Assay Detail

CHEMBL2154120

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ADMET

Inhibition of human OCT2 expressed in HEK-293-Flp-In cells incubated for 3 mins by ASP+ substrate uptake assay

ChEMBL ↗

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Target

Solute carrier family 22 member 2 (CHEMBL1743122) ↗

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Solute carrier family 22 member 2 (CHEMBL1743122) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Solute carrier family 22 member 2

CHEMBL1743122

Anchored from Assay target.

Protein identity Solute carrier family 22 member 2

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Solute carrier family 22 member 2 (CHEMBL1743122) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.

Kido Y, Matsson P, Giacomini KM.
J Med Chem (2011) 54 : 4548 -4558
PubMed 21599003 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	7	5.69	6.22

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL11	IMIPRAMINE	4.0	1	6.22
CHEMBL95	TACRINE	4.0	1	6.17
CHEMBL46	ONDANSETRON	4.0	1	6.05
CHEMBL900	ORPHENADRINE	4.0	1	5.60
CHEMBL932	DIPYRIDAMOLE	4.0	1	5.58
CHEMBL517	DISOPYRAMIDE	4.0	1	5.54
CHEMBL30	CIMETIDINE	4.0	1	4.64

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL11	IMIPRAMINE	IC50	=	600.0	nM	6.22
CHEMBL95	TACRINE	IC50	=	680.0	nM	6.17
CHEMBL46	ONDANSETRON	IC50	=	890.0	nM	6.05
CHEMBL900	ORPHENADRINE	IC50	=	2500.0	nM	5.60
CHEMBL932	DIPYRIDAMOLE	IC50	=	2600.0	nM	5.58
CHEMBL517	DISOPYRAMIDE	IC50	=	2900.0	nM	5.54
CHEMBL30	CIMETIDINE	IC50	=	23000.0	nM	4.64