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Assay Detail

CHEMBL811900

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

Binding
Inhibitory activity against [125I]T3 binding to human TRbeta1 receptor
25
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Thyroid hormone receptor beta (CHEMBL1947)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.
Dow RL, Schneider SR, Paight ES, Hank RF, Chiang P, Cornelius P, Lee E, Newsome WP, Swick AG, Spitzer J, Hargrove DM, Patterson TA, Pandit J, Chrunyk BA, LeMotte PK, Danley DE, Rosner MH, Ammirati MJ, Simons SP, Schulte GK, Tate BF, DaSilva-Jardine P.
Bioorg Med Chem Lett (2003) 13 : 379 -382
PubMed 12565933 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 9.31 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL124126 1 10.70
CHEMBL125381 1 10.52
CHEMBL124205 2 10.40
CHEMBL413699 1 10.15
CHEMBL1544 LIOTHYRONINE 4.0 1 10.10
CHEMBL126693 1 10.00
CHEMBL125728 1 9.89
CHEMBL338602 3 9.80
CHEMBL123920 1 9.64
CHEMBL125946 1 9.55
CHEMBL125317 1 9.51
CHEMBL124039 1 9.40
CHEMBL333650 1 9.34
CHEMBL340158 1 9.34
CHEMBL125242 1 9.20
CHEMBL124318 1 9.19
CHEMBL124819 1 9.14
CHEMBL340490 1 8.72
CHEMBL56801 1 8.70
CHEMBL127338 1 7.89
CHEMBL124145 1 7.57
CHEMBL124844 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL124126 Ki = 0.02 nM 10.70
CHEMBL125381 Ki = 0.03 nM 10.52
CHEMBL124205 Ki = 0.04 nM 10.40
CHEMBL124205 Ki = 0.06 nM 10.22
CHEMBL413699 Ki = 0.07 nM 10.15
CHEMBL1544 LIOTHYRONINE Ki = 0.08 nM 10.10
CHEMBL126693 Ki = 0.1 nM 10.00
CHEMBL125728 Ki = 0.13 nM 9.89
CHEMBL338602 Ki = 0.16 nM 9.80
CHEMBL123920 Ki = 0.23 nM 9.64
CHEMBL125946 Ki = 0.28 nM 9.55
CHEMBL125317 Ki = 0.31 nM 9.51
CHEMBL338602 Ki = 0.37 nM 9.43
CHEMBL124039 Ki = 0.4 nM 9.40
CHEMBL333650 Ki = 0.46 nM 9.34
CHEMBL340158 Ki = 0.46 nM 9.34
CHEMBL338602 Ki = 0.59 nM 9.23
CHEMBL125242 Ki = 0.63 nM 9.20
CHEMBL124318 Ki = 0.64 nM 9.19
CHEMBL124819 Ki = 0.72 nM 9.14
CHEMBL340490 Ki = 1.9 nM 8.72
CHEMBL56801 Ki = 2.0 nM 8.70
CHEMBL127338 Ki = 13.0 nM 7.89
CHEMBL124145 Ki = 27.0 nM 7.57
CHEMBL124844 Ki = 10000.0 nM 5.00