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Assay Detail

CHEMBL896603

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

Binding
Activity against TRAF-alpha-1 expressed in CHOK1 cells by alkaline phosphatase reporter gene assay
25
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.
Garg N, Li YL, Garcia Collazo AM, Litten C, Ryono DE, Zhang M, Caringal Y, Brigance RP, Meng W, Washburn WN, Agback P, Mellström K, Rehnmark S, Rahimi-Ghadim M, Norin T, Grynfarb M, Sandberg J, Grover G, Malm J.
Bioorg Med Chem Lett (2007) 17 : 4131 -4134
PubMed 17543524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.86 9.42
Activity 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39174 1 9.42
CHEMBL236289 2 8.85
CHEMBL236291 2 8.82
CHEMBL41036 1 8.77
CHEMBL391512 2 8.64
CHEMBL391367 2 8.14
CHEMBL440975 2 7.82
CHEMBL236499 2 7.77
CHEMBL393201 2 7.19
CHEMBL236498 2 7.18
CHEMBL236080 2 6.99
CHEMBL236500 2 6.77
CHEMBL391513 2 5.82
CHEMBL236290 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39174 EC50 = 0.38 nM 9.42
CHEMBL236289 EC50 = 1.4 nM 8.85
CHEMBL236291 EC50 = 1.5 nM 8.82
CHEMBL41036 EC50 = 1.7 nM 8.77
CHEMBL391512 EC50 = 2.3 nM 8.64
CHEMBL391367 EC50 = 7.2 nM 8.14
CHEMBL440975 EC50 = 15.0 nM 7.82
CHEMBL236499 EC50 = 17.0 nM 7.77
CHEMBL393201 EC50 = 65.0 nM 7.19
CHEMBL236498 EC50 = 66.0 nM 7.18
CHEMBL236080 EC50 = 103.0 nM 6.99
CHEMBL236500 EC50 = 170.0 nM 6.77
CHEMBL391513 EC50 = 1500.0 nM 5.82
CHEMBL391513 Activity = 72.0 % -
CHEMBL236498 Activity = 74.0 % -
CHEMBL236291 Activity = 65.0 % -
CHEMBL236499 Activity = 78.0 % -
CHEMBL391512 Activity = 88.0 % -
CHEMBL393201 Activity = 21.0 % -
CHEMBL236289 Activity = 78.0 % -
CHEMBL236500 Activity = 13.0 % -
CHEMBL440975 Activity = 83.0 % -
CHEMBL236080 Activity = 75.0 % -
CHEMBL391367 Activity = 81.0 % -
CHEMBL236290 EC50 - -