 500.0 nM -