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Assay Detail

CHEMBL3536010

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ADMET
Inhibition of OATP1B3-mediated [3H]estradiol 17beta-glucuronide uptake in human OATP1B3 expressing HEK293/PDZK1 cells by scintillation counting
3
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293/PDZK1
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Pharmacokinetics and hepatic uptake of eltrombopag, a novel platelet-increasing agent.
Takeuchi K, Sugiura T, Umeda S, Matsubara K, Horikawa M, Nakamichi N, Silver DL, Ishiwata N, Kato Y.
Drug Metab Dispos (2011) 39 : 1088 -1096
PubMed 21422191 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
Ki 1 4.59 4.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461101 ELTROMBOPAG 4.0 2 4.59
CHEMBL574431 SULFOBROMOPHTHALEIN -1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461101 ELTROMBOPAG Ki = 25600.0 nM 4.59
CHEMBL461101 ELTROMBOPAG Inhibition - % -
CHEMBL574431 SULFOBROMOPHTHALEIN Inhibition - % -