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Assay Detail

CHEMBL1781816

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Binding
Inhibition of mouse Oat1 expressed in Xenopus oocytes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 6 (CHEMBL5653)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Elucidation of common pharmacophores from analysis of targeted metabolites transported by the multispecific drug transporter-Organic anion transporter1 (Oat1).
Kouznetsova VL, Tsigelny IF, Nagle MA, Nigam SK.
Bioorg Med Chem (2011) 19 : 3320 -3340
PubMed 21571536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 4.16 4.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL461 HIPPURIC ACID 1 4.25
CHEMBL607712 4-HYDROXYPHENYLPYRUVIC ACID 1 4.14
CHEMBL1162488 PHENYLPYRUVATE 1 4.10
CHEMBL1162497 1 -
CHEMBL1162494 N-ACETYLASPARTIC ACID 1 -
CHEMBL1162489 1 -
CHEMBL1615211 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL461 HIPPURIC ACID Ki = 55600.0 nM 4.25
CHEMBL607712 4-HYDROXYPHENYLPYRUVIC ACID Ki = 73000.0 nM 4.14
CHEMBL1162488 PHENYLPYRUVATE Ki = 79000.0 nM 4.10
CHEMBL1162497 Ki = 3320000.0 nM -
CHEMBL1162494 N-ACETYLASPARTIC ACID Ki = 840000.0 nM -
CHEMBL1162489 Ki = 223000.0 nM -
CHEMBL1615211 Ki = 840000.0 nM -