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Assay Detail

CHEMBL2076234

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

Functional
TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing HeLa cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Solute carrier organic anion transporter family member 1A1 (CHEMBL1781859)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter.
Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL.
Am J Physiol (1996) 270 : F326 -F331
PubMed 8779894 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.31 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1628111 1 5.96
CHEMBL494753 ESTRONE SULFURIC ACID 4.0 1 5.89
CHEMBL1614647 1 5.89
CHEMBL2075012 1 5.80
CHEMBL2074598 1 5.62
CHEMBL2074651 1 5.42
CHEMBL135 ESTRADIOL 4.0 1 5.33
CHEMBL110739 CORTICOSTERONE 3.0 1 5.28
CHEMBL386630 TESTOSTERONE 4.0 1 5.27
CHEMBL193482 ESTRIOL 4.0 1 5.01
CHEMBL2074591 1 5.01
CHEMBL87285 ANDROSTERONE 1 4.97
CHEMBL1405 ESTRONE 4.0 1 4.80
CHEMBL2074705 ANDROSTERONE ACETATE 1 4.12
CHEMBL1627554 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1628111 Ki = 1100.0 nM 5.96
CHEMBL494753 ESTRONE SULFURIC ACID Ki = 1300.0 nM 5.89
CHEMBL1614647 Ki = 1300.0 nM 5.89
CHEMBL2075012 Ki = 1600.0 nM 5.80
CHEMBL2074598 Ki = 2400.0 nM 5.62
CHEMBL2074651 Ki = 3800.0 nM 5.42
CHEMBL135 ESTRADIOL Ki = 4700.0 nM 5.33
CHEMBL110739 CORTICOSTERONE Ki = 5300.0 nM 5.28
CHEMBL386630 TESTOSTERONE Ki = 5400.0 nM 5.27
CHEMBL193482 ESTRIOL Ki = 9800.0 nM 5.01
CHEMBL2074591 Ki = 9700.0 nM 5.01
CHEMBL87285 ANDROSTERONE Ki = 10600.0 nM 4.97
CHEMBL1405 ESTRONE Ki = 15700.0 nM 4.80
CHEMBL2074705 ANDROSTERONE ACETATE Ki = 76200.0 nM 4.12
CHEMBL1627554 Ki > 200000.0 nM -