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Assay Detail

CHEMBL969780

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

ADMET
Growth inhibition of HMVE cells after 72 hrs by alamar blue method
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HMVE
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Adamantyl-substituted retinoid-derived molecules that interact with the orphan nuclear receptor small heterodimer partner: effects of replacing the 1-adamantyl or hydroxyl group on inhibition of cancer cell growth, induction of cancer cell apoptosis, and inhibition of SRC homology 2 domain-containing protein tyrosine phosphatase-2 activity.
Dawson MI, Xia Z, Jiang T, Ye M, Fontana JA, Farhana L, Patel B, Xue LP, Bhuiyan M, Pellicciari R, Macchiarulo A, Nuti R, Zhang XK, Han YH, Tautz L, Hobbs PD, Jong L, Waleh N, Chao WR, Feng GS, Pang Y, Su Y.
J Med Chem (2008) 51 : 5650 -5662
PubMed 18759424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.49 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442016 ADAROTENE 1 7.00
CHEMBL1180 O-DEMETHYLATED ADAPALENE 1 6.48
CHEMBL116238 1 6.47
CHEMBL517254 1 6.30
CHEMBL462681 1 6.22
CHEMBL495117 1 -
CHEMBL461830 1 -
CHEMBL459492 1 -
CHEMBL459491 1 -
CHEMBL459947 1 -
CHEMBL459738 1 -
CHEMBL461003 1 -
CHEMBL517276 1 -
CHEMBL461647 1 -
CHEMBL516618 1 -
CHEMBL1265 ADAPALENE 4.0 1 -
CHEMBL516502 1 -
CHEMBL38 TRETINOIN 4.0 1 -
CHEMBL118143 1 -
CHEMBL492492 1 -
CHEMBL176252 1 -
CHEMBL524028 1 -
CHEMBL493905 1 -
CHEMBL74218 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442016 ADAROTENE IC50 = 100.0 nM 7.00
CHEMBL1180 O-DEMETHYLATED ADAPALENE IC50 = 330.0 nM 6.48
CHEMBL116238 IC50 = 340.0 nM 6.47
CHEMBL517254 IC50 = 500.0 nM 6.30
CHEMBL462681 IC50 = 600.0 nM 6.22
CHEMBL495117 IC50 - -
CHEMBL461830 IC50 > 500.0 nM -
CHEMBL459492 IC50 - -
CHEMBL459491 IC50 > 500.0 nM -
CHEMBL459947 IC50 > 500.0 nM -
CHEMBL459738 IC50 - -
CHEMBL461003 IC50 > 500.0 nM -
CHEMBL517276 IC50 > 500.0 nM -
CHEMBL461647 IC50 - -
CHEMBL516618 IC50 - -
CHEMBL1265 ADAPALENE IC50 - -
CHEMBL516502 IC50 > 500.0 nM -
CHEMBL38 TRETINOIN IC50 > 500.0 nM -
CHEMBL118143 IC50 > 500.0 nM -
CHEMBL492492 IC50 - -
CHEMBL176252 IC50 - -
CHEMBL524028 IC50 - -
CHEMBL493905 IC50 > 500.0 nM -
CHEMBL74218 IC50 > 500.0 nM -