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Assay Detail

CHEMBL2078136

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Functional
TP_TRANSPORTER: inhibition of L-T4 uptake in Oatp14-expressing HEK293 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier.
Tohyama K, Kusuhara H, Sugiyama Y.
Endocrinology (2004) 145 : 4384 -4391
PubMed 15166123 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.44 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559 DEXTROTHYROXINE 4.0 1 6.57
CHEMBL1743304 REVERSE TRIIODOTHYRONINE 1 6.04
CHEMBL41632 TIRATRICOL 3.0 1 5.67
CHEMBL1544 LIOTHYRONINE 4.0 1 4.62
CHEMBL494753 ESTRONE SULFURIC ACID 4.0 1 4.28
CHEMBL1697724 ESTRADIOL 17B GLUCURONIDE 1 -
CHEMBL224867 TAUROCHOLIC ACID 1 -
CHEMBL897 PROBENECID 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559 DEXTROTHYROXINE Ki = 270.0 nM 6.57
CHEMBL1743304 REVERSE TRIIODOTHYRONINE Ki = 910.0 nM 6.04
CHEMBL41632 TIRATRICOL Ki = 2150.0 nM 5.67
CHEMBL1544 LIOTHYRONINE Ki = 24200.0 nM 4.62
CHEMBL494753 ESTRONE SULFURIC ACID Ki = 53100.0 nM 4.28
CHEMBL1697724 ESTRADIOL 17B GLUCURONIDE Ki > 100000.0 nM -
CHEMBL224867 TAUROCHOLIC ACID Ki = 109000.0 nM -
CHEMBL897 PROBENECID Ki = 293000.0 nM -